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LAPATINIB Drug Record

  • Summary
  • Interactions
  • Claims
  • LAPATINIB chembl:CHEMBL554 ApprovedAntineoplastic

    Alternate Names:

    TYVERB
    GW-572016X
    GSK-572016
    LAPATINIB
    GW-2016
    GW-572016
    GW572016
    LAP016
    N-{3-CHLORO-4-[(3-FLUOROBENZYL)OXY]PHENYL}-6-[5-({[2-(METHYLSULFONYL)ETHYL]AMINO}METHYL)-2-FURYL]-4-QUINAZOLINAMINE
    GW 572016
    FMM
    N-{3-CHLORO-4-[(3-FLUOROPHENYL)METHOXY]PHENYL}-6-[5-({[2-(METHYLSULFONYL)ETHYL]AMINO}METHYL)-2-FURANYL]-4-QUINAZOLINAMINE
    chembl:CHEMBL554
    pubchem.compound:208908
    chemidplus:231277-92-2
    rxcui:480167
    drugbank:01259

    Drug Info:

    FDA Approval Breast cancer (HER2+)
    Drug Class Kinase Inhibitors
    FDA Approval approved
    Drug Class Small Molecule
    Drug Indications antineoplastic agent
    Year of Approval 2007
    Drug Class antineoplastic agents, protein kinase inhibitors
    Pharmaceutical Developer GlaxoSmithKline
    Source Reported Drug Name(s) Lapatinib
    Drug Class EGFR inhibitor
    (13 More Sources)

    Publications:

    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.
    Li et al., 2008, BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models., Oncogene
    Frattini et al., 2013, The integrated landscape of driver genomic alterations in glioblastoma., Nat. Genet.
    Gilmer et al., 2008, Impact of common epidermal growth factor receptor and HER2 variants on receptor activity and inhibition by lapatinib., Cancer Res.
    Ross et al., 2010, Randomized phase II multicenter trial of two schedules of lapatinib as first- or second-line monotherapy in patients with advanced or metastatic non-small cell lung cancer., Clin. Cancer Res.
    Leslie et al., 2012, Lapatinib and potential prognostic value of EGFR mutations in a Gynecologic Oncology Group phase II trial of persistent or recurrent endometrial cancer., Gynecol. Oncol.
    Yang et al., 2001, Development of ABX-EGF, a fully human anti-EGF receptor monoclonal antibody, for cancer therapy., Crit. Rev. Oncol. Hematol.
    Rossi A et al., 2013, Should epidermal growth factor receptor tyrosine kinase inhibitors be considered ideal drugs for the treatment of selected advanced non-small cell lung cancer patients?, Cancer Treat Rev
    Mayo C et al., 2012, Pharmacogenetics of EGFR in lung cancer: perspectives and clinical applications., Pharmacogenomics
    Van Cutsem et al., 2009, Cetuximab and chemotherapy as initial treatment for metastatic colorectal cancer., N. Engl. J. Med.
    Vermorken JB et al., 2008, Platinum-based chemotherapy plus cetuximab in head and neck cancer., N Engl J Med
    Funke S et al., 2008, Pharmacogenetics in colorectal cancer: a systematic review., Pharmacogenomics
    Giusti RM et al., 2008, U.S. Food and Drug Administration approval: panitumumab for epidermal growth factor receptor-expressing metastatic colorectal carcinoma with progression following fluoropyrimidine-, oxaliplatin-, and irinotecan-containing chemotherapy regimens., Clin Cancer Res
    Jonker et al., 2007, Cetuximab for the treatment of colorectal cancer., N. Engl. J. Med.
    Bonner JA et al., 2006, Radiotherapy plus cetuximab for squamous-cell carcinoma of the head and neck., N Engl J Med
    Normanno N et al., 2006, Epidermal growth factor receptor (EGFR) signaling in cancer., Gene
    Thatcher N et al., 2005, Gefitinib plus best supportive care in previously treated patients with refractory advanced non-small-cell lung cancer: results from a randomised, placebo-controlled, multicentre study (Iressa Survival Evaluation in Lung Cancer)., Lancet
    Herbst RS et al., 2004, Gefitinib in combination with paclitaxel and carboplatin in advanced non-small-cell lung cancer: a phase III trial--INTACT 2., J Clin Oncol
    Giaccone G et al., 2004, Gefitinib in combination with gemcitabine and cisplatin in advanced non-small-cell lung cancer: a phase III trial--INTACT 1., J Clin Oncol
    Jorissen RN et al., 2003, Epidermal growth factor receptor: mechanisms of activation and signalling., Exp Cell Res
    Jaiswal et al., 2013, Oncogenic ERBB3 mutations in human cancers., Cancer Cell
    Bidard FC et al., 2015, Response to dual HER2 blockade in a patient with HER3-mutant metastatic breast cancer., Ann Oncol
    Prickett et al., 2009, Analysis of the tyrosine kinome in melanoma reveals recurrent mutations in ERBB4., Nat. Genet.
    Canfield et al., 2015, Receptor tyrosine kinase ERBB4 mediates acquired resistance to ERBB2 inhibitors in breast cancer cells., Cell Cycle
    Davies et al., 2012, Preclinical pharmacology of AZD5363, an inhibitor of AKT: pharmacodynamics, antitumor activity, and correlation of monotherapy activity with genetic background., Mol. Cancer Ther.
    Dogruluk et al., 2015, Identification of Variant-Specific Functions of PIK3CA by Rapid Phenotyping of Rare Mutations., Cancer Res.
    Loibl S et al., 2014, PIK3CA mutations are associated with lower rates of pathologic complete response to anti-human epidermal growth factor receptor 2 (her2) therapy in primary HER2-overexpressing breast cancer., J Clin Oncol
    Eichhorn PJ et al., 2008, Phosphatidylinositol 3-kinase hyperactivation results in lapatinib resistance that is reversed by the mTOR/phosphatidylinositol 3-kinase inhibitor NVP-BEZ235., Cancer Res
    Spraggs CF et al., 2013, Genetic characterization to improve interpretation and clinical management of hepatotoxicity caused by tyrosine kinase inhibitors., Pharmacogenomics
    Chan EC et al., 2012, Interaction of lapatinib with cytochrome P450 3A5., Drug Metab Dispos
    Barbara JE et al., 2013, Metabolism-dependent inhibition of CYP3A4 by lapatinib: evidence for formation of a metabolic intermediate complex with a nitroso/oxime metabolite formed via a nitrone intermediate., Drug Metab Dispos
    Spraggs CF et al., 2018, Characterisation of the HLA-DRB1*07:01 biomarker for lapatinib-induced liver toxicity during treatment of early-stage breast cancer patients with lapatinib in combination with trastuzumab and/or taxanes., Pharmacogenomics J
    Schaid DJ et al., 2014, Prospective validation of HLA-DRB1*07:01 allele carriage as a predictive risk factor for lapatinib-induced liver injury., J Clin Oncol
    Spraggs CF et al., 2011, HLA-DQA1*02:01 is a major risk factor for lapatinib-induced hepatotoxicity in women with advanced breast cancer., J Clin Oncol
    Montero-Conde et al., 2013, Relief of feedback inhibition of HER3 transcription by RAF and MEK inhibitors attenuates their antitumor effects in BRAF-mutant thyroid carcinomas., Cancer Discov
    LaBonte et al., 2011, The dual EGFR/HER2 inhibitor lapatinib synergistically enhances the antitumor activity of the histone deacetylase inhibitor panobinostat in colorectal cancer models., Cancer Res.
    Xia et al., 2006, Regulation of survivin by ErbB2 signaling: therapeutic implications for ErbB2-overexpressing breast cancers., Cancer Res.
    Wilson et al., 2011, Neuregulin-1-mediated autocrine signaling underlies sensitivity to HER2 kinase inhibitors in a subset of human cancers., Cancer Cell
    Leung et al., 2015, Combining lapatinib and pertuzumab to overcome lapatinib resistance due to NRG1-mediated signalling in HER2-amplified breast cancer., Oncotarget
    Zhao et al., 2014, Mislocalization of p27 to the cytoplasm of breast cancer cells confers resistance to anti-HER2 targeted therapy., Oncotarget
  • LAPATINIB   HLA-DQA1

    Interaction Score: 2.29

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    24687830 21245432


    Sources:
    PharmGKB FDA

  • LAPATINIB   EEF2K

    Interaction Score: 2.29

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • LAPATINIB   ERBB2

    Interaction Score: 1.17

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

    Interaction Info:
    combination therapy Lapatinib + Palbociclib
    combination therapy Entinostat + Lapatinib
    combination therapy Lapatinib + Paclitaxel

    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 TEND DoCM CIViC PharmGKB TTD FDA OncoKB

  • LAPATINIB   CDH1

    Interaction Score: 0.92

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Lapatinib + Capecitabine
    Indication/Tumor Type breast cancer
    Response Type sensitive

    PMIDs:
    26487584


    Sources:
    JAX-CKB

  • LAPATINIB   EGFR

    Interaction Score: 0.63

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

    Interaction Info:
    Reported Cancer Type Prostate
    Evidence Type Actionable
    Approval Status Preclinical - Cell culture

    PMIDs:
    12214266 16894399 14751502 20110044 20658522 15374980 11752352 14633707 15163842 14737100 14967461 18803986 18408761 25305330 24355130 23917401 18199554 20215545 27595477 22885469 11255078 23022519 22594511 19339720 18784101 18681783 18316547 18003960 16467544 16377102 16257339 14990633 14990632 12648464


    Sources:
    TALC DTC TdgClinicalTrial ClearityFoundationClinicalTrial JAX-CKB TEND DoCM CIViC CancerCommons PharmGKB TTD OncoKB

  • LAPATINIB   ABCB11

    Interaction Score: 0.57

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    23556451


    Sources:
    PharmGKB

  • LAPATINIB   ERBB4

    Interaction Score: 0.49

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Variant Effect gain-of-function
    Pathway activation
    Clinical Status preclinical

    PMIDs:
    19718025 25590338


    Sources:
    DTC JAX-CKB DoCM CIViC PharmGKB

  • LAPATINIB   ERBB3

    Interaction Score: 0.46

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Clinical Status preclinical
    Pathway activation
    Variant Effect gain-of-function

    PMIDs:
    23680147 25398453 25953157


    Sources:
    DoCM CIViC PharmGKB

  • LAPATINIB   CDKN1B

    Interaction Score: 0.38

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    25587029


    Sources:
    CIViC

  • LAPATINIB   HLA-DRB1

    Interaction Score: 0.3

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    28786423 24687830


    Sources:
    PharmGKB FDA

  • LAPATINIB   NRG1

    Interaction Score: 0.29

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    21840482 25691057


    Sources:
    CIViC

  • LAPATINIB   PIK3CA

    Interaction Score: 0.18

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Response Type no benefit
    Approval Status Preclinical - Pdx
    Indication/Tumor Type urinary bladder cancer

    PMIDs:
    22294718 26270481 23940356 26920887 26245675 26627007 25199759 19010894


    Sources:
    JAX-CKB CIViC PharmGKB

  • LAPATINIB   BIRC5

    Interaction Score: 0.13

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    16452223


    Sources:
    NCI

  • LAPATINIB   CCND1

    Interaction Score: 0.11

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • LAPATINIB   FGFR2

    Interaction Score: 0.09

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Evidence Type Actionable
    Approval Status Preclinical - Cell culture
    Response Type sensitive

    PMIDs:
    27595477


    Sources:
    JAX-CKB

  • LAPATINIB   PGR

    Interaction Score: 0.09

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB FDA

  • LAPATINIB   SRC

    Interaction Score: 0.08

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Evidence Type Actionable
    Indication/Tumor Type urinary bladder cancer
    Response Type no benefit

    PMIDs:
    26270481


    Sources:
    JAX-CKB

  • LAPATINIB   BRAF

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Response Type sensitive
    combination therapy Lapatinib + Panobinostat
    Indication/Tumor Type colorectal cancer

    PMIDs:
    23365119 21464044


    Sources:
    JAX-CKB

  • LAPATINIB   CYP3A5

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22511346 23404373


    Sources:
    DTC

  • LAPATINIB   MET

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Crizotinib + Lapatinib
    Indication/Tumor Type esophagus adenocarcinoma
    Response Type sensitive

    PMIDs:
    26432108 27595477


    Sources:
    JAX-CKB

  • LAPATINIB   AURKB

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • LAPATINIB   ESR2

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • LAPATINIB   RET

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • LAPATINIB   KRAS

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Trastuzumab + Lapatinib
    Indication/Tumor Type colorectal cancer
    Response Type sensitive

    PMIDs:
    27108243


    Sources:
    JAX-CKB

  • LAPATINIB   ESR1

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB FDA

  • LAPATINIB   YES1

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • LAPATINIB   CYP3A4

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22511346


    Sources:
    DTC

  • CancerCommons: LAPATINIB

    • Version: 25-July-2013

    Alternate Names:
    208908 PubChem Drug ID

    Drug Info:
    Drug Class EGFR inhibitor
    Source Reported Drug Name(s) Lapatinib
    Pharmaceutical Developer GlaxoSmithKline

    Publications:

  • MyCancerGenome: LAPATINIB

    • Version: 20-Jun-2017

    Alternate Names:
    GSK572016 Development Name
    GW2016 Development Name
    TYKERB Trade Name

    Drug Info:
    Drug Class Kinase Inhibitors
    FDA Approval Breast cancer (HER2+)

    Publications:

  • TdgClinicalTrial: LAPATINIB

    • Version: January-2014

    Alternate Names:

    Drug Info:
    Drug Indications antineoplastic agent
    Drug Class Small Molecule
    FDA Approval approved

    Publications:

  • TEND: LAPATINIB

    • Version: 01-August-2011

    Alternate Names:

    Drug Info:
    Drug Class antineoplastic agents, protein kinase inhibitors
    Year of Approval 2007

    Publications:

  • NCI: GW572016

    • Version: 14-September-2017

    Alternate Names:
    C26653 NCI drug code

    Drug Info:

    Publications:
    Xia et al., 2006, Regulation of survivin by ErbB2 signaling: therapeutic implications for ErbB2-overexpressing breast cancers., Cancer Res.

  • DTC: LAPATINIB

    • Version: 02-September-2020

    Alternate Names:
    CHEMBL554 ChEMBL Drug ID

    Drug Info:

    Publications:
    Barbara JE et al., 2013, Metabolism-dependent inhibition of CYP3A4 by lapatinib: evidence for formation of a metabolic intermediate complex with a nitroso/oxime metabolite formed via a nitrone intermediate., Drug Metab Dispos
    Chan EC et al., 2012, Interaction of lapatinib with cytochrome P450 3A5., Drug Metab Dispos
    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

  • PharmGKB: lapatinib

    • Version: 18-August-2020

    Alternate Names:

    Drug Info:

    Publications:
    Schaid DJ et al., 2014, Prospective validation of HLA-DRB1*07:01 allele carriage as a predictive risk factor for lapatinib-induced liver injury., J Clin Oncol
    Spraggs CF et al., 2018, Characterisation of the HLA-DRB1*07:01 biomarker for lapatinib-induced liver toxicity during treatment of early-stage breast cancer patients with lapatinib in combination with trastuzumab and/or taxanes., Pharmacogenomics J
    Cancer Cell Line Encyclopedia Consortium. et al., 2015, Pharmacogenomic agreement between two cancer cell line data sets., Nature

  • JAX-CKB: Lapatinib

    • Version: 27-September-2017

    Alternate Names:

    Drug Info:

    Publications:
    Pan et al., 2015, Development and Characterization of Bladder Cancer Patient-Derived Xenografts for Molecularly Guided Targeted Therapy., PLoS ONE
    Secrier et al., 2016, Mutational signatures in esophageal adenocarcinoma define etiologically distinct subgroups with therapeutic relevance., Nat. Genet.
    Kwak et al., 2015, Molecular Heterogeneity and Receptor Coamplification Drive Resistance to Targeted Therapy in MET-Amplified Esophagogastric Cancer., Cancer Discov

  • DoCM: LAPATINIB

    • Version: 27-September-2017

    Alternate Names:

    Drug Info:

    Publications:
    Prickett et al., 2009, Analysis of the tyrosine kinome in melanoma reveals recurrent mutations in ERBB4., Nat. Genet.
    Leslie et al., 2012, Lapatinib and potential prognostic value of EGFR mutations in a Gynecologic Oncology Group phase II trial of persistent or recurrent endometrial cancer., Gynecol. Oncol.
    Jaiswal et al., 2013, Oncogenic ERBB3 mutations in human cancers., Cancer Cell

  • CIViC: LAPATINIB

    • Version: 14-September-2020

    Alternate Names:

    Drug Info:

    Publications:
    Li et al., 2008, BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models., Oncogene
    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

  • TTD: Lapatinib

    • Version: 2020.06.01

    Alternate Names:
    D08CDI TTD Drug ID

    Drug Info:

    Publications:

  • TALC: LAPATINIB

    • Version: 12-May-2016

    Alternate Names:
    TYKERB Drug Trade Name

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL554

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

  • ClearityFoundationBiomarkers: LAPATINIB

    • Version: 26-July-2013

    Alternate Names:

    Drug Info:

    Publications:

  • ClearityFoundationClinicalTrial: LAPATINIB

    • Version: 15-June-2013

    Alternate Names:

    Drug Info:

    Publications:

  • OncoKB: Lapatinib

    • Version: 23-July-2020

    Alternate Names:

    Drug Info:

    Publications:

  • FDA: Lapatinib

    • Version: 04-September-2020

    Alternate Names:

    Drug Info:

    Publications:

Disclaimer: This resource is intended for purely research purposes. It should not be used for emergencies or medical or professional advice.

A finding of a drug-gene interaction or potentially druggable category does not necessarily indicate effectiveness (or lack thereof) of any drug or treatment regimen. A finding of no interaction or no potentially druggable category does not necessarily indicate lack of effectiveness of any drug or treatment regimen. Drug-gene interactions or potentially druggable categories are not presented in ranked order of potential or predicted efficacy.

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DGIdb (v4.2.0 - sha1 afd9f30b) • Last updated 2020-10-21