DGIdb - ERBB2 Gene Record

ERBB2 2064 Druggable GenomeClinically ActionableDrug Resistance

Alternate Names:

2064
ERB-B2 RECEPTOR TYROSINE KINASE 2
ERBB2
CD340
HER-2
HER-2/neu
HER2
MLN 19
NEU
NGL
TKR1
164870
3430
ENSG00000141736
OTTHUMG00000179300
P04626
RECEPTOR TYROSINE-PROTEIN KINASE ERBB-2
ERBB2_HUMAN
HER2 (ERBB2/neu)
EGFR (HER1/ERBB1)HER2 (ERBB2/neu)HER3 (ERBB3)
EGFR (HER1/ERBB1)HER2 (ERBB2/neu)HER4 (ERBB4)
MLN19
Metastatic lymph node gene 19 protein
Proto-oncogene Neu
Proto-oncogene c-ErbB-2
Tyrosine kinase-type cell surface receptor HER2
p185erbB2
CD_antigen=CD340
20
2019
NP_001005862
NM_001005862
PA27844
RECEPTOR TYROSINE-PROTEIN KINASE ERBB-2 PRECURSOR (EC 2.7.1.112) (P185ERBB2) (C-ERBB-2) (NEU PROTO-ONCOGENE) (TYROSINE KINASE-TYPE CELL SURFACE RECEPTOR HER2) (MLN 19). [SOURCE:UNIPROT/SWISSPROT;ACC:P04626]
Erbb2 tyrosine kinase receptor
T14597

Gene Info:

Interpro Name	Serine-threonine/tyrosine-protein kinase catalytic domain
Interpro Type	Domain
Interpro Short Name	Ser-Thr/Tyr_kinase_cat_dom
Interpro Acc	IPR001245
Uniprot Evidence	1: Evidence at protein level
Human Readable Name	DRUGGABLE GENOME
Uniprot Status	Swiss-Prot
Human Readable Name	KINASE
Initial Gene Query	HER2/ErbB2
Counted Citations from 1950-2000	6422
Target Subclass	EGFR
Target Subclass	Kinase
Target Main Class	Receptors
Transmembrane Helix Count	1
GuideToPharmacology Gene Category Name	Type I RTKs: ErbB (epidermal growth factor) receptor family
GuideToPharmacology Gene Category ID	320
Target Class	Receptors
Target Subclass	EC:2.7.10.1
Gene Biotype	PROTEIN_CODING

(28 More Sources)

Gene Categories: Category Details

KINASE
TYROSINE KINASE
DRUG RESISTANCE
DRUGGABLE GENOME
CLINICALLY ACTIONABLE

Publications:

Zhang et al., 1998, Tyrosine kinase inhibitors, emodin and its derivative repress HER-2/neu-induced cellular transformation and metastasis-associated properties., Oncogene
Soria et al., 2012, Phase I safety, pharmacokinetic and pharmacodynamic trial of BMS-599626 (AC480), an oral pan-HER receptor tyrosine kinase inhibitor, in patients with advanced solid tumors., Ann. Oncol.
Gavai et al., 2009, Discovery and preclinical evaluation of [4-[[1-(3-fluorophenyl)methyl]-1H-indazol-5-ylamino]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]carbamic acid, (3S)-3-morpholinylmethyl ester (BMS-599626), a selective and orally efficacious inhibitor of human epidermal growth factor receptor 1 and 2 kinases., J. Med. Chem.
Scott et al., 1991, The effects of flosequinan on regional blood flow in normal man., Br J Clin Pharmacol
Lorenzen et al., 2015, Lapatinib versus lapatinib plus capecitabine as second-line treatment in human epidermal growth factor receptor 2-amplified metastatic gastro-oesophageal cancer: a randomised phase II trial of the Arbeitsgemeinschaft Internistische Onkologie., Eur. J. Cancer
Kavuri et al., 2015, HER2 activating mutations are targets for colorectal cancer treatment., Cancer Discov
Greulich et al., 2012, Functional analysis of receptor tyrosine kinase mutations in lung cancer identifies oncogenic extracellular domain mutations of ERBB2., Proc. Natl. Acad. Sci. U.S.A.
Grellety et al., 2016, A clinical case of invasive lobular breast carcinoma with ERBB2 and CDH1 mutations presenting a dramatic response to anti-HER2-directed therapy., Ann. Oncol.
Boulbes et al., 2015, HER family kinase domain mutations promote tumor progression and can predict response to treatment in human breast cancer., Mol Oncol
Sartore-Bianchi et al., 2016, Dual-targeted therapy with trastuzumab and lapatinib in treatment-refractory, KRAS codon 12/13 wild-type, HER2-positive metastatic colorectal cancer (HERACLES): a proof-of-concept, multicentre, open-label, phase 2 trial., Lancet Oncol.
Manole et al., 2016, JNK Pathway Activation Modulates Acquired Resistance to EGFR/HER2-Targeted Therapies., Cancer Res.
Witkiewicz et al., 2014, CDK4/6 inhibition provides a potent adjunct to Her2-targeted therapies in preclinical breast cancer models., Genes Cancer
Clavarezza et al., 2016, Dual Block with Lapatinib and Trastuzumab Versus Single-Agent Trastuzumab Combined with Chemotherapy as Neoadjuvant Treatment of HER2-Positive Breast Cancer: A Meta-analysis of Randomized Trials., Clin. Cancer Res.
Satoh et al., 2014, Lapatinib plus paclitaxel versus paclitaxel alone in the second-line treatment of HER2-amplified advanced gastric cancer in Asian populations: TyTAN--a randomized, phase III study., J. Clin. Oncol.
Johnston et al., 2009, Lapatinib combined with letrozole versus letrozole and placebo as first-line therapy for postmenopausal hormone receptor-positive metastatic breast cancer., J. Clin. Oncol.
Wisinski et al., 2016, Phase I Study of an AKT Inhibitor (MK-2206) Combined with Lapatinib in Adult Solid Tumors Followed by Dose Expansion in Advanced HER2+ Breast Cancer., Clin. Cancer Res.
Baselga et al., 2016, Relationship between Tumor Biomarkers and Efficacy in EMILIA, a Phase III Study of Trastuzumab Emtansine in HER2-Positive Metastatic Breast Cancer., Clin. Cancer Res.
Guarneri et al., 2015, Prospective Biomarker Analysis of the Randomized CHER-LOB Study Evaluating the Dual Anti-HER2 Treatment With Trastuzumab and Lapatinib Plus Chemotherapy as Neoadjuvant Therapy for HER2-Positive Breast Cancer., Oncologist
Li et al., 2014, Modulation of ErbB2 blockade in ErbB2-positive cancers: the role of ErbB2 Mutations and PHLDA1., PLoS ONE
Rexer et al., 2013, Human breast cancer cells harboring a gatekeeper T798M mutation in HER2 overexpress EGFR ligands and are sensitive to dual inhibition of EGFR and HER2., Clin. Cancer Res.
de Martino et al., 2014, Impact of ERBB2 mutations on in vitro sensitivity of bladder cancer to lapatinib., Cancer Biol. Ther.
Biswas et al., 2016, Genomic profiling of multiple sequentially acquired tumor metastatic sites from an "exceptional responder" lung adenocarcinoma patient reveals extensive genomic heterogeneity and novel somatic variants driving treatment response., Cold Spring Harb Mol Case Stud
Zuo et al., 2016, Dual Characteristics of Novel HER2 Kinase Domain Mutations in Response to HER2-Targeted Therapies in Human Breast Cancer., Clin. Cancer Res.
Morrison Joly et al., 2016, Rictor/mTORC2 Drives Progression and Therapeutic Resistance of HER2-Amplified Breast Cancers., Cancer Res.
Hecht et al., 2016, Lapatinib in Combination With Capecitabine Plus Oxaliplatin in Human Epidermal Growth Factor Receptor 2-Positive Advanced or Metastatic Gastric, Esophageal, or Gastroesophageal Adenocarcinoma: TRIO-013/LOGiC--A Randomized Phase III Trial., J. Clin. Oncol.
Kotschy et al., 2016, The MCL1 inhibitor S63845 is tolerable and effective in diverse cancer models., Nature
Leto et al., 2015, Sustained Inhibition of HER3 and EGFR Is Necessary to Induce Regression of HER2-Amplified Gastrointestinal Carcinomas., Clin. Cancer Res.
Bertotti et al., 2011, A molecularly annotated platform of patient-derived xenografts ("xenopatients") identifies HER2 as an effective therapeutic target in cetuximab-resistant colorectal cancer., Cancer Discov
Wainberg et al., 2010, Lapatinib, a dual EGFR and HER2 kinase inhibitor, selectively inhibits HER2-amplified human gastric cancer cells and is synergistic with trastuzumab in vitro and in vivo., Clin. Cancer Res.
Kwak et al., 2015, Molecular Heterogeneity and Receptor Coamplification Drive Resistance to Targeted Therapy in MET-Amplified Esophagogastric Cancer., Cancer Discov
Secrier et al., 2016, Mutational signatures in esophageal adenocarcinoma define etiologically distinct subgroups with therapeutic relevance., Nat. Genet.
Bose et al., 2013, Activating HER2 mutations in HER2 gene amplification negative breast cancer., Cancer Discov
Kancha et al., 2011, Differential sensitivity of ERBB2 kinase domain mutations towards lapatinib., PLoS ONE
Trowe et al., 2008, EXEL-7647 inhibits mutant forms of ErbB2 associated with lapatinib resistance and neoplastic transformation., Clin. Cancer Res.
Pan et al., 2015, Development and Characterization of Bladder Cancer Patient-Derived Xenografts for Molecularly Guided Targeted Therapy., PLoS ONE
Hanker et al., 2013, Mutant PIK3CA accelerates HER2-driven transgenic mammary tumors and induces resistance to combinations of anti-HER2 therapies., Proc. Natl. Acad. Sci. U.S.A.
Kim et al., 2008, The growth inhibitory effect of lapatinib, a dual inhibitor of EGFR and HER2 tyrosine kinase, in gastric cancer cell lines., Cancer Lett.
Cancer Cell Line Encyclopedia Consortium. et al., 2015, Pharmacogenomic agreement between two cancer cell line data sets., Nature
Lyu A et al., 2014, Design and synthesis of Lapatinib derivatives containing a branched side chain as HER1/HER2 targeting antitumor drug candidates., Eur J Med Chem
Sridhar J et al., 2014, Identification of quinones as HER2 inhibitors for the treatment of trastuzumab resistant breast cancer., Bioorg Med Chem Lett
Ali et al., 2014, Response of an ERBB2-mutated inflammatory breast carcinoma to human epidermal growth factor receptor 2-targeted therapy., J. Clin. Oncol.
Lee et al., 2006, Somatic mutations of ERBB2 kinase domain in gastric, colorectal, and breast carcinomas., Clin. Cancer Res.
Chang et al., 2016, Identifying recurrent mutations in cancer reveals widespread lineage diversity and mutational specificity., Nat. Biotechnol.
MacConaill et al., 2014, Prospective enterprise-level molecular genotyping of a cohort of cancer patients., J Mol Diagn
Geyer et al., 2006, Lapatinib plus capecitabine for HER2-positive advanced breast cancer., N. Engl. J. Med.
Xia et al., 2005, Combining lapatinib (GW572016), a small molecule inhibitor of ErbB1 and ErbB2 tyrosine kinases, with therapeutic anti-ErbB2 antibodies enhances apoptosis of ErbB2-overexpressing breast cancer cells., Oncogene
Baselga et al., 2012, Lapatinib with trastuzumab for HER2-positive early breast cancer (NeoALTTO): a randomised, open-label, multicentre, phase 3 trial., Lancet
Lee et al., 2016, Serum Human Epidermal Growth Factor 2 Extracellular Domain as a Predictive Biomarker for Lapatinib Treatment Efficacy in Patients With Advanced Breast Cancer., J. Clin. Oncol.
Guarneri et al., 2012, Preoperative chemotherapy plus trastuzumab, lapatinib, or both in human epidermal growth factor receptor 2-positive operable breast cancer: results of the randomized phase II CHER-LOB study., J. Clin. Oncol.
Blackwell et al., 2010, Randomized study of Lapatinib alone or in combination with trastuzumab in women with ErbB2-positive, trastuzumab-refractory metastatic breast cancer., J. Clin. Oncol.
Xia et al., 2002, Anti-tumor activity of GW572016: a dual tyrosine kinase inhibitor blocks EGF activation of EGFR/erbB2 and downstream Erk1/2 and AKT pathways., Oncogene
Johnston et al., 2006, Lapatinib: a novel EGFR/HER2 tyrosine kinase inhibitor for cancer., Drugs Today
Zhou et al., 2004, Effects of the EGFR/HER2 kinase inhibitor GW572016 on EGFR- and HER2-overexpressing breast cancer cell line proliferation, radiosensitization, and resistance., Int. J. Radiat. Oncol. Biol. Phys.
Tevaarwerk et al., 2009, Lapatinib: a small-molecule inhibitor of epidermal growth factor receptor and human epidermal growth factor receptor-2 tyrosine kinases used in the treatment of breast cancer., Clin Ther
Vazquez-Martin et al., 2011, Lapatinib, a dual HER1/HER2 tyrosine kinase inhibitor, augments basal cleavage of HER2 extracellular domain (ECD) to inhibit HER2-driven cancer cell growth., J. Cell. Physiol.
Wood et al., 2004, A unique structure for epidermal growth factor receptor bound to GW572016 (Lapatinib): relationships among protein conformation, inhibitor off-rate, and receptor activity in tumor cells., Cancer Res.
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Grana et al., 2003, Epidermal growth factor receptor autocrine signaling in RIE-1 cells transformed by the Ras oncogene enhances radiation resistance., Cancer Res.
Burris, 2004, Dual kinase inhibition in the treatment of breast cancer: initial experience with the EGFR/ErbB-2 inhibitor lapatinib., Oncologist
Xia et al., 2004, Truncated ErbB2 receptor (p95ErbB2) is regulated by heregulin through heterodimer formation with ErbB3 yet remains sensitive to the dual EGFR/ErbB2 kinase inhibitor GW572016., Oncogene
Langer, 2004, Emerging role of epidermal growth factor receptor inhibition in therapy for advanced malignancy: focus on NSCLC., Int. J. Radiat. Oncol. Biol. Phys.
Medina et al., 2008, Lapatinib: a dual inhibitor of human epidermal growth factor receptor tyrosine kinases., Clin Ther
Bachelot T et al., 2013, Lapatinib plus capecitabine in patients with previously untreated brain metastases from HER2-positive metastatic breast cancer (LANDSCAPE): a single-group phase 2 study., Lancet Oncol
Lin NU et al., 2009, Multicenter phase II study of lapatinib in patients with brain metastases from HER2-positive breast cancer., Clin Cancer Res
Leary et al., 2015, Antiproliferative Effect of Lapatinib in HER2-Positive and HER2-Negative/HER3-High Breast Cancer: Results of the Presurgical Randomized MAPLE Trial (CRUK E/06/039)., Clin. Cancer Res.
Franklin et al., 2004, Insights into ErbB signaling from the structure of the ErbB2-pertuzumab complex., Cancer Cell
Yarlagadda B et al., 2019, Trastuzumab and pertuzumab in circulating tumor DNA ERBB2-amplified HER2-positive refractory cholangiocarcinoma., NPJ Precis Oncol
Meric-Bernstam F et al., 2019, Pertuzumab plus trastuzumab for HER2-amplified metastatic colorectal cancer (MyPathway): an updated report from a multicentre, open-label, phase 2a, multiple basket study., Lancet Oncol
Hainsworth JD et al., 2018, Targeted Therapy for Advanced Solid Tumors on the Basis of Molecular Profiles: Results From MyPathway, an Open-Label, Phase IIa Multiple Basket Study., J Clin Oncol
Baselga et al., 2012, Pertuzumab plus trastuzumab plus docetaxel for metastatic breast cancer., N. Engl. J. Med.
Swain et al., 2015, Pertuzumab, trastuzumab, and docetaxel in HER2-positive metastatic breast cancer., N. Engl. J. Med.
Blumenthal et al., 2013, First FDA approval of dual anti-HER2 regimen: pertuzumab in combination with trastuzumab and docetaxel for HER2-positive metastatic breast cancer., Clin. Cancer Res.
Martin et al., 2016, Trastuzumab emtansine (T-DM1) plus docetaxel with or without pertuzumab in patients with HER2-positive locally advanced or metastatic breast cancer: results from a phase Ib/IIa study., Ann. Oncol.
Kodack et al., 2017, The brain microenvironment mediates resistance in luminal breast cancer to PI3K inhibition through HER3 activation., Sci Transl Med
Sharon E et al., 2010, Sustained response of carcinoma ex pleomorphic adenoma treated with trastuzumab and capecitabine., Head Neck Oncol
von Minckwitz et al., 2009, Trastuzumab beyond progression in human epidermal growth factor receptor 2-positive advanced breast cancer: a german breast group 26/breast international group 03-05 study., J. Clin. Oncol.
Bartsch et al., 2007, Capecitabine and trastuzumab in heavily pretreated metastatic breast cancer., J. Clin. Oncol.
Saura et al., 2014, Safety and efficacy of neratinib in combination with capecitabine in patients with metastatic human epidermal growth factor receptor 2-positive breast cancer., J. Clin. Oncol.
Safran et al., 2004, Herceptin and gemcitabine for metastatic pancreatic cancers that overexpress HER-2/neu., Cancer Invest.
Martin et al., 2013, A phase two randomised trial of neratinib monotherapy versus lapatinib plus capecitabine combination therapy in patients with HER2+ advanced breast cancer., Eur. J. Cancer
Chan et al., 2016, Neratinib after trastuzumab-based adjuvant therapy in patients with HER2-positive breast cancer (ExteNET): a multicentre, randomised, double-blind, placebo-controlled, phase 3 trial., Lancet Oncol.
Awada et al., 2016, Neratinib Plus Paclitaxel vs Trastuzumab Plus Paclitaxel in Previously Untreated Metastatic ERBB2-Positive Breast Cancer: The NEfERT-T Randomized Clinical Trial., JAMA Oncol
Hanker et al., 2017, An Acquired HER2(T798I) Gatekeeper Mutation Induces Resistance to Neratinib in a Patient with HER2 Mutant-Driven Breast Cancer., Cancer Discov
Lopez et al., 2015, Dual HER2/PIK3CA Targeting Overcomes Single-Agent Acquired Resistance in HER2-Amplified Uterine Serous Carcinoma Cell Lines In Vitro and In Vivo., Mol. Cancer Ther.
Kosaka et al., 2017, Response Heterogeneity of EGFR and HER2 Exon 20 Insertions to Covalent EGFR and HER2 Inhibitors., Cancer Res.
Ma et al., 2017, Neratinib Efficacy and Circulating Tumor DNA Detection of HER2 Mutations in HER2 Nonamplified Metastatic Breast Cancer., Clin. Cancer Res.
Gandhi et al., 2014, Phase I study of neratinib in combination with temsirolimus in patients with human epidermal growth factor receptor 2-dependent and other solid tumors., J. Clin. Oncol.
Burstein et al., 2010, Neratinib, an irreversible ErbB receptor tyrosine kinase inhibitor, in patients with advanced ErbB2-positive breast cancer., J. Clin. Oncol.
Chow et al., 2013, Combination neratinib (HKI-272) and paclitaxel therapy in patients with HER2-positive metastatic breast cancer., Br. J. Cancer
Lin et al., 2012, A phase II study of afatinib (BIBW 2992), an irreversible ErbB family blocker, in patients with HER2-positive metastatic breast cancer progressing after trastuzumab., Breast Cancer Res. Treat.
Canonici A et al., 2013, Neratinib overcomes trastuzumab resistance in HER2 amplified breast cancer., Oncotarget
Martin M et al., 2017, Neratinib after trastuzumab-based adjuvant therapy in HER2-positive breast cancer (ExteNET): 5-year analysis of a randomised, double-blind, placebo-controlled, phase 3 trial., Lancet Oncol
Singh H et al., 2018, U.S. Food and Drug Administration Approval: Neratinib for the Extended Adjuvant Treatment of Early-Stage HER2-Positive Breast Cancer., Clin Cancer Res
Wong et al., 2011, Antitumor and antiangiogenic activities of BMS-690514, an inhibitor of human EGF and VEGF receptor kinase families., Clin. Cancer Res.
Yu et al., 2002, Modulation of p53, ErbB1, ErbB2, and Raf-1 expression in lung cancer cells by depsipeptide FR901228., J. Natl. Cancer Inst.
Jeong et al., 2017, HER2 Amplification and Cetuximab Efficacy in Patients With Metastatic Colorectal Cancer Harboring Wild-type RAS and BRAF., Clin Colorectal Cancer
Yonesaka et al., 2011, Activation of ERBB2 signaling causes resistance to the EGFR-directed therapeutic antibody cetuximab., Sci Transl Med
Aung et al., 2016, Testing ERBB2 p.L755S kinase domain mutation as a druggable target in a patient with advanced colorectal cancer., Cold Spring Harb Mol Case Stud
Ring et al., 2015, Phase I Study to Assess the Combination of Afatinib with Trastuzumab in Patients with Advanced or Metastatic HER2-Positive Breast Cancer., Clin. Cancer Res.
Takashima et al., 2014, Phase II study of S-1 in combination with trastuzumab for HER2-positive metastatic breast cancer., Anticancer Res.
André et al., 2014, Everolimus for women with trastuzumab-resistant, HER2-positive, advanced breast cancer (BOLERO-3): a randomised, double-blind, placebo-controlled phase 3 trial., Lancet Oncol.
Ding et al., 2014, Trastuzumab and oxaliplatin exhibit a synergistic antitumor effect in HER2-postive gastric cancer cells., Anticancer Drugs
Bachelot et al., 2014, Sunitinib in combination with trastuzumab for the treatment of advanced breast cancer: activity and safety results from a phase II study., BMC Cancer
Berns et al., 2007, A functional genetic approach identifies the PI3K pathway as a major determinant of trastuzumab resistance in breast cancer., Cancer Cell
Wang et al., 2011, PI3K pathway activation results in low efficacy of both trastuzumab and lapatinib., BMC Cancer
Saura et al., 2014, Phase Ib study of Buparlisib plus Trastuzumab in patients with HER2-positive advanced or metastatic breast cancer that has progressed on Trastuzumab-based therapy., Clin. Cancer Res.
Hamad et al., 2017, Neoadjuvant Treatment With Trastuzumab and FOLFOX Induces a Complete Pathologic Response in a Metastatic ERBB2 (HER2)-Amplified Duodenal Cancer., J Natl Compr Canc Netw
Xiao et al., 2016, A Potent HER3 Monoclonal Antibody That Blocks Both Ligand-Dependent and -Independent Activities: Differential Impacts of PTEN Status on Tumor Response., Mol. Cancer Ther.
Finn et al., 2009, PD 0332991, a selective cyclin D kinase 4/6 inhibitor, preferentially inhibits proliferation of luminal estrogen receptor-positive human breast cancer cell lines in vitro., Breast Cancer Res.
Borley et al., 2014, Impact of HER2 copy number in IHC2+/FISH-amplified breast cancer on outcome of adjuvant trastuzumab treatment in a large UK cancer network., Br. J. Cancer
Bang et al., 2010, Trastuzumab in combination with chemotherapy versus chemotherapy alone for treatment of HER2-positive advanced gastric or gastro-oesophageal junction cancer (ToGA): a phase 3, open-label, randomised controlled trial., Lancet
Tanaka et al., 2011, The selective class I PI3K inhibitor CH5132799 targets human cancers harboring oncogenic PIK3CA mutations., Clin. Cancer Res.
Chuang et al., 2017, ERBB2-Mutated Metastatic Non-Small Cell Lung Cancer: Response and Resistance to Targeted Therapies., J Thorac Oncol
Yu et al., 2015, Targeting AKT1-E17K and the PI3K/AKT Pathway with an Allosteric AKT Inhibitor, ARQ 092., PLoS ONE
Espelin et al., 2016, Dual HER2 Targeting with Trastuzumab and Liposomal-Encapsulated Doxorubicin (MM-302) Demonstrates Synergistic Antitumor Activity in Breast and Gastric Cancer., Cancer Res.
Lin et al., 2007, The role of trastuzumab in early stage breast cancer: current data and treatment recommendations., Curr Treat Options Oncol
Levêque et al., 2008, Clinical pharmacology of trastuzumab., Curr Clin Pharmacol
Treish et al., 2000, Pharmacology and therapeutic use of trastuzumab in breast cancer., Am J Health Syst Pharm
Minuti et al., 2012, Increased MET and HGF gene copy numbers are associated with trastuzumab failure in HER2-positive metastatic breast cancer., Br. J. Cancer
Bookman et al., 2003, Evaluation of monoclonal humanized anti-HER2 antibody, trastuzumab, in patients with recurrent or refractory ovarian or primary peritoneal carcinoma with overexpression of HER2: a phase II trial of the Gynecologic Oncology Group., J. Clin. Oncol.
McAlpine et al., 2009, HER2 overexpression and amplification is present in a subset of ovarian mucinous carcinomas and can be targeted with trastuzumab therapy., BMC Cancer
Fleming et al., 2010, Phase II trial of trastuzumab in women with advanced or recurrent, HER2-positive endometrial carcinoma: a Gynecologic Oncology Group study., Gynecol. Oncol.
Diver et al., 2015, The Therapeutic Challenge of Targeting HER2 in Endometrial Cancer., Oncologist
Doi et al., 2015, Phase 1 pharmacokinetic study of the oral pan-AKT inhibitor MK-2206 in Japanese patients with advanced solid tumors., Cancer Chemother. Pharmacol.
Chlebowski et al., 1976, Metallophosphoryl and Apophosphoryl Alkaline Phosphatases., J. Biol. Chem.
Bland et al., 1976, Rapid infusion of sodium bicarbonate and albumin into high-risk premature infants soon after birth: a controlled, prospective trial., Am. J. Obstet. Gynecol.
Andre et al., 2010, Phase I study of everolimus plus weekly paclitaxel and trastuzumab in patients with metastatic breast cancer pretreated with trastuzumab., J. Clin. Oncol.
Jerusalem et al., 2011, Phase I trial of oral mTOR inhibitor everolimus in combination with trastuzumab and vinorelbine in pre-treated patients with HER2-overexpressing metastatic breast cancer., Breast Cancer Res. Treat.
1998, Pharmacogenomics at work., Nat Biotechnol
Coté D et al., 2018, Germline single nucleotide polymorphisms in ERBB3 and BARD1 genes result in a worse relapse free survival response for HER2-positive breast cancer patients treated with adjuvant based docetaxel, carboplatin and trastuzumab (TCH)., PLoS One
Beauclair S et al., 2007, Role of the HER2 [Ile655Val] genetic polymorphism in tumorogenesis and in the risk of trastuzumab-related cardiotoxicity., Ann Oncol
Stemmler et al., 2006, Application of intrathecal trastuzumab (Herceptintrade mark) for treatment of meningeal carcinomatosis in HER2-overexpressing metastatic breast cancer., Oncol. Rep.
Altundag et al., 2004, Adjuvant targeted therapy with trastuzumab may decrease metastatic capacity in specific group of oropharyngeal cancer patients: downregulation of E-cadherin-catenin complex by cooperative effect of erbB-2 and human papillomavirus type 16 E6/E7 protooncogenes., Med. Hypotheses
Mazières et al., 2016, Lung cancer patients with HER2 mutations treated with chemotherapy and HER2-targeted drugs: results from the European EUHER2 cohort., Ann. Oncol.
Chakrabarty et al., 2013, Trastuzumab-resistant cells rely on a HER2-PI3K-FoxO-survivin axis and are sensitive to PI3K inhibitors., Cancer Res.
Piccart-Gebhart et al., 2005, Trastuzumab after adjuvant chemotherapy in HER2-positive breast cancer., N. Engl. J. Med.
Santin et al., 2008, Trastuzumab treatment in patients with advanced or recurrent endometrial carcinoma overexpressing HER2/neu., Int J Gynaecol Obstet
Kinehara et al., 2015, Favorable response to trastuzumab plus irinotecan combination therapy in two patients with HER2-positive relapsed small-cell lung cancer., Lung Cancer
Marty et al., 2005, Randomized phase II trial of the efficacy and safety of trastuzumab combined with docetaxel in patients with human epidermal growth factor receptor 2-positive metastatic breast cancer administered as first-line treatment: the M77001 study group., J. Clin. Oncol.
Slamon et al., 2001, Use of chemotherapy plus a monoclonal antibody against HER2 for metastatic breast cancer that overexpresses HER2., N. Engl. J. Med.
Hirotsu et al., 2017, Intrinsic HER2 V777L mutation mediates resistance to trastuzumab in a breast cancer patient., Med. Oncol.
Fader AN et al., 2018, Randomized Phase II Trial of Carboplatin-Paclitaxel Versus Carboplatin-Paclitaxel-Trastuzumab in Uterine Serous Carcinomas That Overexpress Human Epidermal Growth Factor Receptor 2/neu., J Clin Oncol
Takahashi H et al., 2019, Phase II Trial of Trastuzumab and Docetaxel in Patients With Human Epidermal Growth Factor Receptor 2-Positive Salivary Duct Carcinoma., J Clin Oncol
Li et al., 2015, HER2 insertion YVMA mutant lung cancer: Long natural history and response to afatinib., Lung Cancer
Perera et al., 2009, HER2YVMA drives rapid development of adenosquamous lung tumors in mice that are sensitive to BIBW2992 and rapamycin combination therapy., Proc. Natl. Acad. Sci. U.S.A.
De Grève et al., 2012, Clinical activity of afatinib (BIBW 2992) in patients with lung adenocarcinoma with mutations in the kinase domain of HER2/neu., Lung Cancer
Cortés et al., 2015, Afatinib alone or afatinib plus vinorelbine versus investigator's choice of treatment for HER2-positive breast cancer with progressive brain metastases after trastuzumab, lapatinib, or both (LUX-Breast 3): a randomised, open-label, multicentre, phase 2 trial., Lancet Oncol.
Goh et al., 2016, Clonal Evolutionary Analysis during HER2 Blockade in HER2-Positive Inflammatory Breast Cancer: A Phase II Open-Label Clinical Trial of Afatinib +/- Vinorelbine., PLoS Med.
Khelwatty et al., 2011, Growth response of human colorectal tumour cell lines to treatment with afatinib (BIBW2992), an irreversible erbB family blocker, and its association with expression of HER family members., Int. J. Oncol.
Tsai et al., 2015, Synergistic Blockade of EGFR and HER2 by New-Generation EGFR Tyrosine Kinase Inhibitor Enhances Radiation Effect in Bladder Cancer Cells., Mol. Cancer Ther.
Costa et al., 2016, Pulse Afatinib for ERBB2 Exon 20 Insertion-Mutated Lung Adenocarcinomas., J Thorac Oncol
Kwak et al., 2013, Phase 2 trial of afatinib, an ErbB family blocker, in solid tumors genetically screened for target activation., Cancer
Choudhury et al., 2016, Afatinib Activity in Platinum-Refractory Metastatic Urothelial Carcinoma in Patients With ERBB Alterations., J. Clin. Oncol.
Suzawa et al., 2016, Antitumor effect of afatinib, as a human epidermal growth factor receptor 2-targeted therapy, in lung cancers harboring HER2 oncogene alterations., Cancer Sci.
Janjigian et al., 2013, Monitoring afatinib treatment in HER2-positive gastric cancer with 18F-FDG and 89Zr-trastuzumab PET., J. Nucl. Med.
Peters S et al., 2018, Activity of Afatinib in Heavily Pretreated Patients With ERBB2 Mutation-Positive Advanced NSCLC: Findings From a Global Named Patient Use Program., J Thorac Oncol
Suzuki et al., 2009, Antitumor activity of a dual epidermal growth factor receptor and ErbB2 kinase inhibitor MP-412 (AV-412) in mouse xenograft models., Cancer Sci.
Suzuki et al., 2007, Pharmacological characterization of MP-412 (AV-412), a dual epidermal growth factor receptor and ErbB2 tyrosine kinase inhibitor., Cancer Sci.
Shimizu et al., 2014, Phase I first-in-human study of CUDC-101, a multitargeted inhibitor of HDACs, EGFR, and HER2 in patients with advanced solid tumors., Clin. Cancer Res.
Mu et al., 2014, AZD8931, an equipotent, reversible inhibitor of signaling by epidermal growth factor receptor (EGFR), HER2, and HER3: preclinical activity in HER2 non-amplified inflammatory breast cancer models., J. Exp. Clin. Cancer Res.
Wang et al., 2006, HER2 kinase domain mutation results in constitutive phosphorylation and activation of HER2 and EGFR and resistance to EGFR tyrosine kinase inhibitors., Cancer Cell
Karlan et al., 1994, Glucocorticoids stabilize HER-2/neu messenger RNA in human epithelial ovarian carcinoma cells., Gynecol. Oncol.
Konecny et al., 2001, HER-2/neu overexpression and in vitro chemosensitivity to CMF and FEC in primary breast cancer., Breast Cancer Res. Treat.
Phillips et al., 2016, ABT-414, an Antibody-Drug Conjugate Targeting a Tumor-Selective EGFR Epitope., Mol. Cancer Ther.
Nam et al., 2011, Antitumor activity of HM781-36B, an irreversible Pan-HER inhibitor, alone or in combination with cytotoxic chemotherapeutic agents in gastric cancer., Cancer Lett.
Láng et al., 2006, [Trastuzumab (Herceptin) in the adjuvant treatment of HER-2-positive early breast cancer]., Magy Onkol
Spicer et al., 2015, Phase 1 dose-escalation study of S-222611, an oral reversible dual tyrosine kinase inhibitor of EGFR and HER2, in patients with solid tumours., Eur. J. Cancer
Tanaka et al., 2014, Preclinical antitumor activity of S-222611, an oral reversible tyrosine kinase inhibitor of epidermal growth factor receptor and human epidermal growth factor receptor 2., Cancer Sci.
Herrera-Abreu et al., 2016, Early Adaptation and Acquired Resistance to CDK4/6 Inhibition in Estrogen Receptor-Positive Breast Cancer., Cancer Res.
Gonzales et al., 2008, Antitumor activity and pharmacokinetic properties of PF-00299804, a second-generation irreversible pan-erbB receptor tyrosine kinase inhibitor., Mol. Cancer Ther.
Kalous et al., 2012, Dacomitinib (PF-00299804), an irreversible Pan-HER inhibitor, inhibits proliferation of HER2-amplified breast cancer cell lines resistant to trastuzumab and lapatinib., Mol. Cancer Ther.
Kris et al., 2015, Targeting HER2 aberrations as actionable drivers in lung cancers: phase II trial of the pan-HER tyrosine kinase inhibitor dacomitinib in patients with HER2-mutant or amplified tumors., Ann. Oncol.
Nam et al., 2012, Evaluation of the antitumor effects and mechanisms of PF00299804, a pan-HER inhibitor, alone or in combination with chemotherapy or targeted agents in gastric cancer., Mol. Cancer Ther.
Strasser et al., 2006, 5-FdUrd-araC heterodinucleoside re-establishes sensitivity in 5-FdUrd- and AraC-resistant MCF-7 breast cancer cells overexpressing ErbB2., Differentiation
Lopez et al., 2014, Taselisib, a selective inhibitor of PIK3CA, is highly effective on PIK3CA-mutated and HER2/neu amplified uterine serous carcinoma in vitro and in vivo., Gynecol. Oncol.
Ferrario et al., 2016, Phase I/II Trial of Sorafenib in Combination with Vinorelbine as First-Line Chemotherapy for Metastatic Breast Cancer., PLoS ONE
Hurley et al., 2006, Docetaxel, cisplatin, and trastuzumab as primary systemic therapy for human epidermal growth factor receptor 2-positive locally advanced breast cancer., J. Clin. Oncol.
Wada K et al., 2015, Novel curcumin analogs to overcome EGFR-TKI lung adenocarcinoma drug resistance and reduce EGFR-TKI-induced GI adverse effects., Bioorg Med Chem
Takahashi Y et al., 2008, Nakijiquinones G-I, new sesquiterpenoid quinones from marine sponge., Bioorg Med Chem
Nordstrom JL et al., 2011, Anti-tumor activity and toxicokinetics analysis of MGAH22, an anti-HER2 monoclonal antibody with enhanced Fcγ receptor binding properties., Breast Cancer Res
Bang et al., 2017, First-in-human phase 1 study of margetuximab (MGAH22), an Fc-modified chimeric monoclonal antibody, in patients with HER2-positive advanced solid tumors., Ann. Oncol.
Mackey et al., 2015, Primary results of ROSE/TRIO-12, a randomized placebo-controlled phase III trial evaluating the addition of ramucirumab to first-line docetaxel chemotherapy in metastatic breast cancer., J. Clin. Oncol.
Moulder et al., 2017, Phase I Study of ONT-380, a HER2 Inhibitor, in Patients with HER2(+)-Advanced Solid Tumors, with an Expansion Cohort in HER2(+) Metastatic Breast Cancer (MBC)., Clin. Cancer Res.
Kulukian A et al., 2020, Preclinical Activity of HER2-Selective Tyrosine Kinase Inhibitor Tucatinib as a Single Agent or in Combination with Trastuzumab or Docetaxel in Solid Tumor Models., Mol Cancer Ther
Borges VF et al., 2018, Tucatinib Combined With Ado-Trastuzumab Emtansine in Advanced ERBB2/HER2-Positive Metastatic Breast Cancer: A Phase 1b Clinical Trial., JAMA Oncol
Prickett et al., 2009, Analysis of the tyrosine kinome in melanoma reveals recurrent mutations in ERBB4., Nat. Genet.
Basu et al., 2015, First-in-Human Pharmacokinetic and Pharmacodynamic Study of the Dual m-TORC 1/2 Inhibitor AZD2014., Clin. Cancer Res.
Ring et al., 1996, Suicide gene expression induced in tumour cells transduced with recombinant adenoviral, retroviral and plasmid vectors containing the ERBB2 promoter., Gene Ther.
Jordan et al., 2016, HER2 expression identifies dynamic functional states within circulating breast cancer cells., Nature
Qian et al., 2012, Cancer network disruption by a single molecule inhibitor targeting both histone deacetylase activity and phosphatidylinositol 3-kinase signaling., Clin. Cancer Res.
Liu et al., 2013, BAY 80-6946 is a highly selective intravenous PI3K inhibitor with potent p110α and p110δ activities in tumor cell lines and xenograft models., Mol. Cancer Ther.
Shah et al., 2017, Effect of Fluorouracil, Leucovorin, and Oxaliplatin With or Without Onartuzumab in HER2-Negative, MET-Positive Gastroesophageal Adenocarcinoma: The METGastric Randomized Clinical Trial., JAMA Oncol
Liu et al., 2007, Downregulation of erbB3 abrogates erbB2-mediated tamoxifen resistance in breast cancer cells., Int. J. Cancer
Raspollini et al., 2005, HER-2/neu oncogene in uterine carcinosarcoma on tamoxifen therapy., Pathol. Res. Pract.
Kurokawa et al., 2001, Inhibition of erbB receptor (HER) tyrosine kinases as a strategy to abrogate antiestrogen resistance in human breast cancer., Clin. Cancer Res.
Takagi et al., 2014, HER2 and HER3 cooperatively regulate cancer cell growth and determine sensitivity to the novel investigational EGFR/HER2 kinase inhibitor TAK-285., Oncoscience
Gravalos et al., 2008, HER2 in gastric cancer: a new prognostic factor and a novel therapeutic target., Ann. Oncol.
Nakayama et al., 2013, Antitumor Activity of TAK-285, an Investigational, Non-Pgp Substrate HER2/EGFR Kinase Inhibitor, in Cultured Tumor Cells, Mouse and Rat Xenograft Tumors, and in an HER2-Positive Brain Metastasis Model., J Cancer
Wang et al., 2016, Bruton's Tyrosine Kinase Inhibitors Prevent Therapeutic Escape in Breast Cancer Cells., Mol. Cancer Ther.
Chong et al., 2017, Mapping genetic vulnerabilities reveals BTK as a novel therapeutic target in oesophageal cancer., Gut
Ma et al., 2017, Phase I Study and Biomarker Analysis of Pyrotinib, a Novel Irreversible Pan-ErbB Receptor Tyrosine Kinase Inhibitor, in Patients With Human Epidermal Growth Factor Receptor 2-Positive Metastatic Breast Cancer., J. Clin. Oncol.
Krishnan et al., 2014, Targeting the disordered C terminus of PTP1B with an allosteric inhibitor., Nat. Chem. Biol.
Ziemba et al., 2001, Repair of triplex-directed DNA alkylation by nucleotide excision repair., Nucleic Acids Res.
Ortiz-Cuaran et al., 2016, Heterogeneous Mechanisms of Primary and Acquired Resistance to Third-Generation EGFR Inhibitors., Clin. Cancer Res.
Utermark et al., 2012, The p110α and p110β isoforms of PI3K play divergent roles in mammary gland development and tumorigenesis., Genes Dev.
Yap et al., 2012, AT13148 is a novel, oral multi-AGC kinase inhibitor with potent pharmacodynamic and antitumor activity., Clin. Cancer Res.
Masui et al., 1991, Direct DNA sequencing of the rat neu oncogene transmembrane domain reveals no mutation in urinary bladder carcinomas induced by N-butyl-N-(4-hydroxybutyl)nitrosamine, N-[4-(5-nitro-2-furyl)-2-thiazolyl]formamide or N-methyl-N-nitrosourea., Carcinogenesis
Erjala et al., 2006, Signaling via ErbB2 and ErbB3 associates with resistance and epidermal growth factor receptor (EGFR) amplification with sensitivity to EGFR inhibitor gefitinib in head and neck squamous cell carcinoma cells., Clin. Cancer Res.
Piechocki et al., 2007, Breast cancer expressing the activated HER2/neu is sensitive to gefitinib in vitro and in vivo and acquires resistance through a novel point mutation in the HER2/neu., Cancer Res.
Carmi C et al., 2010, Novel irreversible epidermal growth factor receptor inhibitors by chemical modulation of the cysteine-trap portion., J Med Chem
van der Lee et al., 2015, The Preclinical Profile of the Duocarmycin-Based HER2-Targeting ADC SYD985 Predicts for Clinical Benefit in Low HER2-Expressing Breast Cancers., Mol. Cancer Ther.
Black et al., 2016, SYD985, a Novel Duocarmycin-Based HER2-Targeting Antibody-Drug Conjugate, Shows Antitumor Activity in Uterine Serous Carcinoma with HER2/Neu Expression., Mol. Cancer Ther.
Andrade-Vieira et al., 2014, Pre-clinical study of drug combinations that reduce breast cancer burden due to aberrant mTOR and metabolism promoted by LKB1 loss., Oncotarget
Tang et al., 2015, BGB-283, a Novel RAF Kinase and EGFR Inhibitor, Displays Potent Antitumor Activity in BRAF-Mutated Colorectal Cancers., Mol. Cancer Ther.
Proia et al., 2015, 23814, an Inhibitory Antibody of Ligand-Mediated Notch1 Activation, Modulates Angiogenesis and Inhibits Tumor Growth without Gastrointestinal Toxicity., Mol. Cancer Ther.
Mocanu MM et al., 2014, Epigallocatechin 3-O-gallate induces 67 kDa laminin receptor-mediated cell death accompanied by downregulation of ErbB proteins and altered lipid raft clustering in mammary and epidermoid carcinoma cells., J Nat Prod
Yeh et al., 1999, From HER2/Neu signal cascade to androgen receptor and its coactivators: a novel pathway by induction of androgen target genes through MAP kinase in prostate cancer cells., Proc. Natl. Acad. Sci. U.S.A.
Venkatesan et al., 2010, PKI-179: an orally efficacious dual phosphatidylinositol-3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitor., Bioorg. Med. Chem. Lett.
Ogitani et al., 2016, DS-8201a, A Novel HER2-Targeting ADC with a Novel DNA Topoisomerase I Inhibitor, Demonstrates a Promising Antitumor Efficacy with Differentiation from T-DM1., Clin. Cancer Res.
Yan et al., 2013, Evaluation and clinical analyses of downstream targets of the Akt inhibitor GDC-0068., Clin. Cancer Res.
Esmat et al., 2006, Cytotoxicity of a natural anthraquinone (Aloin) against human breast cancer cell lines with and without ErbB-2: topoisomerase IIalpha coamplification., Cancer Biol. Ther.
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Mallon et al., 2011, Antitumor efficacy of PKI-587, a highly potent dual PI3K/mTOR kinase inhibitor., Clin. Cancer Res.
Sonnenblick et al., 2017, Impact of Diabetes, Insulin, and Metformin Use on the Outcome of Patients With Human Epidermal Growth Factor Receptor 2-Positive Primary Breast Cancer: Analysis From the ALTTO Phase III Randomized Trial., J. Clin. Oncol.
Hart et al., 2013, VS-5584, a novel and highly selective PI3K/mTOR kinase inhibitor for the treatment of cancer., Mol. Cancer Ther.
Piechocki et al., 2006, Iressa induces cytostasis and augments Fas-mediated apoptosis in acinic cell adenocarcinoma overexpressing HER2/neu., Int. J. Cancer

TRASTUZUMAB ERBB2

Interaction Score: 1.65

Interaction Types & Directionality:

antibody (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Receptor protein-tyrosine kinase erbB-2 inhibitor

Notes

PMIDs:
23220880 16397024 25157968 26243863 26619011 22908275 27626067 27108243 25370464 24982373 27140927 23801166 24742739 17679724 24300914 24606768 17936563 21676217 24470511 26245675 27697991 23948973 28784859 26880266 19874578 28539475 26296355 24691421 20728210 21558396 26432108 28167203 23940356 26469692 26759238 17660958 18690878 11752352 11098307 22850551 12525520 20003286 19840887 26099744 26104654 2605 2013 20975068 21107682 9788323 30071039 17693647 16596213 15236790 20504363 26598547 31453370 30857956 29320312 23204226 22257673 22149875 19289619 16236737 26874901 18555254 25693012 25601188 20124187 22493419 16091755 15911866 11248153 27900589 29146401 29523624 29584549 30452336

Sources:
TALC ClearityFoundationBiomarkers MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial JAX-CKB ChemblInteractions NCI CGI DoCM CIViC GuideToPharmacology PharmGKB TTD FDA OncoKB
NERATINIB ERBB2

Interaction Score: 1.5

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Evidence Type Actionable

combination therapy Capecitabine + Neratinib

Approval Status FDA approved

PMIDs:
22908275 23953056 26874901 27078022 28274957 27697991 28539475 26333383 26243863 23220880 28363995 28679771 24323026 22046346 24516025 16397024 26619011 25157968 20142587 23632474 22418700 24009064 25287822 29146401 29523624

Sources:
TALC MyCancerGenome TdgClinicalTrial JAX-CKB ChemblInteractions CGI DoCM CIViC GuideToPharmacology MyCancerGenomeClinicalTrial PharmGKB TTD FDA OncoKB
MARGETUXIMAB ERBB2

Interaction Score: 1.48

Interaction Types & Directionality:

antibody (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Trial Name MGAH22

Novel drug target Established target

Mechanism of Interaction Receptor protein-tyrosine kinase erbB-2 inhibitor

PMIDs:
22129105 28119295

Sources:
TdgClinicalTrial JAX-CKB ChemblInteractions GuideToPharmacology TTD
AFATINIB ERBB2

Interaction Score: 1.35

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Alteration ERBB2:amp

Drug family ERBB2&EGFR inhibitor 2nd gen

Direct Interaction? False

PMIDs:
23632474 22418700 20142587 26559459 19122144 22325357 25370464 26596672 27923043 21617858 25589492 23948973 24971884 26243863 26964772 28274957 23775486 27044931 28363995 26545934 28167203 23578997 26296355 30096481

Sources:
TALC MyCancerGenome TdgClinicalTrial JAX-CKB CGI CIViC GuideToPharmacology MyCancerGenomeClinicalTrial
TRASTUZUMAB DUOCARMAZINE ERBB2

Interaction Score: 1.27

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type uterine corpus serous adenocarcinoma

Response Type sensitive

Approval Status Preclinical

PMIDs:
25589493 27256376

Sources:
JAX-CKB
TAK-285 ERBB2

Interaction Score: 1.27

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Receptor protein-tyrosine kinase erbB-2 inhibitor

Direct Interaction yes

Indication/Tumor Type Her2-receptor positive breast cancer

PMIDs:
25594012 18441328 23983820

Sources:
JAX-CKB ChemblInteractions TTD
DACOMITINIB ERBB2

Interaction Score: 1.27

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
18606718 22761403 25899785 22135232 28363995

Sources:
TALC MyCancerGenome TdgClinicalTrial JAX-CKB ChemblInteractions CGI CIViC GuideToPharmacology MyCancerGenomeClinicalTrial TTD
CP-724714 ERBB2

Interaction Score: 1.27

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
None found

Sources:
ChemblInteractions GuideToPharmacology TTD
MUBRITINIB ERBB2

Interaction Score: 1.27

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
None found

Sources:
MyCancerGenome ChemblInteractions GuideToPharmacology
PERTUZUMAB ERBB2

Interaction Score: 1.27

Interaction Types & Directionality:

antibody (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
15093539 31453370 30857956 29320312 22149875 25693012 23801166 27052654 28539475 22586653 23940356

Sources:
TALC ClearityFoundationBiomarkers MyCancerGenome TdgClinicalTrial JAX-CKB ChemblInteractions CGI CIViC GuideToPharmacology PharmGKB TTD FDA OncoKB
LAPATINIB ERBB2

Interaction Score: 1.16

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

combination therapy Lapatinib;Chemotherapy

Drug family ERBB2 inhibitor;Chemotherapy

Alteration ERBB2:amp

PMIDs:
2015169 25694417 26243863 22908275 26487584 25435280 27108243 27450453 25221644 27140927 24868024 19786658 27026198 26920887 26245675 25238247 23948973 24971884 27900369 27697991 27197158 26628478 27760111 26296355 22586653 20179222 26432108 27595477 23220880 22046346 18413839 26270481 23940356 18774637 26570998 25305330 24355130 24516025 16397024 26619011 25157968 17192538 16091755 22257673 26811533 22493419 20124187 12214266 16894399 14751502 20110044 20658522 15374980 11752352 14633707 15163842 14737100 14967461 18803986 23122784 19228746 25398453

Sources:
TALC DTC ClearityFoundationBiomarkers MyCancerGenome TdgClinicalTrial JAX-CKB CGI TEND DoCM CIViC GuideToPharmacology PharmGKB TTD FDA OncoKB
TUCATINIB ERBB2

Interaction Score: 1.13

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type stomach carcinoma

Approval Status Phase I

Indication/Tumor Type Her2-receptor positive breast cancer

PMIDs:
28053022 32241871 29955792

Sources:
TALC TdgClinicalTrial JAX-CKB GuideToPharmacology TTD
MM-111 ERBB2

Interaction Score: 1.06

Interaction Types & Directionality:

antibody (inhibitory)

Interaction Info:

combination therapy Paclitaxel + Trastuzumab + MM-111

Indication/Tumor Type stomach cancer

Response Type sensitive

PMIDs:
None found

Sources:
MyCancerGenome TdgClinicalTrial JAX-CKB GuideToPharmacology TTD
S-222611 ERBB2

Interaction Score: 1.06

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Receptor protein-tyrosine kinase erbB-2 inhibitor

Indication/Tumor Type stomach cancer

PMIDs:
25434923 24837299

Sources:
JAX-CKB ChemblInteractions TTD
AC-480 ERBB2

Interaction Score: 1.06

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name AC480

Novel drug target Established target

Mechanism of Interaction Receptor protein-tyrosine kinase erbB-2 inhibitor

PMIDs:
21576284 19821562

Sources:
TALC DTC MyCancerGenome TdgClinicalTrial JAX-CKB ChemblInteractions GuideToPharmacology TTD
SAPITINIB ERBB2

Interaction Score: 0.99

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Mechanism of Interaction Receptor protein-tyrosine kinase erbB-2 inhibitor

Direct Interaction yes

PMIDs:
24886365

Sources:
TALC MyCancerGenome JAX-CKB ChemblInteractions GuideToPharmacology TTD
TRASTUZUMAB DERUXTECAN ERBB2

Interaction Score: 0.84

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type breast cancer

Response Type sensitive

Approval Status Preclinical - Pdx & cell culture

PMIDs:
27026201

Sources:
JAX-CKB
T-DM1 ERBB2

Interaction Score: 0.84

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Docetaxel + T-DM1 + Pertuzumab

Indication/Tumor Type Her2-receptor positive breast cancer

Response Type sensitive

PMIDs:
27052654

Sources:
JAX-CKB
NAKIJIQUINONE I ERBB2

Interaction Score: 0.84

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
18676149

Sources:
DTC
PYROTINIB ERBB2

Interaction Score: 0.84

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type non-small cell lung carcinoma

Response Type sensitive

Approval Status Phase II

PMIDs:
28498781

Sources:
JAX-CKB ChemblInteractions GuideToPharmacology
NAKIJIQUINONES G ERBB2

Interaction Score: 0.84

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
18676149

Sources:
DTC
GANCOTAMAB ERBB2

Interaction Score: 0.84

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy MM-302 + Trastuzumab

Indication/Tumor Type stomach cancer

Response Type sensitive

PMIDs:
26759238

Sources:
JAX-CKB ChemblInteractions TTD
NAKIJIQUINONES H ERBB2

Interaction Score: 0.84

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
18676149

Sources:
DTC
VARLITINIB ERBB2

Interaction Score: 0.84

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name ARRY-334543

combination therapy trastuzumab + varlitinib

PMIDs:
None found

Sources:
TdgClinicalTrial JAX-CKB ChemblInteractions TTD
MP-412 ERBB2

Interaction Score: 0.7

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type breast cancer

Response Type sensitive

Approval Status Preclinical - Cell line xenograft

PMIDs:
19459856 17888033

Sources:
TdgClinicalTrial JAX-CKB ChemblInteractions
TESEVATINIB ERBB2

Interaction Score: 0.48

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Receptor protein-tyrosine kinase erbB-2 inhibitor

Direct Interaction yes

Evidence Type Actionable

PMIDs:
19718025 18413839

Sources:
TALC MyCancerGenome TdgClinicalTrial JAX-CKB ChemblInteractions GuideToPharmacology
IRESSA ERBB2

Interaction Score: 0.42

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16470840

Sources:
NCI
ANTHRAQUINONE ERBB2

Interaction Score: 0.42

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16357514

Sources:
NCI
TIPIRACIL ERBB2

Interaction Score: 0.42

Interaction Types & Directionality:

n/a

Interaction Info:

Combination therapy Tipiracil,Trifluridine

PMIDs:
None found

Sources:
FDA
MASOPROCOL ERBB2

Interaction Score: 0.42

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
ZENOCUTUZUMAB ERBB2

Interaction Score: 0.42

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
ADO-TRASTUZUMAB EMTANSINE ERBB2

Interaction Score: 0.42

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
TRODUSQUEMINE ERBB2

Interaction Score: 0.42

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type Her2-receptor positive breast cancer

Response Type sensitive

Approval Status Preclinical - Cell line xenograft

PMIDs:
24845231

Sources:
JAX-CKB
MEDI-4276 ERBB2

Interaction Score: 0.42

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
ONARTUZUMAB ERBB2

Interaction Score: 0.42

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Onartuzumab + mFOLFOX6

Indication/Tumor Type gastric adenocarcinoma

Response Type no benefit

PMIDs:
27918764

Sources:
JAX-CKB
ELGEMTUMAB ERBB2

Interaction Score: 0.42

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy LJM716 + Neratinib

Indication/Tumor Type breast cancer

Response Type sensitive

PMIDs:
28539475

Sources:
JAX-CKB
HERCEPTIN ERBB2

Interaction Score: 0.42

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17216002 15581051

Sources:
NCI
POZIOTINIB ERBB2

Interaction Score: 0.42

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Epidermal growth factor receptor inhibitor

Direct Interaction yes

Indication/Tumor Type stomach cancer

PMIDs:
21306821

Sources:
JAX-CKB ChemblInteractions GuideToPharmacology MyCancerGenomeClinicalTrial
DEPATUXIZUMAB MAFODOTIN ERBB2

Interaction Score: 0.42

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Cell line xenograft

Response Type sensitive

PMIDs:
26846818

Sources:
JAX-CKB
LAPULEUCEL-T ERBB2

Interaction Score: 0.42

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Phase II

Response Type no benefit

PMIDs:
None found

Sources:
JAX-CKB
INSM-18 ERBB2

Interaction Score: 0.42

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name INSM-18

Mechanism of Interaction Receptor protein-tyrosine kinase erbB-2 inhibitor

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions
HEMAY-022 ERBB2

Interaction Score: 0.42

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Receptor protein-tyrosine kinase erbB-2 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
BMS-690514 ERBB2

Interaction Score: 0.36

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Receptor protein-tyrosine kinase erbB-2 inhibitor

Notes

PMIDs:
21531814

Sources:
TALC MyCancerGenome JAX-CKB ChemblInteractions GuideToPharmacology
CANERTINIB ERBB2

Interaction Score: 0.3

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type Advanced Solid Tumor

Response Type sensitive

Approval Status Preclinical

PMIDs:
16843263

Sources:
MyCancerGenome JAX-CKB GuideToPharmacology TTD
AEE-788 ERBB2

Interaction Score: 0.3

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type Advanced Solid Tumor

Response Type sensitive

Approval Status Preclinical

PMIDs:
22046346

Sources:
MyCancerGenome JAX-CKB ChemblInteractions GuideToPharmacology
PELITINIB ERBB2

Interaction Score: 0.28

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

PMIDs:
None found

Sources:
TALC MyCancerGenome
ALLITINIB ERBB2

Interaction Score: 0.28

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Receptor protein-tyrosine kinase erbB-2 inhibitor

Direct Interaction yes

Specific Action of the Ligand Inhibition

PMIDs:
None found

Sources:
ChemblInteractions GuideToPharmacology
ERTUMAXOMAB ERBB2

Interaction Score: 0.28

Interaction Types & Directionality:

n/a

Interaction Info:

Mechanism of Interaction Receptor protein-tyrosine kinase erbB-2 other

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions TTD
OSIMERTINIB ERBB2

Interaction Score: 0.25

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type lung adenocarcinoma

Response Type resistant

Approval Status Preclinical

PMIDs:
27252416

Sources:
JAX-CKB CGI
METHYLCURCUMIN ERBB2

Interaction Score: 0.21

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
25753330

Sources:
DTC
PKI-179 ERBB2

Interaction Score: 0.21

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type Her2-receptor positive breast cancer

Response Type sensitive

Approval Status Preclinical - Cell line xenograft

PMIDs:
20797855

Sources:
JAX-CKB
DIMETHYLCURCUMIN ERBB2

Interaction Score: 0.21

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
25753330

Sources:
DTC
URACIL ERBB2

Interaction Score: 0.21

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
1682063

Sources:
NCI
MDX-210 ERBB2

Interaction Score: 0.21

Interaction Types & Directionality:

n/a

Interaction Info:

Mechanism of Interaction Receptor protein-tyrosine kinase erbB-2 other

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
GANCICLOVIR ERBB2

Interaction Score: 0.21

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
8986436

Sources:
NCI
LAPATINIB DITOSYLATE ERBB2

Interaction Score: 0.21

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Receptor protein-tyrosine kinase erbB-2 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
CUDC-101 ERBB2

Interaction Score: 0.21

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
25107918

Sources:
TALC TdgClinicalTrial JAX-CKB ChemblInteractions GuideToPharmacology TTD
MK-2206 ERBB2

Interaction Score: 0.15

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy MK2206;Trastuzumab

Drug family Allosteric AKT inhibitor;ERBB2 mAb inhibitor

Alteration ERBB2:over

PMIDs:
26104654 2605 2013 27026198

Sources:
JAX-CKB CGI
RG-4733 ERBB2

Interaction Score: 0.14

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy RO4929097 + Paclitaxel

Indication/Tumor Type Her2-receptor negative breast cancer

Response Type sensitive

PMIDs:
27556950

Sources:
JAX-CKB
AFATINIB DIMALEATE ERBB2

Interaction Score: 0.14

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Receptor protein-tyrosine kinase erbB-2 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
TIVOZANIB ERBB2

Interaction Score: 0.14

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy 23814 + Tivozanib

Indication/Tumor Type breast cancer

Response Type sensitive

PMIDs:
25995436

Sources:
JAX-CKB
RAMUCIRUMAB ERBB2

Interaction Score: 0.14

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Phase III

Response Type no benefit

PMIDs:
25185099

Sources:
JAX-CKB
LIFIRAFENIB ERBB2

Interaction Score: 0.14

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type Her2-receptor positive breast cancer

Response Type predicted – sensitive

Approval Status Preclinical - Cell culture

PMIDs:
26208524

Sources:
JAX-CKB
ROCILETINIB ERBB2

Interaction Score: 0.14

Interaction Types & Directionality:

n/a

Interaction Info:

Drug family 3rd generation EGFR inhibitor

Alteration ERBB2:amp

PMIDs:
None found

Sources:
CGI
CANERTINIB DIHYDROCHLORIDE ERBB2

Interaction Score: 0.14

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Receptor protein-tyrosine kinase erbB-2 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
TRIFLURIDINE ERBB2

Interaction Score: 0.14

Interaction Types & Directionality:

n/a

Interaction Info:

Combination therapy Tipiracil,Trifluridine

PMIDs:
None found

Sources:
FDA
SERIBANTUMAB ERBB2

Interaction Score: 0.14

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Phase II

Response Type predicted – sensitive

PMIDs:
None found

Sources:
JAX-CKB
ERIBULIN ERBB2

Interaction Score: 0.12

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB FDA
AT-13148 ERBB2

Interaction Score: 0.12

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type Her2-receptor positive breast cancer

Response Type sensitive

Approval Status Preclinical - Cell line xenograft

PMIDs:
22781553

Sources:
JAX-CKB
CAPECITABINE ERBB2

Interaction Score: 0.12

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type breast cancer

combination therapy Capecitabine + Neratinib

combination therapy ARRY-380 + Capecitabine + Trastuzumab

PMIDs:
20504363 19289619 17192538 26487584 17679724 26920887 26432108 25287822

Sources:
JAX-CKB CIViC
TASELISIB ERBB2

Interaction Score: 0.12

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy GDC-0032 + Neratinib

Indication/Tumor Type uterine corpus serous adenocarcinoma

Response Type sensitive

PMIDs:
25172762 26333383

Sources:
JAX-CKB
FALNIDAMOL ERBB2

Interaction Score: 0.11

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology
IPATASERTIB ERBB2

Interaction Score: 0.11

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type Her2-receptor positive breast cancer

Response Type sensitive

Approval Status Preclinical - Cell line xenograft

PMIDs:
24141624

Sources:
JAX-CKB
VISTUSERTIB ERBB2

Interaction Score: 0.11

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Phase I

Response Type predicted – sensitive

PMIDs:
25805799

Sources:
JAX-CKB
OSIMERTINIB MESYLATE ERBB2

Interaction Score: 0.11

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Epidermal growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
JNJ-26483327 ERBB2

Interaction Score: 0.09

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Receptor protein-tyrosine kinase erbB-2 inhibitor

PMIDs:
None found

Sources:
ChemblInteractions TTD
IBRUTINIB ERBB2

Interaction Score: 0.09

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
27256378 28830912

Sources:
JAX-CKB CIViC GuideToPharmacology
FULVESTRANT ERBB2

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy [Tamoxifen,Letrozole,Anastrozole,Exemestane,Fulvestrant,LHRH analogues or antagonist]

Drug family [Hormonal therapy]

Alteration ERBB2:norm;ESR1:over

PMIDs:
None found

Sources:
CGI PharmGKB FDA
ABEMACICLIB ERBB2

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

Alteration ERBB2:norm;ESR1:over

Drug family CDK4/6 inhibitor

PMIDs:
None found

Sources:
CGI PharmGKB FDA
BUPARLISIB ERBB2

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy BKM120 + Bevacizumab

Indication/Tumor Type Her2-receptor positive breast cancer

Response Type sensitive

PMIDs:
24470511 23948973 28539475 23940356

Sources:
JAX-CKB
LETROZOLE ERBB2

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy [Tamoxifen,Letrozole,Anastrozole,Exemestane,Fulvestrant,LHRH analogues or antagonist]

Drug family [Hormonal therapy]

Alteration ERBB2:norm;ESR1:over

PMIDs:
19786658

Sources:
JAX-CKB CGI
PILARALISIB ERBB2

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Trastuzumab + XL147

Evidence Type Actionable

Approval Status Preclinical

PMIDs:
23948973 23204226

Sources:
JAX-CKB CIViC
CRIZOTINIB ERBB2

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

Alteration MET:amp;ERBB2:amp

Drug family ALK inhibitor;ERBB2 mAb inhibitor

combination therapy Crizotinib;Trastuzumab

PMIDs:
27595477 26432108

Sources:
JAX-CKB CGI
FILGRASTIM ERBB2

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16549824

Sources:
NCI
CETUXIMAB ERBB2

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type colorectal cancer

Response Type resistant

Approval Status Preclinical - Cell line xenograft

PMIDs:
28223103 22586653 23948973 21900593 26243863 26296355

Sources:
JAX-CKB CIViC
TALAZOPARIB ERBB2

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB FDA
EVEROLIMUS ERBB2

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Phase III

Response Type sensitive

PMIDs:
24742739 20975068 21107682

Sources:
JAX-CKB CGI PharmGKB FDA
VS-5584 ERBB2

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type gastric adenocarcinoma

Response Type sensitive

Approval Status Preclinical - Cell line xenograft

PMIDs:
23270925

Sources:
JAX-CKB
CHLORAMBUCIL ERBB2

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
11691913

Sources:
NCI
PA-799 ERBB2

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type ovarian cancer

combination therapy CH5132799 + Trastuzumab

Approval Status Preclinical - Cell line xenograft

PMIDs:
21558396

Sources:
JAX-CKB
PALBOCICLIB ERBB2

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

Alteration ERBB2:norm;ESR1:over

Drug family CDK4/6 inhibitor

combination therapy Palbociclib + Trastuzumab

PMIDs:
25221644 27020857 19874578

Sources:
JAX-CKB CGI PharmGKB FDA
GEFITINIB ERBB2

Interaction Score: 0.06

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type breast cancer

Response Type resistant

Approval Status Preclinical

PMIDs:
16818711 23220880 26545934 17638894 20151670

Sources:
DTC JAX-CKB NCI MyCancerGenomeClinicalTrial PharmGKB
EXEMESTANE ERBB2

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy [Tamoxifen,Letrozole,Anastrozole,Exemestane,Fulvestrant,LHRH analogues or antagonist]

Drug family [Hormonal therapy]

Alteration ERBB2:norm;ESR1:over

PMIDs:
None found

Sources:
JAX-CKB CGI
LEUCOVORIN ERBB2

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Trastuzumab + Fluorouracil + Leucovorin + Oxaliplatin

Indication/Tumor Type gastric adenocarcinoma

Response Type resistant

PMIDs:
27626067 28784859 26432108

Sources:
JAX-CKB
FLOXURIDINE ERBB2

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17177846

Sources:
NCI
AZD-8055 ERBB2

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type breast cancer

Response Type sensitive

Approval Status Preclinical

PMIDs:
25436981

Sources:
JAX-CKB
PICTILISIB ERBB2

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Palbociclib + GDC-0941

Indication/Tumor Type Her2-receptor positive breast cancer

Response Type sensitive

PMIDs:
27020857 22802530

Sources:
JAX-CKB CIViC
PLUMBAGIN ERBB2

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
24355130

Sources:
DTC
TEMSIROLIMUS ERBB2

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Phase I

Response Type predicted – sensitive

PMIDs:
24323026

Sources:
JAX-CKB
DOCETAXEL ERBB2

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Docetaxel + T-DM1 + Pertuzumab

Indication/Tumor Type Her2-receptor positive breast cancer

Response Type sensitive

PMIDs:
22149875 25693012 30071039 25185099 23801166 27052654 30452336

Sources:
JAX-CKB CIViC PharmGKB
RIBOCICLIB ERBB2

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB FDA
VINORELBINE ERBB2

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

Approval Status Phase Ib/II

Response Type predicted – sensitive

Indication/Tumor Type Her2-receptor negative breast cancer

PMIDs:
27992451 24742739

Sources:
JAX-CKB
COPANLISIB ERBB2

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type Her2-receptor positive breast cancer

Response Type sensitive

Approval Status Preclinical - Cell line xenograft

PMIDs:
24170767

Sources:
JAX-CKB
FIMEPINOSTAT ERBB2

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type breast cancer

Response Type sensitive

Approval Status Preclinical

PMIDs:
22693356

Sources:
JAX-CKB
OXALIPLATIN ERBB2

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Trastuzumab + Fluorouracil + Leucovorin + Oxaliplatin

Indication/Tumor Type gastric adenocarcinoma

Response Type resistant

PMIDs:
24300914 28784859 26432108

Sources:
JAX-CKB
ROMIDEPSIN ERBB2

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
11929951

Sources:
NCI
GEDATOLISIB ERBB2

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type Her2-receptor positive breast cancer

Response Type sensitive

Approval Status Preclinical - Cell line xenograft

PMIDs:
17314276 21325073

Sources:
JAX-CKB
OLAPARIB ERBB2

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type Her2-receptor negative breast cancer

Response Type predicted – sensitive

Approval Status Phase III

PMIDs:
None found

Sources:
JAX-CKB PharmGKB FDA
PANITUMUMAB ERBB2

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type colorectal cancer

Response Type resistant

Approval Status Preclinical

PMIDs:
26243863

Sources:
JAX-CKB
IXABEPILONE ERBB2

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB FDA
PACLITAXEL ERBB2

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

Approval Status Preclinical - Pdx & cell culture

Indication/Tumor Type inflammatory breast carcinoma

combination therapy Sapitinib + Paclitaxel

PMIDs:
24886365 24868024 27078022 27556950 26432108 26469692 29584549

Sources:
JAX-CKB CIViC
BEVACIZUMAB ERBB2

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy BKM120 + Bevacizumab

Indication/Tumor Type Her2-receptor positive breast cancer

Response Type sensitive

PMIDs:
26432108 23940356

Sources:
JAX-CKB
CI-1040 ERBB2

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type breast cancer

Response Type resistant

Approval Status Preclinical

PMIDs:
23948973

Sources:
JAX-CKB
TAMOXIFEN ERBB2

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy [Tamoxifen,Letrozole,Anastrozole,Exemestane,Fulvestrant,LHRH analogues or antagonist]

Drug family [Hormonal therapy]

Alteration ERBB2:norm;ESR1:over

PMIDs:
17266042 15901136 11916237

Sources:
NCI CGI
EPIGALOCATECHIN GALLATE ERBB2

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
24456004

Sources:
DTC
ERLOTINIB ERBB2

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type lung adenocarcinoma

Response Type resistant

Approval Status Clinical Study

PMIDs:
27900369

Sources:
DTC JAX-CKB PharmGKB
EMODIN ERBB2

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
9671406

Sources:
NCI
PONATINIB ERBB2

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Pdx

Response Type no benefit

PMIDs:
26270481

Sources:
JAX-CKB
ANASTROZOLE ERBB2

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy [Tamoxifen,Letrozole,Anastrozole,Exemestane,Fulvestrant,LHRH analogues or antagonist]

Drug family [Hormonal therapy]

Alteration ERBB2:norm;ESR1:over

PMIDs:
None found

Sources:
CGI
ACALABRUTINIB ERBB2

Interaction Score: 0.03

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology
DIETHYLSTILBESTROL ERBB2

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
14647453

Sources:
NCI
TRASTUZUMAB EMTANSINE ERBB2

Interaction Score: 0.03

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Receptor protein-tyrosine kinase erbB-2 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
EPIRUBICIN ERBB2

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
11759828

Sources:
NCI
ALPELISIB ERBB2

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB FDA
SELUMETINIB ERBB2

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical

Response Type decreased response

PMIDs:
24971884

Sources:
JAX-CKB
ENTINOSTAT ERBB2

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Entinostat + Lapatinib + Trastuzumab

Indication/Tumor Type Her2-receptor positive breast cancer

Response Type sensitive

PMIDs:
None found

Sources:
JAX-CKB
CHEMBL35482 ERBB2

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10318905

Sources:
NCI
METFORMIN ERBB2

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type Her2-receptor positive breast cancer

Response Type predicted – sensitive

Approval Status Phase III

PMIDs:
28375706

Sources:
JAX-CKB
HYDROCORTISONE ERBB2

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
7909787

Sources:
NCI
CARBOPLATIN ERBB2

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
30071039 29584549

Sources:
CIViC PharmGKB
SUNITINIB ERBB2

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Sunitinib + Trastuzumab

Indication/Tumor Type Her2-receptor positive breast cancer

Response Type sensitive

PMIDs:
24606768

Sources:
JAX-CKB
FLUOROURACIL ERBB2

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

combination therapy Trastuzumab + Fluorouracil + Leucovorin + Oxaliplatin

Indication/Tumor Type gastric adenocarcinoma

PMIDs:
27626067 28784859 26432108

Sources:
JAX-CKB
IRINOTECAN ERBB2

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
25601188

Sources:
CIViC
GEMCITABINE ERBB2

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Phase II

Response Type predicted – sensitive

PMIDs:
15581051

Sources:
JAX-CKB NCI
SIROLIMUS ERBB2

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
19122144

Sources:
CIViC
CURCUMIN ERBB2

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
25753330

Sources:
DTC
GW843682X ERBB2

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ALISERTIB ERBB2

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
SORAFENIB ERBB2

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

Approval Status Phase Ib/II

Indication/Tumor Type Her2-receptor negative breast cancer

combination therapy Sorafenib + Vinorelbine

PMIDs:
27992451

Sources:
JAX-CKB
GO-6976 ERBB2

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CEDIRANIB ERBB2

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
VANDETANIB ERBB2

Interaction Score: 0.01

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Epidermal growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
SOTRASTAURIN ERBB2

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DASATINIB ERBB2

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CYCLOPHOSPHAMIDE ERBB2

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Guideline

Response Type sensitive

PMIDs:
None found

Sources:
JAX-CKB
R-406 ERBB2

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOXORUBICIN ERBB2

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Guideline

Response Type sensitive

PMIDs:
None found

Sources:
JAX-CKB
TAE-684 ERBB2

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ILORASERTIB ERBB2

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CENISERTIB ERBB2

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CISPLATIN ERBB2

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Cisplatin + Gemcitabine + Sorafenib

Indication/Tumor Type invasive bladder transitional cell carcinoma

Response Type predicted – sensitive

PMIDs:
None found

Sources:
JAX-CKB

Ensembl: ENSG00000141736
- Version: 101_38
Alternate Names:

ERBB2 Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:
HopkinsGroom: P04626
- Version: 11-September-2012
Alternate Names:

P04626 Uniprot Accession

RECEPTOR TYROSINE-PROTEIN KINASE ERBB-2 Uniprot Protein Name

2064 Entrez Gene Id

Gene Info:

Interpro Name Serine-threonine/tyrosine-protein kinase catalytic domain

Interpro Type Domain

Interpro Short Name Ser-Thr/Tyr_kinase_cat_dom

Gene Categories:

KINASE, DRUGGABLE GENOME

Publications:

RussLampel: ENSG00000141736

Version: 26-July-2011

Alternate Names:

RECEPTOR TYROSINE-PROTEIN KINASE ERBB-2 PRECURSOR (EC 2.7.1.112) (P185ERBB2) (C-ERBB-2) (NEU PROTO-ONCOGENE) (TYROSINE KINASE-TYPE CELL SURFACE RECEPTOR HER2) (MLN 19). [SOURCE:UNIPROT/SWISSPROT;ACC:P04626] Description

ERBB2 Display Id

ENSG00000141736 Ensembl Gene Id

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Publications:

BaderLabGenes: ERBB2
- Version: February-2014
Alternate Names:

2064 Entrez Gene ID

Gene Info:

Initial Gene Query HER2/ErbB2

Counted Citations from 1950-2000 6422

Gene Categories:

KINASE

Publications:
TdgClinicalTrial: P04626
- Version: January-2014
Alternate Names:

ERBB2 Gene Symbol

Gene Info:

Target Class Receptors

Target Subclass EC:2.7.10.1

Publications:
TEND: P04626
- Version: 01-August-2011
Alternate Names:

P04626 Uniprot Accession

ERBB2_HUMAN Uniprot Id

2064 Entrez Gene Id

Gene Info:

Target Subclass EGFR

Target Subclass Kinase

Target Main Class Receptors

Publications:
GuideToPharmacology: 2064
- Version: 29-September-2020
Alternate Names:

3430 HUGO Gene ID

3430 HUGO Gene Symbol

erb-b2 receptor tyrosine kinase 2 HUGO Gene Name

Gene Info:

GuideToPharmacology Gene Category Name Type I RTKs: ErbB (epidermal growth factor) receptor family

GuideToPharmacology Gene Category ID 320

Publications:

JAX-CKB: ERBB2

Version: 27-September-2017

Alternate Names:

2064 CKB Entrez Id

ERBB2 CKB Gene Synonym

CD340 CKB Gene Synonym

Gene Info:

Publications:

Kancha et al., 2011, Differential sensitivity of ERBB2 kinase domain mutations towards lapatinib., PLoS ONE

Suzuki et al., 2007, Pharmacological characterization of MP-412 (AV-412), a dual epidermal growth factor receptor and ErbB2 tyrosine kinase inhibitor., Cancer Sci.

Suzuki et al., 2009, Antitumor activity of a dual epidermal growth factor receptor and ErbB2 kinase inhibitor MP-412 (AV-412) in mouse xenograft models., Cancer Sci.

PharmGKB: ERBB2

Version: 18-August-2020

Alternate Names:

PA27844 PharmGKB ID

Gene Info:

Publications:

Bose et al., 2013, Activating HER2 mutations in HER2 gene amplification negative breast cancer., Cancer Discov

Cancer Cell Line Encyclopedia Consortium. et al., 2015, Pharmacogenomic agreement between two cancer cell line data sets., Nature

Coté D et al., 2018, Germline single nucleotide polymorphisms in ERBB3 and BARD1 genes result in a worse relapse free survival response for HER2-positive breast cancer patients treated with adjuvant based docetaxel, carboplatin and trastuzumab (TCH)., PLoS One

CIViC: ERBB2

Version: 14-September-2020

Alternate Names:

2064 Entrez Gene ID

20 CIViC Gene ID

Gene Info:

Gene Categories:

DRUG RESISTANCE, CLINICALLY ACTIONABLE

Publications:

Hirotsu et al., 2017, Intrinsic HER2 V777L mutation mediates resistance to trastuzumab in a breast cancer patient., Med. Oncol.

Krop et al., 2014, Trastuzumab emtansine versus treatment of physician's choice for pretreated HER2-positive advanced breast cancer (TH3RESA): a randomised, open-label, phase 3 trial., Lancet Oncol.

Jhaveri KL et al., 2019, Ado-trastuzumab emtansine (T-DM1) in patients with HER2-amplified tumors excluding breast and gastric/gastroesophageal junction (GEJ) adenocarcinomas: results from the NCI-MATCH trial (EAY131) subprotocol Q., Ann Oncol

TTD: Erbb2 tyrosine kinase receptor

Version: 2020.06.01

Alternate Names:

HER2 TTD Gene Abbreviation

T14597 TTD Target ID

Gene Info:

Publications:

Dosio F et al., 2011, Immunotoxins and anticancer drug conjugate assemblies: the role of the linkage between components., Toxins (Basel)

Nordstrom JL et al., 2011, Anti-tumor activity and toxicokinetics analysis of MGAH22, an anti-HER2 monoclonal antibody with enhanced Fcγ receptor binding properties., Breast Cancer Res

NCI: ERBB2

Version: 14-September-2017

Alternate Names:

Gene Info:

Publications:

Zhang et al., 1998, Tyrosine kinase inhibitors, emodin and its derivative repress HER-2/neu-induced cellular transformation and metastasis-associated properties., Oncogene

Yu et al., 2002, Modulation of p53, ErbB1, ErbB2, and Raf-1 expression in lung cancer cells by depsipeptide FR901228., J. Natl. Cancer Inst.

Strasser et al., 2006, 5-FdUrd-araC heterodinucleoside re-establishes sensitivity in 5-FdUrd- and AraC-resistant MCF-7 breast cancer cells overexpressing ErbB2., Differentiation

CGI: ERBB2

Version: 27-September-2017

Alternate Names:

Gene Info:

Publications:

Chow et al., 2013, Combination neratinib (HKI-272) and paclitaxel therapy in patients with HER2-positive metastatic breast cancer., Br. J. Cancer

Lin et al., 2012, A phase II study of afatinib (BIBW 2992), an irreversible ErbB family blocker, in patients with HER2-positive metastatic breast cancer progressing after trastuzumab., Breast Cancer Res. Treat.

Burstein et al., 2010, Neratinib, an irreversible ErbB receptor tyrosine kinase inhibitor, in patients with advanced ErbB2-positive breast cancer., J. Clin. Oncol.

DoCM: ERBB2

Version: 27-September-2017

Alternate Names:

Gene Info:

Publications:

Chang et al., 2016, Identifying recurrent mutations in cancer reveals widespread lineage diversity and mutational specificity., Nat. Biotechnol.

Greulich et al., 2012, Functional analysis of receptor tyrosine kinase mutations in lung cancer identifies oncogenic extracellular domain mutations of ERBB2., Proc. Natl. Acad. Sci. U.S.A.

MacConaill et al., 2014, Prospective enterprise-level molecular genotyping of a cohort of cancer patients., J Mol Diagn

DTC: ERBB2

Version: 02-September-2020

Alternate Names:

Gene Info:

Publications:

Takahashi Y et al., 2008, Nakijiquinones G-I, new sesquiterpenoid quinones from marine sponge., Bioorg Med Chem

Wada K et al., 2015, Novel curcumin analogs to overcome EGFR-TKI lung adenocarcinoma drug resistance and reduce EGFR-TKI-induced GI adverse effects., Bioorg Med Chem

Gavai et al., 2009, Discovery and preclinical evaluation of [4-[[1-(3-fluorophenyl)methyl]-1H-indazol-5-ylamino]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]carbamic acid, (3S)-3-morpholinylmethyl ester (BMS-599626), a selective and orally efficacious inhibitor of human epidermal growth factor receptor 1 and 2 kinases., J. Med. Chem.

MyCancerGenome: ERBB2
- Version: 20-Jun-2017
Alternate Names:

2064 Entrez Gene Id

ERBB2 MyCancerGenome Gene Symbol

HER2 (ERBB2/neu) MyCancerGenome Reported Gene Name

Gene Info:

Publications:
HingoraniCasas: ENSG00000141736
- Version: 31-May-2017
Alternate Names:

ENSG00000141736 Gene Symbol

ERBB2 Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

Publications:
TALC: HER2
- Version: 12-May-2016
Alternate Names:

HER2 Gene Symbol

Gene Info:

Publications:
ChemblInteractions: HER2
- Version: chembl_23
Alternate Names:

MLN19 GENE_SYMBOL

NEU GENE_SYMBOL

NGL GENE_SYMBOL

Gene Info:

Publications:
OncoKB: ERBB2
- Version: 23-July-2020
Alternate Names:

2064 OncoKB Entrez Id

CD340 OncoKB Gene Synonym

MLN 19 OncoKB Gene Synonym

Gene Info:

Publications:
Tempus: ERBB2
- Version: 11-November-2018
Alternate Names:

ERBB2 Gene Symbol

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:
dGene: ERBB2
- Version: 27-Jun-2013
Alternate Names:

2064 Gene ID

CD340 dGene Synonym

HER-2 dGene Synonym

Gene Info:

Gene Categories:

KINASE, TYROSINE KINASE

Publications:
GO: ERBB2
- Version: 01-May-2021
Alternate Names:

HER2 GO Gene Synonym

MLN19 GO Gene Synonym

NEU GO Gene Synonym

Gene Info:

Gene Categories:

TYROSINE KINASE

Publications:
Pharos: ERBB2
- Version: 01-May-2021
Alternate Names:

Receptor tyrosine-protein kinase erbB-2 Gene Name

P04626 UniProt ID

Gene Info:

Gene Categories:

KINASE

Publications:
MskImpact: ERBB2
- Version: May-2015
Alternate Names:

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:
ClearityFoundationClinicalTrial: ERBB2
- Version: 15-June-2013
Alternate Names:

Gene Info:

Publications:
ClearityFoundationBiomarkers: ERBB2
- Version: 26-July-2013
Alternate Names:

Gene Info:

Publications:
MyCancerGenomeClinicalTrial: ERBB2
- Version: 30-February-2014
Alternate Names:

Gene Info:

Publications:
FoundationOneGenes: ERBB2
- Version: 03-September-2020
Alternate Names:

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:
CarisMolecularIntelligence: ERBB2
- Version: 04-September-2020
Alternate Names:

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:
FDA: ERBB2
- Version: 04-September-2020
Alternate Names:

Gene Info:

Publications:
Oncomine: ERBB2
- Version: v3
Alternate Names:

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:

Direct Interaction	yes
Mechanism of Interaction	Receptor protein-tyrosine kinase erbB-2 inhibitor
Notes

Evidence Type	Actionable
combination therapy	Capecitabine + Neratinib
Approval Status	FDA approved

Trial Name	MGAH22
Novel drug target	Established target
Mechanism of Interaction	Receptor protein-tyrosine kinase erbB-2 inhibitor

Alteration	ERBB2:amp
Drug family	ERBB2&EGFR inhibitor 2nd gen
Direct Interaction?	False

Indication/Tumor Type	uterine corpus serous adenocarcinoma
Response Type	sensitive
Approval Status	Preclinical

Direct Interaction?	False
Endogenous Drug?	False
Specific Action of the Ligand	Inhibition

Direct Interaction?	True
Endogenous Drug?	False
Specific Action of the Ligand	Inhibition

combination therapy	Lapatinib;Chemotherapy
Drug family	ERBB2 inhibitor;Chemotherapy
Alteration	ERBB2:amp

Indication/Tumor Type	stomach carcinoma
Approval Status	Phase I
Indication/Tumor Type	Her2-receptor positive breast cancer

combination therapy	Paclitaxel + Trastuzumab + MM-111
Indication/Tumor Type	stomach cancer
Response Type	sensitive

antibody (inhibitory)
inhibitor (inhibitory)

antibody (inhibitory)
inhibitor (inhibitory)

antibody (inhibitory)
inhibitor (inhibitory)

antagonist (inhibitory)
inhibitor (inhibitory)

Trial Name	AC480
Novel drug target	Established target
Mechanism of Interaction	Receptor protein-tyrosine kinase erbB-2 inhibitor

Indication/Tumor Type	breast cancer
Response Type	sensitive
Approval Status	Preclinical - Pdx & cell culture

combination therapy	Docetaxel + T-DM1 + Pertuzumab
Indication/Tumor Type	Her2-receptor positive breast cancer
Response Type	sensitive

Indication/Tumor Type	non-small cell lung carcinoma
Response Type	sensitive
Approval Status	Phase II

combination therapy	MM-302 + Trastuzumab
Indication/Tumor Type	stomach cancer
Response Type	sensitive

combination therapy	Onartuzumab + mFOLFOX6
Indication/Tumor Type	gastric adenocarcinoma
Response Type	no benefit

combination therapy	LJM716 + Neratinib
Indication/Tumor Type	breast cancer
Response Type	sensitive

Mechanism of Interaction	Epidermal growth factor receptor inhibitor
Direct Interaction	yes
Indication/Tumor Type	stomach cancer

Indication/Tumor Type	Advanced Solid Tumor
Response Type	sensitive
Approval Status	Preclinical

Indication/Tumor Type	lung adenocarcinoma
Response Type	resistant
Approval Status	Preclinical

ERBB2 Gene Record

ERBB2 2064 Druggable GenomeClinically ActionableDrug Resistance

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: antibody (inhibitory) inhibitor (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Receptor protein-tyrosine kinase erbB-2 inhibitor Notes

Sources: TALC ClearityFoundationBiomarkers MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial JAX-CKB ChemblInteractions NCI CGI DoCM CIViC GuideToPharmacology PharmGKB TTD FDA OncoKB

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Evidence Type Actionable combination therapy Capecitabine + Neratinib Approval Status FDA approved

PMIDs: 22908275 23953056 26874901 27078022 28274957 27697991 28539475 26333383 26243863 23220880 28363995 28679771 24323026 22046346 24516025 16397024 26619011 25157968 20142587 23632474 22418700 24009064 25287822 29146401 29523624

Sources: TALC MyCancerGenome TdgClinicalTrial JAX-CKB ChemblInteractions CGI DoCM CIViC GuideToPharmacology MyCancerGenomeClinicalTrial PharmGKB TTD FDA OncoKB

Interaction Types & Directionality: antibody (inhibitory) inhibitor (inhibitory)

Interaction Info: Trial Name MGAH22 Novel drug target Established target Mechanism of Interaction Receptor protein-tyrosine kinase erbB-2 inhibitor

PMIDs: 22129105 28119295

Sources: TdgClinicalTrial JAX-CKB ChemblInteractions GuideToPharmacology TTD

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Alteration ERBB2:amp Drug family ERBB2&EGFR inhibitor 2nd gen Direct Interaction? False

PMIDs: 23632474 22418700 20142587 26559459 19122144 22325357 25370464 26596672 27923043 21617858 25589492 23948973 24971884 26243863 26964772 28274957 23775486 27044931 28363995 26545934 28167203 23578997 26296355 30096481

Sources: TALC MyCancerGenome TdgClinicalTrial JAX-CKB CGI CIViC GuideToPharmacology MyCancerGenomeClinicalTrial

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type uterine corpus serous adenocarcinoma Response Type sensitive Approval Status Preclinical

PMIDs: 25589493 27256376

Sources: JAX-CKB

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Receptor protein-tyrosine kinase erbB-2 inhibitor Direct Interaction yes Indication/Tumor Type Her2-receptor positive breast cancer

PMIDs: 25594012 18441328 23983820

Sources: JAX-CKB ChemblInteractions TTD

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction? False Endogenous Drug? False Specific Action of the Ligand Inhibition

PMIDs: 18606718 22761403 25899785 22135232 28363995

Sources: TALC MyCancerGenome TdgClinicalTrial JAX-CKB ChemblInteractions CGI CIViC GuideToPharmacology MyCancerGenomeClinicalTrial TTD

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction? True Endogenous Drug? False Specific Action of the Ligand Inhibition

PMIDs: None found

Sources: ChemblInteractions GuideToPharmacology TTD

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction? True Endogenous Drug? False Specific Action of the Ligand Inhibition

PMIDs: None found

Sources: MyCancerGenome ChemblInteractions GuideToPharmacology

Interaction Types & Directionality: antibody (inhibitory) inhibitor (inhibitory)

Interaction Info: Direct Interaction? True Endogenous Drug? False Specific Action of the Ligand Inhibition

PMIDs: 15093539 31453370 30857956 29320312 22149875 25693012 23801166 27052654 28539475 22586653 23940356

Sources: TALC ClearityFoundationBiomarkers MyCancerGenome TdgClinicalTrial JAX-CKB ChemblInteractions CGI CIViC GuideToPharmacology PharmGKB TTD FDA OncoKB

Interaction Types & Directionality: antagonist (inhibitory) inhibitor (inhibitory)

Interaction Info: combination therapy Lapatinib;Chemotherapy Drug family ERBB2 inhibitor;Chemotherapy Alteration ERBB2:amp

Sources: TALC DTC ClearityFoundationBiomarkers MyCancerGenome TdgClinicalTrial JAX-CKB CGI TEND DoCM CIViC GuideToPharmacology PharmGKB TTD FDA OncoKB

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Indication/Tumor Type stomach carcinoma Approval Status Phase I Indication/Tumor Type Her2-receptor positive breast cancer

PMIDs: 28053022 32241871 29955792

Sources: TALC TdgClinicalTrial JAX-CKB GuideToPharmacology TTD

Interaction Types & Directionality: antibody (inhibitory)

Interaction Info: combination therapy Paclitaxel + Trastuzumab + MM-111 Indication/Tumor Type stomach cancer Response Type sensitive

PMIDs: None found

Sources: MyCancerGenome TdgClinicalTrial JAX-CKB GuideToPharmacology TTD

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Receptor protein-tyrosine kinase erbB-2 inhibitor Indication/Tumor Type stomach cancer

PMIDs: 25434923 24837299

Sources: JAX-CKB ChemblInteractions TTD

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name AC480 Novel drug target Established target Mechanism of Interaction Receptor protein-tyrosine kinase erbB-2 inhibitor

PMIDs: 21576284 19821562

Sources: TALC DTC MyCancerGenome TdgClinicalTrial JAX-CKB ChemblInteractions GuideToPharmacology TTD

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Notes Mechanism of Interaction Receptor protein-tyrosine kinase erbB-2 inhibitor Direct Interaction yes

PMIDs: 24886365

Sources: TALC MyCancerGenome JAX-CKB ChemblInteractions GuideToPharmacology TTD

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type breast cancer Response Type sensitive Approval Status Preclinical - Pdx & cell culture

PMIDs: 27026201

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info: combination therapy Docetaxel + T-DM1 + Pertuzumab Indication/Tumor Type Her2-receptor positive breast cancer Response Type sensitive

PMIDs: 27052654

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 18676149

Sources: DTC

Interaction Types & Directionality:

antibody (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Receptor protein-tyrosine kinase erbB-2 inhibitor

Notes

Sources:
TALC ClearityFoundationBiomarkers MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial JAX-CKB ChemblInteractions NCI CGI DoCM CIViC GuideToPharmacology PharmGKB TTD FDA OncoKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Evidence Type Actionable

combination therapy Capecitabine + Neratinib

Approval Status FDA approved

PMIDs:
22908275 23953056 26874901 27078022 28274957 27697991 28539475 26333383 26243863 23220880 28363995 28679771 24323026 22046346 24516025 16397024 26619011 25157968 20142587 23632474 22418700 24009064 25287822 29146401 29523624

Sources:
TALC MyCancerGenome TdgClinicalTrial JAX-CKB ChemblInteractions CGI DoCM CIViC GuideToPharmacology MyCancerGenomeClinicalTrial PharmGKB TTD FDA OncoKB

Interaction Types & Directionality:

antibody (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Trial Name MGAH22

Novel drug target Established target

Mechanism of Interaction Receptor protein-tyrosine kinase erbB-2 inhibitor

PMIDs:
22129105 28119295

Sources:
TdgClinicalTrial JAX-CKB ChemblInteractions GuideToPharmacology TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Alteration ERBB2:amp

Drug family ERBB2&EGFR inhibitor 2nd gen

Direct Interaction? False

PMIDs:
23632474 22418700 20142587 26559459 19122144 22325357 25370464 26596672 27923043 21617858 25589492 23948973 24971884 26243863 26964772 28274957 23775486 27044931 28363995 26545934 28167203 23578997 26296355 30096481

Sources:
TALC MyCancerGenome TdgClinicalTrial JAX-CKB CGI CIViC GuideToPharmacology MyCancerGenomeClinicalTrial

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type uterine corpus serous adenocarcinoma

Response Type sensitive

Approval Status Preclinical

PMIDs:
25589493 27256376

Sources:
JAX-CKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Receptor protein-tyrosine kinase erbB-2 inhibitor

Direct Interaction yes

Indication/Tumor Type Her2-receptor positive breast cancer

PMIDs:
25594012 18441328 23983820

Sources:
JAX-CKB ChemblInteractions TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
18606718 22761403 25899785 22135232 28363995

Sources:
TALC MyCancerGenome TdgClinicalTrial JAX-CKB ChemblInteractions CGI CIViC GuideToPharmacology MyCancerGenomeClinicalTrial TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
None found

Sources:
ChemblInteractions GuideToPharmacology TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
None found

Sources:
MyCancerGenome ChemblInteractions GuideToPharmacology

Interaction Types & Directionality:

antibody (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
15093539 31453370 30857956 29320312 22149875 25693012 23801166 27052654 28539475 22586653 23940356

Sources:
TALC ClearityFoundationBiomarkers MyCancerGenome TdgClinicalTrial JAX-CKB ChemblInteractions CGI CIViC GuideToPharmacology PharmGKB TTD FDA OncoKB

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

combination therapy Lapatinib;Chemotherapy

Drug family ERBB2 inhibitor;Chemotherapy

Alteration ERBB2:amp

Sources:
TALC DTC ClearityFoundationBiomarkers MyCancerGenome TdgClinicalTrial JAX-CKB CGI TEND DoCM CIViC GuideToPharmacology PharmGKB TTD FDA OncoKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type stomach carcinoma

Approval Status Phase I

Indication/Tumor Type Her2-receptor positive breast cancer

PMIDs:
28053022 32241871 29955792

Sources:
TALC TdgClinicalTrial JAX-CKB GuideToPharmacology TTD

Interaction Types & Directionality:

antibody (inhibitory)

Interaction Info:

combination therapy Paclitaxel + Trastuzumab + MM-111

Indication/Tumor Type stomach cancer

Response Type sensitive

PMIDs:
None found

Sources:
MyCancerGenome TdgClinicalTrial JAX-CKB GuideToPharmacology TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Receptor protein-tyrosine kinase erbB-2 inhibitor

Indication/Tumor Type stomach cancer

PMIDs:
25434923 24837299

Sources:
JAX-CKB ChemblInteractions TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name AC480

Novel drug target Established target

Mechanism of Interaction Receptor protein-tyrosine kinase erbB-2 inhibitor

PMIDs:
21576284 19821562

Sources:
TALC DTC MyCancerGenome TdgClinicalTrial JAX-CKB ChemblInteractions GuideToPharmacology TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Mechanism of Interaction Receptor protein-tyrosine kinase erbB-2 inhibitor

Direct Interaction yes

PMIDs:
24886365

Sources:
TALC MyCancerGenome JAX-CKB ChemblInteractions GuideToPharmacology TTD

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type breast cancer

Response Type sensitive

Approval Status Preclinical - Pdx & cell culture

PMIDs:
27026201

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Docetaxel + T-DM1 + Pertuzumab

Indication/Tumor Type Her2-receptor positive breast cancer

Response Type sensitive

PMIDs:
27052654

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

PMIDs:
18676149

Sources:
DTC

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type non-small cell lung carcinoma

Response Type sensitive

Approval Status Phase II

PMIDs:
28498781

Sources:
JAX-CKB ChemblInteractions GuideToPharmacology

Interaction Types & Directionality:

n/a

PMIDs:
18676149

Sources:
DTC

combination therapy	MK2206;Trastuzumab
Drug family	Allosteric AKT inhibitor;ERBB2 mAb inhibitor
Alteration	ERBB2:over

combination therapy	RO4929097 + Paclitaxel
Indication/Tumor Type	Her2-receptor negative breast cancer
Response Type	sensitive

combination therapy	23814 + Tivozanib
Indication/Tumor Type	breast cancer
Response Type	sensitive

combination therapy	GDC-0032 + Neratinib
Indication/Tumor Type	uterine corpus serous adenocarcinoma
Response Type	sensitive

combination therapy	[Tamoxifen,Letrozole,Anastrozole,Exemestane,Fulvestrant,LHRH analogues or antagonist]
Drug family	[Hormonal therapy]
Alteration	ERBB2:norm;ESR1:over

combination therapy	BKM120 + Bevacizumab
Indication/Tumor Type	Her2-receptor positive breast cancer
Response Type	sensitive

combination therapy	Trastuzumab + XL147
Evidence Type	Actionable
Approval Status	Preclinical

Alteration	MET:amp;ERBB2:amp
Drug family	ALK inhibitor;ERBB2 mAb inhibitor
combination therapy	Crizotinib;Trastuzumab

Indication/Tumor Type	colorectal cancer
Response Type	resistant
Approval Status	Preclinical - Cell line xenograft

Indication/Tumor Type	ovarian cancer
combination therapy	CH5132799 + Trastuzumab
Approval Status	Preclinical - Cell line xenograft