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BRAF Gene Record

  • Summary
  • Interactions
  • Claims
  • BRAF 673 Druggable GenomeClinically ActionableDrug Resistance

    Alternate Names:

    673
    B-RAF PROTO-ONCOGENE, SERINE/THREONINE KINASE
    BRAF
    B-RAF1
    B-raf
    BRAF1
    NS7
    RAFB1
    164757
    1097
    ENSG00000157764
    OTTHUMG00000157457
    P15056
    PA25408
    v-raf murine sarcoma viral oncogene homolog B1
    B-RAF PROTO-ONCOGENE SERINE/THREONINE-PROTEIN KINASE (EC 2.7.1.37) (P94) (V-RAF MURINE SARCOMA VIRAL ONCOGENE HOMOLOG B1). [SOURCE:UNIPROT/SWISSPROT;ACC:P15056]
    p94
    Proto-oncogene B-Raf
    Serine/threonine-protein kinase B-raf
    5
    BRAF1_HUMAN
    BRAF_HUMAN
    RAF
    T99089

    Gene Info:

    Target Class Enzymes
    Target Subclass EC:2.7.11.1
    Human Readable Name DRUGGABLE GENOME
    Target Subclass 2.7.11.1
    Target Main Class Enzymes
    CancerCommons Reported Gene Name BRAF (V660) E/K
    CancerCommons Reported Gene Name BRAF
    CancerCommons Reported Gene Name Pan-RAF
    CancerCommons Reported Gene Name BRAF V600E
    Interpro Short Name Ser-Thr/Tyr_kinase_cat_dom
    Interpro Name Serine-threonine/tyrosine-protein kinase catalytic domain
    Uniprot Evidence 1: Evidence at protein level
    Interpro Acc IPR001245
    Uniprot Status Swiss-Prot
    Interpro Type Domain
    Human Readable Name KINASE
    Gene Biotype PROTEIN_CODING
    (26 More Sources)

    Gene Categories: Category Details

    KINASE
    SERINE THREONINE KINASE
    DRUG RESISTANCE
    DRUGGABLE GENOME
    CLINICALLY ACTIONABLE

    Publications:

    Mok et al., 2015, Inhibition of colony stimulating factor-1 receptor improves antitumor efficacy of BRAF inhibition., BMC Cancer
    Greger et al., 2012, Combinations of BRAF, MEK, and PI3K/mTOR inhibitors overcome acquired resistance to the BRAF inhibitor GSK2118436 dabrafenib, mediated by NRAS or MEK mutations., Mol. Cancer Ther.
    Martinelli et al., 2013, Antitumor activity of pimasertib, a selective MEK 1/2 inhibitor, in combination with PI3K/mTOR inhibitors or with multi-targeted kinase inhibitors in pimasertib-resistant human lung and colorectal cancer cells., Int. J. Cancer
    Okimoto RA et al., 2016 Nov 22, Preclinical efficacy of a RAF inhibitor that evades paradoxical MAPK pathway activation in protein kinase BRAF-mutant lung cancer., Proc Natl Acad Sci U S A
    Basile et al., 2014, Inhibition of mutant BRAF splice variant signaling by next-generation, selective RAF inhibitors., Pigment Cell Melanoma Res
    Dienstmann et al., 2015, Database of genomic biomarkers for cancer drugs and clinical targetability in solid tumors., Cancer Discov
    Nicolaides et al., 2011, Targeted therapy for BRAFV600E malignant astrocytoma., Clin. Cancer Res.
    Hoftijzer et al., 2009, Beneficial effects of sorafenib on tumor progression, but not on radioiodine uptake, in patients with differentiated thyroid carcinoma., Eur. J. Endocrinol.
    Rad et al., 2013, A genetic progression model of Braf(V600E)-induced intestinal tumorigenesis reveals targets for therapeutic intervention., Cancer Cell
    Maldonado et al., 2003, Determinants of BRAF mutations in primary melanomas., J. Natl. Cancer Inst.
    Yang et al., 2012, Antitumor activity of BRAF inhibitor vemurafenib in preclinical models of BRAF-mutant colorectal cancer., Cancer Res.
    Villanueva et al., 2010, Acquired resistance to BRAF inhibitors mediated by a RAF kinase switch in melanoma can be overcome by cotargeting MEK and IGF-1R/PI3K., Cancer Cell
    Tiacci et al., 2011, BRAF mutations in hairy-cell leukemia., N. Engl. J. Med.
    Sosman et al., 2012, Survival in BRAF V600-mutant advanced melanoma treated with vemurafenib., N. Engl. J. Med.
    Brose et al., 2002, BRAF and RAS mutations in human lung cancer and melanoma., Cancer Res.
    Gupta-Abramson et al., 2008, Phase II trial of sorafenib in advanced thyroid cancer., J. Clin. Oncol.
    Ho et al., 2013, Selumetinib-enhanced radioiodine uptake in advanced thyroid cancer., N. Engl. J. Med.
    Rizzo et al., 2010, Prognostic vs predictive molecular biomarkers in colorectal cancer: is KRAS and BRAF wild type status required for anti-EGFR therapy?, Cancer Treat. Rev.
    Lovly et al., 2012, Routine multiplex mutational profiling of melanomas enables enrollment in genotype-driven therapeutic trials., PLoS ONE
    Falchook et al., 2013, BRAF mutant gastrointestinal stromal tumor: first report of regression with BRAF inhibitor dabrafenib (GSK2118436) and whole exomic sequencing for analysis of acquired resistance., Oncotarget
    Mao et al., 2013, Resistance to BRAF inhibition in BRAF-mutant colon cancer can be overcome with PI3K inhibition or demethylating agents., Clin. Cancer Res.
    Chen et al., 2014, BRAFV600E mutation and its association with clinicopathological features of colorectal cancer: a systematic review and meta-analysis., PLoS ONE
    Nakayama et al., 2008, KRAS or BRAF mutation status is a useful predictor of sensitivity to MEK inhibition in ovarian cancer., Br. J. Cancer
    Huillard et al., 2012, Cooperative interactions of BRAFV600E kinase and CDKN2A locus deficiency in pediatric malignant astrocytoma as a basis for rational therapy., Proc. Natl. Acad. Sci. U.S.A.
    Peeters et al., 2013, Massively parallel tumor multigene sequencing to evaluate response to panitumumab in a randomized phase III study of metastatic colorectal cancer., Clin. Cancer Res.
    Nagore et al., 2014, Prognostic value of BRAF mutations in localized cutaneous melanoma., J. Am. Acad. Dermatol.
    Pratilas et al., 2008, Genetic predictors of MEK dependence in non-small cell lung cancer., Cancer Res.
    McArthur et al., 2014, Safety and efficacy of vemurafenib in BRAF(V600E) and BRAF(V600K) mutation-positive melanoma (BRIM-3): extended follow-up of a phase 3, randomised, open-label study., Lancet Oncol.
    Mao et al., 2011, BRAF V600E mutation and resistance to anti-EGFR monoclonal antibodies in patients with metastatic colorectal cancer: a meta-analysis., Mol. Biol. Rep.
    De Roock et al., 2009, Clinical biomarkers in oncology: focus on colorectal cancer., Mol Diagn Ther
    Haldar et al., 2011, Epidermal growth factor receptor blockers for the treatment of ovarian cancer., Cochrane Database Syst Rev
    Penna et al., 2016, Primary cross-resistance to BRAFV600E-, MEK1/2- and PI3K/mTOR-specific inhibitors in BRAF-mutant melanoma cells counteracted by dual pathway blockade., Oncotarget
    Corcoran et al., 2012, EGFR-mediated re-activation of MAPK signaling contributes to insensitivity of BRAF mutant colorectal cancers to RAF inhibition with vemurafenib., Cancer Discov
    Xing et al., 2014, BRAF V600E and TERT promoter mutations cooperatively identify the most aggressive papillary thyroid cancer with highest recurrence., J. Clin. Oncol.
    Tejpar et al., 2010, Prognostic and predictive biomarkers in resected colon cancer: current status and future perspectives for integrating genomics into biomarker discovery., Oncologist
    Faber et al., 2014, mTOR inhibition specifically sensitizes colorectal cancers with KRAS or BRAF mutations to BCL-2/BCL-XL inhibition by suppressing MCL-1., Cancer Discov
    Agaimy et al., 2009, V600E BRAF mutations are alternative early molecular events in a subset of KIT/PDGFRA wild-type gastrointestinal stromal tumours., J. Clin. Pathol.
    De Roock et al., 2010, Effects of KRAS, BRAF, NRAS, and PIK3CA mutations on the efficacy of cetuximab plus chemotherapy in chemotherapy-refractory metastatic colorectal cancer: a retrospective consortium analysis., Lancet Oncol.
    Kloos et al., 2009, Phase II trial of sorafenib in metastatic thyroid cancer., J. Clin. Oncol.
    Ponti et al., 2012, Overwhelming response to Dabrafenib in a patient with double BRAF mutation (V600E; V600M) metastatic malignant melanoma., J Hematol Oncol
    Paraiso et al., 2012, The HSP90 inhibitor XL888 overcomes BRAF inhibitor resistance mediated through diverse mechanisms., Clin. Cancer Res.
    Kirkwood et al., 2012, Phase II, open-label, randomized trial of the MEK1/2 inhibitor selumetinib as monotherapy versus temozolomide in patients with advanced melanoma., Clin. Cancer Res.
    Cardarella et al., 2013, Clinical, pathologic, and biologic features associated with BRAF mutations in non-small cell lung cancer., Clin. Cancer Res.
    Nissan et al., 2014, Loss of NF1 in cutaneous melanoma is associated with RAS activation and MEK dependence., Cancer Res.
    Flaherty et al., 2012, Combined BRAF and MEK inhibition in melanoma with BRAF V600 mutations., N. Engl. J. Med.
    Jalili et al., 2012, Dual suppression of the cyclin-dependent kinase inhibitors CDKN2C and CDKN1A in human melanoma., J. Natl. Cancer Inst.
    Gandhi et al., 2009, Alterations in genes of the EGFR signaling pathway and their relationship to EGFR tyrosine kinase inhibitor sensitivity in lung cancer cell lines., PLoS ONE
    Rudin et al., 2013, Molecular characterization of acquired resistance to the BRAF inhibitor dabrafenib in a patient with BRAF-mutant non-small-cell lung cancer., J Thorac Oncol
    Hauschild et al., 2012, Dabrafenib in BRAF-mutated metastatic melanoma: a multicentre, open-label, phase 3 randomised controlled trial., Lancet
    Prahallad et al., 2012, Unresponsiveness of colon cancer to BRAF(V600E) inhibition through feedback activation of EGFR., Nature
    Boulalas et al., Mutational analysis of the BRAF gene in transitional cell carcinoma of the bladder., Int. J. Biol. Markers
    Sarker et al., 2015, First-in-human phase I study of pictilisib (GDC-0941), a potent pan-class I phosphatidylinositol-3-kinase (PI3K) inhibitor, in patients with advanced solid tumors., Clin. Cancer Res.
    Crescenzi et al., 2014, Immunohistochemistry for BRAF(V600E) antibody VE1 performed in core needle biopsy samples identifies mutated papillary thyroid cancers., Horm. Metab. Res.
    Andrulis et al., 2013, Targeting the BRAF V600E mutation in multiple myeloma., Cancer Discov
    Rubinstein et al., 2010, Incidence of the V600K mutation among melanoma patients with BRAF mutations, and potential therapeutic response to the specific BRAF inhibitor PLX4032., J Transl Med
    Kim et al., 2013, Clinical responses to vemurafenib in patients with metastatic papillary thyroid cancer harboring BRAF(V600E) mutation., Thyroid
    Dienstmann et al., 2011, BRAF as a target for cancer therapy., Anticancer Agents Med Chem
    Chapman et al., 2011, Improved survival with vemurafenib in melanoma with BRAF V600E mutation., N. Engl. J. Med.
    Tol et al., 2010, Markers for EGFR pathway activation as predictor of outcome in metastatic colorectal cancer patients treated with or without cetuximab., Eur. J. Cancer
    Ji et al., 2013, Vemurafenib synergizes with nutlin-3 to deplete survivin and suppresses melanoma viability and tumor growth., Clin. Cancer Res.
    Morris et al., 2013, Discovery of a novel ERK inhibitor with activity in models of acquired resistance to BRAF and MEK inhibitors., Cancer Discov
    Sen et al., 2012, Kinase-impaired BRAF mutations in lung cancer confer sensitivity to dasatinib., Sci Transl Med
    Patel et al., 2013, Clinical responses to selumetinib (AZD6244; ARRY-142886)-based combination therapy stratified by gene mutations in patients with metastatic melanoma., Cancer
    He et al., 2014, Prognostic value of the BRAF V600E mutation in papillary thyroid carcinoma., Oncol Lett
    Menzies et al., 2014, Dabrafenib and trametinib, alone and in combination for BRAF-mutant metastatic melanoma., Clin. Cancer Res.
    Lam et al., 2010, Phase II clinical trial of sorafenib in metastatic medullary thyroid cancer., J. Clin. Oncol.
    Di Nicolantonio et al., 2008, Wild-type BRAF is required for response to panitumumab or cetuximab in metastatic colorectal cancer., J. Clin. Oncol.
    Zecchin et al., 2013, BRAF V600E is a determinant of sensitivity to proteasome inhibitors., Mol. Cancer Ther.
    Hayes et al., 2012, Phase II efficacy and pharmacogenomic study of Selumetinib (AZD6244; ARRY-142886) in iodine-131 refractory papillary thyroid carcinoma with or without follicular elements., Clin. Cancer Res.
    Chang et al., 2016, Identifying recurrent mutations in cancer reveals widespread lineage diversity and mutational specificity., Nat. Biotechnol.
    Meckbach et al., 2014, BRAF-V600 mutations have no prognostic impact in stage IV melanoma patients treated with monochemotherapy., PLoS ONE
    Ascierto et al., 2013, Phase II trial (BREAK-2) of the BRAF inhibitor dabrafenib (GSK2118436) in patients with metastatic melanoma., J. Clin. Oncol.
    De Roock et al., 2011, KRAS, BRAF, PIK3CA, and PTEN mutations: implications for targeted therapies in metastatic colorectal cancer., Lancet Oncol.
    Walczyk et al., 2014, The BRAF(V600E) mutation in papillary thyroid microcarcinoma: does the mutation have an impact on clinical outcome?, Clin. Endocrinol. (Oxf)
    Howell et al., 2011, Both BRAF V600E mutation and older age (≥ 65 years) are associated with recurrent papillary thyroid cancer., Ann. Surg. Oncol.
    Wan et al., 2004, Mechanism of activation of the RAF-ERK signaling pathway by oncogenic mutations of B-RAF., Cell
    Flaherty et al., 2012, Improved survival with MEK inhibition in BRAF-mutated melanoma., N. Engl. J. Med.
    Coffee et al., 2013, Concomitant BRAF and PI3K/mTOR blockade is required for effective treatment of BRAF(V600E) colorectal cancer., Clin. Cancer Res.
    Kurman et al., 2011, Molecular pathogenesis and extraovarian origin of epithelial ovarian cancer--shifting the paradigm., Hum. Pathol.
    Falchook et al., 2012, Activity of the oral MEK inhibitor trametinib in patients with advanced melanoma: a phase 1 dose-escalation trial., Lancet Oncol.
    Hatzivassiliou et al., 2013, Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers., Nature
    MacConaill et al., 2014, Prospective enterprise-level molecular genotyping of a cohort of cancer patients., J Mol Diagn
    Rowland et al., 2015, Meta-analysis of BRAF mutation as a predictive biomarker of benefit from anti-EGFR monoclonal antibody therapy for RAS wild-type metastatic colorectal cancer., Br. J. Cancer
    Flaherty et al., 2010, Inhibition of mutated, activated BRAF in metastatic melanoma., N. Engl. J. Med.
    Ohashi et al., 2012, Lung cancers with acquired resistance to EGFR inhibitors occasionally harbor BRAF gene mutations but lack mutations in KRAS, NRAS, or MEK1., Proc. Natl. Acad. Sci. U.S.A.
    Falchook et al., 2012, Dabrafenib in patients with melanoma, untreated brain metastases, and other solid tumours: a phase 1 dose-escalation trial., Lancet
    Paik et al., 2011, Clinical characteristics of patients with lung adenocarcinomas harboring BRAF mutations., J. Clin. Oncol.
    Naoki et al., 2002, Missense mutations of the BRAF gene in human lung adenocarcinoma., Cancer Res.
    Gautschi et al., 2012, A patient with BRAF V600E lung adenocarcinoma responding to vemurafenib., J Thorac Oncol
    Davies et al., 2002, Mutations of the BRAF gene in human cancer., Nature
    Jordan et al., 2012, Vemurafenib for the treatment of melanoma., Expert Opin Pharmacother
    Shi H et al., 2014, Acquired resistance and clonal evolution in melanoma during BRAF inhibitor therapy., Cancer Discov
    Hoogstraat et al., 2015, Detailed imaging and genetic analysis reveal a secondary BRAF(L505H) resistance mutation and extensive intrapatient heterogeneity in metastatic BRAF mutant melanoma patients treated with vemurafenib., Pigment Cell Melanoma Res
    Wagenaar et al., 2014, Resistance to vemurafenib resulting from a novel mutation in the BRAFV600E kinase domain., Pigment Cell Melanoma Res
    Dahlman et al., 2012, BRAF(L597) mutations in melanoma are associated with sensitivity to MEK inhibitors., Cancer Discov
    Sahadudheen et al., 2016, Long Term Survival and Continued Complete Response of Vemurafenib in a Metastatic Melanoma Patient with BRAF V600K Mutation., Case Rep Oncol Med
    Bahadoran et al., 2013, Major clinical response to a BRAF inhibitor in a patient with a BRAF L597R-mutated melanoma., J. Clin. Oncol.
    Hutchinson et al., 2013, BRAF fusions define a distinct molecular subset of melanomas with potential sensitivity to MEK inhibition., Clin. Cancer Res.
    Ribas A et al., 2014, Combination of vemurafenib and cobimetinib in patients with advanced BRAF(V600)-mutated melanoma: a phase 1b study., Lancet Oncol
    Ascierto PA et al., 2016, Cobimetinib combined with vemurafenib in advanced BRAF(V600)-mutant melanoma (coBRIM): updated efficacy results from a randomised, double-blind, phase 3 trial., Lancet Oncol
    Hyman et al., 2015, Vemurafenib in Multiple Nonmelanoma Cancers with BRAF V600 Mutations., N. Engl. J. Med.
    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
    Silkin SV et al., 2016, Complete Clinical Response of BRAF-Mutated Cholangiocarcinoma to Vemurafenib, Panitumumab, and Irinotecan., J Gastrointest Cancer
    Hong et al., 2016, Phase IB Study of Vemurafenib in Combination with Irinotecan and Cetuximab in Patients with Metastatic Colorectal Cancer with BRAFV600E Mutation., Cancer Discov
    Sharman et al., 2014, Vemurafenib response in 2 patients with posttransplant refractory BRAF V600E-mutated multiple myeloma., Clin Lymphoma Myeloma Leuk
    Brose et al., 2016, Vemurafenib in patients with BRAF(V600E)-positive metastatic or unresectable papillary thyroid cancer refractory to radioactive iodine: a non-randomised, multicentre, open-label, phase 2 trial., Lancet Oncol.
    Klempner et al., 2016, BRAFV600E Mutations in High-Grade Colorectal Neuroendocrine Tumors May Predict Responsiveness to BRAF-MEK Combination Therapy., Cancer Discov
    Larkin et al., 2014, Combined vemurafenib and cobimetinib in BRAF-mutated melanoma., N. Engl. J. Med.
    Ali et al., 2014, Extended Antitumor Response of a BRAF V600E Papillary Thyroid Carcinoma to Vemurafenib., Case Rep Oncol
    Savarese et al., beta-Adrenergic receptor decrease in diabetic rat hearts., Life Sci.
    Whittaker et al., 2013, A genome-scale RNA interference screen implicates NF1 loss in resistance to RAF inhibition., Cancer Discov
    Dietrich et al., 2012, BRAF inhibition in refractory hairy-cell leukemia., N. Engl. J. Med.
    Peng et al., 2015, Inhibition of RAF Isoforms and Active Dimers by LY3009120 Leads to Anti-tumor Activities in RAS or BRAF Mutant Cancers., Cancer Cell
    Yao et al., 2017, Tumours with class 3 BRAF mutants are sensitive to the inhibition of activated RAS., Nature
    Nazarian et al., 2010, Melanomas acquire resistance to B-RAF(V600E) inhibition by RTK or N-RAS upregulation., Nature
    Gautschi et al., 2013, Lung adenocarcinoma with BRAF G469L mutation refractory to vemurafenib., Lung Cancer
    Van Allen et al., 2014, The genetic landscape of clinical resistance to RAF inhibition in metastatic melanoma., Cancer Discov
    Peters et al., 2013, Dramatic response induced by vemurafenib in a BRAF V600E-mutated lung adenocarcinoma., J. Clin. Oncol.
    Tiacci et al., 2015, Targeting Mutant BRAF in Relapsed or Refractory Hairy-Cell Leukemia., N. Engl. J. Med.
    Lin et al., 2015, The Hippo effector YAP promotes resistance to RAF- and MEK-targeted cancer therapies., Nat. Genet.
    Joshi et al., 2015, Trametinib with or without vemurafenib in BRAF mutated non-small cell lung cancer., PLoS ONE
    Kotschy et al., 2016, The MCL1 inhibitor S63845 is tolerable and effective in diverse cancer models., Nature
    Yao et al., 2015, BRAF Mutants Evade ERK-Dependent Feedback by Different Mechanisms that Determine Their Sensitivity to Pharmacologic Inhibition., Cancer Cell
    Wagle et al., 2011, Dissecting therapeutic resistance to RAF inhibition in melanoma by tumor genomic profiling., J. Clin. Oncol.
    Herrero et al., 2015, Small Molecule Inhibition of ERK Dimerization Prevents Tumorigenesis by RAS-ERK Pathway Oncogenes., Cancer Cell
    Shi et al., 2014, A novel AKT1 mutant amplifies an adaptive melanoma response to BRAF inhibition., Cancer Discov
    Chen et al., 2016, Oncogenic BRAF Deletions That Function as Homodimers and Are Sensitive to Inhibition by RAF Dimer Inhibitor LY3009120., Cancer Discov
    Peh et al., 2016, The Combination of Vemurafenib and Procaspase-3 Activation Is Synergistic in Mutant BRAF Melanomas., Mol. Cancer Ther.
    Shen et al., 2016, Loss of cohesin complex components STAG2 or STAG3 confers resistance to BRAF inhibition in melanoma., Nat. Med.
    Karoulia et al., 2016, An Integrated Model of RAF Inhibitor Action Predicts Inhibitor Activity against Oncogenic BRAF Signaling., Cancer Cell
    Zick et al., 2017, Treatment inferred from mutations identified using massive parallel sequencing leads to clinical benefit in some heavily pretreated cancer patients., Medicine (Baltimore)
    Kirouac et al., 2017, Clinical responses to ERK inhibition in BRAF(V600E)-mutant colorectal cancer predicted using a computational model., NPJ Syst Biol Appl
    Bonnevaux et al., 2016, Concomitant Inhibition of PI3Kβ and BRAF or MEK in PTEN-Deficient/BRAF-Mutant Melanoma Treatment: Preclinical Assessment of SAR260301 Oral PI3Kβ-Selective Inhibitor., Mol. Cancer Ther.
    Choi et al., 2014, Identification of PLX4032-resistance mechanisms and implications for novel RAF inhibitors., Pigment Cell Melanoma Res
    Kordes et al., 2016, Cooperation of BRAF(F595L) and mutant HRAS in histiocytic sarcoma provides new insights into oncogenic BRAF signaling., Leukemia
    Banerjee et al., 2016, A Rare Finding of a BRAF Mutation in Renal Cell Carcinoma with Response to BRAF-Directed Targeted Therapy., Cureus
    Narita et al., 2014, Novel ATP-competitive MEK inhibitor E6201 is effective against vemurafenib-resistant melanoma harboring the MEK1-C121S mutation in a preclinical model., Mol. Cancer Ther.
    Oddo et al., 2016, Molecular Landscape of Acquired Resistance to Targeted Therapy Combinations in BRAF-Mutant Colorectal Cancer., Cancer Res.
    Sweetlove et al., 2015, Inhibitors of pan-PI3K Signaling Synergize with BRAF or MEK Inhibitors to Prevent BRAF-Mutant Melanoma Cell Growth., Front Oncol
    Feng et al., 2016, A Novel Plant Sesquiterpene Lactone Derivative, DETD-35, Suppresses BRAFV600E Mutant Melanoma Growth and Overcomes Acquired Vemurafenib Resistance in Mice., Mol. Cancer Ther.
    Feng et al., 2015, SBI-0640756 Attenuates the Growth of Clinically Unresponsive Melanomas by Disrupting the eIF4F Translation Initiation Complex., Cancer Res.
    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
    Yaeger et al., 2015, Pilot trial of combined BRAF and EGFR inhibition in BRAF-mutant metastatic colorectal cancer patients., Clin. Cancer Res.
    Kopetz et al., 2015, Phase II Pilot Study of Vemurafenib in Patients With Metastatic BRAF-Mutated Colorectal Cancer., J. Clin. Oncol.
    Connolly et al., 2014, Anticancer activity of combination targeted therapy using cetuximab plus vemurafenib for refractory BRAF (V600E)-mutant metastatic colorectal carcinoma., Curr Oncol
    Budina-Kolomets et al., 2016, HSP70 Inhibition Limits FAK-Dependent Invasion and Enhances the Response to Melanoma Treatment with BRAF Inhibitors., Cancer Res.
    Yang W et al., 2015, Design, synthesis and biological evaluation of bis-aryl ureas and amides based on 2-amino-3-purinylpyridine scaffold as DFG-out B-Raf kinase inhibitors., Eur J Med Chem
    Tsai et al., 2008, Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity., Proc. Natl. Acad. Sci. U.S.A.
    Donadieu J et al., 2019, Vemurafenib for Refractory Multisystem Langerhans Cell Histiocytosis in Children: An International Observational Study., J Clin Oncol
    Ugurel S et al., 2015, A multicenter DeCOG study on predictors of vemurafenib therapy outcome in melanoma: pretreatment impacts survival., Ann Oncol
    Selt F et al., 2017, Establishment and application of a novel patient-derived KIAA1549:BRAF-driven pediatric pilocytic astrocytoma model for preclinical drug testing., Oncotarget
    Sievert AJ et al., 2013, Paradoxical activation and RAF inhibitor resistance of BRAF protein kinase fusions characterizing pediatric astrocytomas., Proc Natl Acad Sci U S A
    Ahronian et al., 2015, Clinical Acquired Resistance to RAF Inhibitor Combinations in BRAF-Mutant Colorectal Cancer through MAPK Pathway Alterations., Cancer Discov
    Corcoran RB et al., 2018, Combined BRAF, EGFR, and MEK Inhibition in Patients with <i>BRAF</i><sup>V600E</sup>-Mutant Colorectal Cancer., Cancer Discov
    2016, Triple Therapy Improves Colorectal Cancer Response., Cancer Discov
    Yaeger R et al., 2019, Response to Anti-EGFR Therapy in Patients with BRAF non-V600-Mutant Metastatic Colorectal Cancer., Clin Cancer Res
    Whittaker et al., 2010, Gatekeeper mutations mediate resistance to BRAF-targeted therapies., Sci Transl Med
    Su et al., 2012, RAF265 inhibits the growth of advanced human melanoma tumors., Clin. Cancer Res.
    Wilhelm et al., 2011, Regorafenib (BAY 73-4506): a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity., Int. J. Cancer
    Napolitano et al., 2015, Primary and Acquired Resistance of Colorectal Cancer to Anti-EGFR Monoclonal Antibody Can Be Overcome by Combined Treatment of Regorafenib with Cetuximab., Clin. Cancer Res.
    Whittaker et al., 2015, Combined Pan-RAF and MEK Inhibition Overcomes Multiple Resistance Mechanisms to Selective RAF Inhibitors., Mol. Cancer Ther.
    McNew et al., 2016, MEK and TAK1 Regulate Apoptosis in Colon Cancer Cells with KRAS-Dependent Activation of Proinflammatory Signaling., Mol. Cancer Res.
    Nikolaev et al., 2011, Exome sequencing identifies recurrent somatic MAP2K1 and MAP2K2 mutations in melanoma., Nat. Genet.
    Beloueche-Babari et al., 2013, Acute tumour response to the MEK1/2 inhibitor selumetinib (AZD6244, ARRY-142886) evaluated by non-invasive diffusion-weighted MRI., Br. J. Cancer
    Friedman et al., 2015, Landscape of Targeted Anti-Cancer Drug Synergies in Melanoma Identifies a Novel BRAF-VEGFR/PDGFR Combination Treatment., PLoS ONE
    Beadnell et al., 2016, The Mitogen-Activated Protein Kinase Pathway Facilitates Resistance to the Src Inhibitor Dasatinib in Thyroid Cancer., Mol. Cancer Ther.
    Emery et al., 2009, MEK1 mutations confer resistance to MEK and B-RAF inhibition., Proc. Natl. Acad. Sci. U.S.A.
    Olow et al., 2016, BRAF Status in Personalizing Treatment Approaches for Pediatric Gliomas., Clin. Cancer Res.
    Fangusaro J et al., 2019, Selumetinib in paediatric patients with BRAF-aberrant or neurofibromatosis type 1-associated recurrent, refractory, or progressive low-grade glioma: a multicentre, phase 2 trial., Lancet Oncol
    Bardelli et al., 2012, The road to resistance: EGFR mutation and cetuximab., Nat. Med.
    Bentivegna et al., 2008, Rapid identification of somatic mutations in colorectal and breast cancer tissues using mismatch repair detection (MRD)., Hum. Mutat.
    Girotti et al., 2013, Inhibiting EGF receptor or SRC family kinase signaling overcomes BRAF inhibitor resistance in melanoma., Cancer Discov
    Lu et al., 2017, Engineering and Functional Characterization of Fusion Genes Identifies Novel Oncogenic Drivers of Cancer., Cancer Res.
    Manchado et al., 2016, A combinatorial strategy for treating KRAS-mutant lung cancer., Nature
    Drobysheva et al., 2017, Targeted MAPK Pathway Inhibitors in Patients With Disseminated Pilocytic Astrocytomas., J Natl Compr Canc Netw
    Corcoran et al., 2015, Combined BRAF and MEK Inhibition With Dabrafenib and Trametinib in BRAF V600-Mutant Colorectal Cancer., J. Clin. Oncol.
    Long et al., 2016, Overall Survival and Durable Responses in Patients With BRAF V600-Mutant Metastatic Melanoma Receiving Dabrafenib Combined With Trametinib., J. Clin. Oncol.
    Kim et al., 2013, Phase II study of the MEK1/MEK2 inhibitor Trametinib in patients with metastatic BRAF-mutant cutaneous melanoma previously treated with or without a BRAF inhibitor., J. Clin. Oncol.
    Marconcini et al., 2017, Metastatic BRAF K601E-mutated melanoma reaches complete response to MEK inhibitor trametinib administered for over 36 months., Exp Hematol Oncol
    Carlino et al., 2015, Preexisting MEK1P124 mutations diminish response to BRAF inhibitors in metastatic melanoma patients., Clin. Cancer Res.
    Long et al., 2014, Combined BRAF and MEK inhibition versus BRAF inhibition alone in melanoma., N. Engl. J. Med.
    Long GV et al., 2017 Sep 10, Adjuvant Dabrafenib plus Trametinib in Stage III BRAF-Mutated Melanoma., N Engl J Med
    Ziemke et al., 2016, Sensitivity of KRAS-Mutant Colorectal Cancers to Combination Therapy That Cotargets MEK and CDK4/6., Clin. Cancer Res.
    Wagle et al., 2014, MAP kinase pathway alterations in BRAF-mutant melanoma patients with acquired resistance to combined RAF/MEK inhibition., Cancer Discov
    Yu et al., 2015, Targeting AKT1-E17K and the PI3K/AKT Pathway with an Allosteric AKT Inhibitor, ARQ 092., PLoS ONE
    Lange et al., 2014, Biological and molecular effects of small molecule kinase inhibitors on low-passage human colorectal cancer cell lines., Biomed Res Int
    Waizenegger et al., 2016, A Novel RAF Kinase Inhibitor with DFG-Out-Binding Mode: High Efficacy in BRAF-Mutant Tumor Xenograft Models in the Absence of Normal Tissue Hyperproliferation., Mol. Cancer Ther.
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    Gibson et al., 2017, Genomic Heterogeneity and Exceptional Response to Dual Pathway Inhibition in Anaplastic Thyroid Cancer., Clin. Cancer Res.
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    Flaherty, 2006, Chemotherapy and targeted therapy combinations in advanced melanoma., Clin. Cancer Res.
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    Herkert et al., 2016, Maximizing the Efficacy of MAPK-Targeted Treatment in PTENLOF/BRAFMUT Melanoma through PI3K and IGF1R Inhibition., Cancer Res.
    Hoeflich et al., 2009, Antitumor efficacy of the novel RAF inhibitor GDC-0879 is predicted by BRAFV600E mutational status and sustained extracellular signal-regulated kinase/mitogen-activated protein kinase pathway suppression., Cancer Res.
    Dummer R et al., 2018, Encorafenib plus binimetinib versus vemurafenib or encorafenib in patients with BRAF-mutant melanoma (COLUMBUS): a multicentre, open-label, randomised phase 3 trial., Lancet Oncol
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    Hoeflich et al., 2012, Intermittent administration of MEK inhibitor GDC-0973 plus PI3K inhibitor GDC-0941 triggers robust apoptosis and tumor growth inhibition., Cancer Res.
    Anderson et al., 2016, PIK3CA mutations enable targeting of a breast tumor dependency through mTOR-mediated MCL-1 translation., Sci Transl Med
    Di Nicolantonio et al., 2010, Deregulation of the PI3K and KRAS signaling pathways in human cancer cells determines their response to everolimus., J. Clin. Invest.
    Mohseni et al., 2010, PIK3CA and KRAS mutations predict for response to everolimus therapy: now that's RAD001., J. Clin. Invest.
    Janku et al., 2011, PIK3CA mutations in patients with advanced cancers treated with PI3K/AKT/mTOR axis inhibitors., Mol. Cancer Ther.
    Souglakos J et al., 2009, Prognostic and predictive value of common mutations for treatment response and survival in patients with metastatic colorectal cancer., Br J Cancer
    Tol J et al., 2009, BRAF mutation in metastatic colorectal cancer., N Engl J Med
    Peng et al., 2016, Loss of PTEN Promotes Resistance to T Cell-Mediated Immunotherapy., Cancer Discov
    Garnett et al., 2012, Systematic identification of genomic markers of drug sensitivity in cancer cells., Nature
    Casadevall et al., 2016, Dabrafenib in an elderly patient with metastatic melanoma and BRAF V600R mutation: a case report., J Med Case Rep
    Planchard et al., 2016, Dabrafenib in patients with BRAF(V600E)-positive advanced non-small-cell lung cancer: a single-arm, multicentre, open-label, phase 2 trial., Lancet Oncol.
    Loaiza-Bonilla A et al., 2014, Dramatic response to dabrafenib and trametinib combination in a BRAF V600E-mutated cholangiocarcinoma: implementation of a molecular tumour board and next-generation sequencing for personalized medicine., Ecancermedicalscience
    Lavingia V et al., 2016, Impressive response to dual <i>BRAF</i> and MEK inhibition in patients with BRAF mutant intrahepatic cholangiocarcinoma-2 case reports and a brief review., J Gastrointest Oncol
    Kocsis J et al., 2017, Combined dabrafenib and trametinib treatment in a case of chemotherapy-refractory extrahepatic BRAF V600E mutant cholangiocarcinoma: dramatic clinical and radiological response with a confusing synchronic new liver lesion., J Gastrointest Oncol
    Ponti et al., 2013, The somatic affairs of BRAF: tailored therapies for advanced malignant melanoma and orphan non-V600E (V600R-M) mutations., J. Clin. Pathol.
    Gibney et al., 2013, Clinical development of dabrafenib in BRAF mutant melanoma and other malignancies., Expert Opin Drug Metab Toxicol
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    Hargrave DR et al., 2019, Efficacy and Safety of Dabrafenib in Pediatric Patients with <i>BRAF</i> V600 Mutation-Positive Relapsed or Refractory Low-Grade Glioma: Results from a Phase I/IIa Study., Clin Cancer Res
    van Geel et al., 2017, A Phase Ib Dose-Escalation Study of Encorafenib and Cetuximab with or without Alpelisib in Metastatic BRAF-Mutant Colorectal Cancer., Cancer Discov
    Montagut et al., 2012, Identification of a mutation in the extracellular domain of the Epidermal Growth Factor Receptor conferring cetuximab resistance in colorectal cancer., Nat. Med.
    Ciardiello et al., 2016, Cetuximab continuation after first progression in metastatic colorectal cancer (CAPRI-GOIM): a randomized phase II trial of FOLFOX plus cetuximab versus FOLFOX., Ann. Oncol.
    Hechtman et al., 2015, AKT1 E17K in Colorectal Carcinoma Is Associated with BRAF V600E but Not MSI-H Status: A Clinicopathologic Comparison to PIK3CA Helical and Kinase Domain Mutants., Mol. Cancer Res.
    Hsu HC et al., 2016, Mutations of KRAS/NRAS/BRAF predict cetuximab resistance in metastatic colorectal cancer patients., Oncotarget
    Loupakis et al., 2009, KRAS codon 61, 146 and BRAF mutations predict resistance to cetuximab plus irinotecan in KRAS codon 12 and 13 wild-type metastatic colorectal cancer., Br. J. Cancer
    Shinozaki E et al., 2017, Clinical significance of BRAF non-V600E mutations on the therapeutic effects of anti-EGFR monoclonal antibody treatment in patients with pretreated metastatic colorectal cancer: the Biomarker Research for anti-EGFR monoclonal Antibodies by Comprehensive Cancer genomics (BREAC) study., Br J Cancer
    Dietlein et al., 2015, A Synergistic Interaction between Chk1- and MK2 Inhibitors in KRAS-Mutant Cancer., Cell
    Herath et al., 2016, The DNA Repair Inhibitor DT01 as a Novel Therapeutic Strategy for Chemosensitization of Colorectal Liver Metastasis., Mol. Cancer Ther.
    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
    Byron et al., 2012, Sensitivity to the MEK inhibitor E6201 in melanoma cells is associated with mutant BRAF and wildtype PTEN status., Mol. Cancer
    Tripathy et al., 2017, Ribociclib (LEE011): Mechanism of Action and Clinical Impact of This Selective Cyclin-Dependent Kinase 4/6 Inhibitor in Various Solid Tumors., Clin. Cancer Res.
    Koelblinger P et al., 2018, Development of encorafenib for BRAF-mutated advanced melanoma., Curr Opin Oncol
    Moschos SJ et al., 2015, Targeted therapies in melanoma., Surg Oncol Clin N Am
    Li Z et al., 2016, Encorafenib (LGX818), a potent BRAF inhibitor, induces senescence accompanied by autophagy in BRAFV600E melanoma cells., Cancer Lett
    Hong et al., 2015, Phase I Dose-Escalation Study of the Multikinase Inhibitor Lenvatinib in Patients with Advanced Solid Tumors and in an Expanded Cohort of Patients with Melanoma., Clin. Cancer Res.
    Frederick et al., 2014, Clinical profiling of BCL-2 family members in the setting of BRAF inhibition offers a rationale for targeting de novo resistance using BH3 mimetics., PLoS ONE
    Vinik et al., 2016, Patient-Reported Outcomes and Quality of Life with Sunitinib Versus Placebo for Pancreatic Neuroendocrine Tumors: Results From an International Phase III Trial., Target Oncol
    Lerner et al., 2015, Targeting a Plk1-Controlled Polarity Checkpoint in Therapy-Resistant Glioblastoma-Propagating Cells., Cancer Res.
    Ghosh C et al., 2020, A Combinatorial Strategy for Targeting <i>BRAF</i> <sup>V600E</sup>-Mutant Cancers with BRAF<sup>V600E</sup> Inhibitor (PLX4720) and Tyrosine Kinase Inhibitor (Ponatinib)., Clin Cancer Res
    Berman et al., 2000, The Protein Data Bank., Nucleic Acids Res.
    García-García et al., 2015, MEK plus PI3K/mTORC1/2 Therapeutic Efficacy Is Impacted by TP53 Mutation in Preclinical Models of Colorectal Cancer., Clin. Cancer Res.
    Hassan et al., 2014, Catalytic mTOR inhibitors can overcome intrinsic and acquired resistance to allosteric mTOR inhibitors., Oncotarget
    Hollestelle et al., 2007, Phosphatidylinositol-3-OH kinase or RAS pathway mutations in human breast cancer cell lines., Mol. Cancer Res.
    Mallon et al., 2011, Antitumor efficacy of PKI-587, a highly potent dual PI3K/mTOR kinase inhibitor., Clin. Cancer Res.
    Ahmed et al., 2013, Epigenetic and genetic features of 24 colon cancer cell lines., Oncogenesis
    James et al., 2012, CEP-32496: a novel orally active BRAF(V600E) inhibitor with selective cellular and in vivo antitumor activity., Mol. Cancer Ther.
    Lieu et al., 2015, Antitumor activity of a potent MEK inhibitor, TAK-733, against colorectal cancer cell lines and patient derived xenografts., Oncotarget
    Acquaviva et al., 2014, Overcoming acquired BRAF inhibitor resistance in melanoma via targeted inhibition of Hsp90 with ganetespib., Mol. Cancer Ther.
    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.
    Kavuri et al., 2015, HER2 activating mutations are targets for colorectal cancer treatment., Cancer Discov
    Vasbinder MM et al., 2013, Discovery and optimization of a novel series of potent mutant B-Raf(V600E) selective kinase inhibitors., J Med Chem
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    Iverson et al., 2009, RDEA119/BAY 869766: a potent, selective, allosteric inhibitor of MEK1/2 for the treatment of cancer., Cancer Res.
    Foster et al., 2015, The Selective PI3K Inhibitor XL147 (SAR245408) Inhibits Tumor Growth and Survival and Potentiates the Activity of Chemotherapeutic Agents in Preclinical Tumor Models., Mol. Cancer Ther.
    Smith et al., 2015, The HSP90 inhibitor ganetespib potentiates the antitumor activity of EGFR tyrosine kinase inhibition in mutant and wild-type non-small cell lung cancer., Target Oncol
  • DABRAFENIB   BRAF

    Interaction Score: 4.76

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

    Interaction Info:
    Response Type predicted – resistant
    Indication/Tumor Type ovarian cancer
    combination therapy AMG 232 + Trametinib + Dabrafenib

    PMIDs:
    28512244 26392102 26811525 27500726 27659046 27770002 22608338 26732095 27255157 25265492 28891408 24265153 24265154 27080216 27048246 27697975 28784858 28268064 22735384 24885690 27312529 22389471 27797976 25370473 27523909 24265155 25452114 25673644 25265494 23031422 29072975 23020132 29431699 25435907 28078132 28480077 25399551 27283860 24583796 23463675 23621583 25656898 22038996 19773371 23845441 14679157 22180495 21156289 21663470 22356324 12460918 18541894 23406027 21129611 22536370 23470635 23251002 24594804 19018267 22586120 23325582 24388723 19010912 24508103 20857202 19537845 21975775 26678033 22448344 25024077 20350999 24163374 19561230 20619739 19255327 22351686 22048237 23833300 24576830 22997239 19238210 23524406 22281684 19404918 25370471 24570209 23612012 20630094 23489023 21426297 21639808 20413299 23812671 23614898 22649091 22972589 24396464 20368568 19001320 24107445 22241789 26619011 24586605 23918947 21163703 24354346 21594703 15035987 22663011 23549875 21683865 22805292 23934108 25157968 25989278 20818844 22773810 21483012 12460919 22743296 12068308 38 2014 8009 2013 8006 2015 31811016 28947956


    Sources:
    TALC MyCancerGenome TdgClinicalTrial JAX-CKB DoCM COSMIC CIViC CancerCommons MyCancerGenomeClinicalTrial PharmGKB TTD FDA OncoKB

  • VEMURAFENIB   BRAF

    Interaction Score: 3.63

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Clinical Status late trials
    Clinical Status early trials
    Clinical Status case report

    PMIDs:
    25656898 22038996 19773371 23845441 14679157 22180495 21156289 21663470 22356324 12460918 18541894 23406027 21129611 22536370 23470635 23251002 24594804 19018267 22586120 23325582 24388723 19010912 24508103 20857202 19537845 21975775 26678033 22448344 25024077 20350999 24163374 19561230 20619739 19255327 23031422 22351686 22048237 23833300 24576830 22389471 23020132 22997239 19238210 23524406 22735384 22281684 19404918 25370471 24570209 23612012 20630094 23489023 21426297 21639808 20413299 23812671 23614898 22649091 22972589 24396464 24583796 20368568 19001320 24107445 22241789 26619011 24586605 23918947 21163703 24354346 21594703 15035987 22663011 23549875 21683865 22805292 23934108 25157968 25989278 20818844 22773810 22608338 21483012 12460919 22743296 12068308 23094782 24265155 25515853 24112705 22798288 26989536 23715574 24345920 25037139 27480103 26287849 29320312 26687137 27729313 24997557 27460442 27048246 25265494 24987354 231718 23288408 22621641 26343583 28783719 21107323 24035431 24265153 23733758 26352686 25665005 25706985 27760111 25939769 26343582 21383288 26267534 24265152 26732095 27297867 27500726 27523909 28514312 28649441 27196754 24283590 26582644 26918217 24448821 27312529 26137449 27048951 26603897 23365119 25589621 26460303 24523613 26984758 25462267 18287029 31513482 25524477 28002790 23533272


    Sources:
    TALC DTC ClearityFoundationBiomarkers MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial JAX-CKB ChemblInteractions DoCM COSMIC CIViC MyCancerGenomeClinicalTrial PharmGKB TTD FDA OncoKB

  • PLX8394   BRAF

    Interaction Score: 3.19

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Indication/Tumor Type Advanced Solid Tumor
    Response Type sensitive
    Approval Status Preclinical

    PMIDs:
    27834212 24422853


    Sources:
    JAX-CKB TTD OncoKB

  • PANITUMUMAB   BRAF

    Interaction Score: 2.97

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Panitumumab + Dabrafenib + Trametinib
    combination therapy Vemurafenib + Panitumumab
    Clinical Status late trials

    PMIDs:
    23325582 21163703 20619739 28783719 25673644 29431699 26687137 19001320 22038996 19773371 23845441 14679157 22180495 21156289 21663470 22356324 12460918 18541894 23406027 21129611 22536370 23470635 23251002 24594804 19018267 22586120 24388723 19010912 24508103 20857202 19537845 21975775 26678033 22448344 25024077 20350999 24163374 19561230 19255327 23031422 22351686 22048237 23833300 24576830 22389471 23020132 22997239 19238210 23524406 22735384 22281684 19404918 25370471 24570209 23612012 20630094 23489023 21426297 21639808 20413299 23812671 23614898 22649091 22972589 24396464 24583796 20368568 24107445 22241789 26619011 24586605 23918947 24354346 21594703 15035987 22663011 23549875 21683865 22805292 23934108 25157968 25989278 20818844 22773810 22608338 21483012 12460919 22743296 12068308 27770002 27312529 28514312 25589621 31515458


    Sources:
    JAX-CKB DoCM CIViC OncoKB

  • TRAMETINIB   BRAF

    Interaction Score: 2.22

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Trametinib + Dabrafenib
    Indication/Tumor Type colorectal cancer
    Response Type sensitive

    PMIDs:
    28512244 27338794 28784858 26392102 24265152 26811525 27500726 26343583 27770002 27760111 23248257 28344857 25370473 25706985 26732095 22663011 25265492 28891408 26369631 24265154 24265153 26469692 25309914 26916115 27048246 27697975 27222538 28268064 27297867 25665005 27312529 22389471 27797976 22805292 27488531 22798288 28783719 31010895 29903880 25452114 26314551 24933606 25265494 22169769 24345920 29072975 23020132 29431699 25399551 27283860 24583796 2493360 23715574 25656898 22038996 19773371 23845441 14679157 22180495 21156289 21663470 22356324 12460918 18541894 23406027 21129611 22536370 23470635 23251002 24594804 19018267 22586120 23325582 24388723 19010912 24508103 20857202 19537845 21975775 26678033 22448344 25024077 20350999 24163374 19561230 20619739 19255327 23031422 22351686 22048237 23833300 24576830 22997239 19238210 23524406 22735384 22281684 19404918 25370471 24570209 23612012 20630094 23489023 21426297 21639808 20413299 23812671 23614898 22649091 22972589 24396464 20368568 19001320 24107445 22241789 26619011 24586605 23918947 21163703 24354346 21594703 15035987 23549875 21683865 23934108 25157968 25989278 20818844 22773810 22608338 21483012 12460919 22743296 12068308 8006 2015 30792255 29156677 28947956


    Sources:
    ClearityFoundationBiomarkers JAX-CKB DoCM CIViC PharmGKB FDA OncoKB

  • SB590885   BRAF

    Interaction Score: 1.91

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Indication/Tumor Type Advanced Solid Tumor
    Response Type resistant
    Approval Status Preclinical

    PMIDs:
    27523909 20538618


    Sources:
    JAX-CKB

  • CETUXIMAB   BRAF

    Interaction Score: 1.6

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Cetuximab + PLX4720
    combination therapy Vemurafenib + Cetuximab
    combination therapy Cetuximab + Dabrafenib + SCH772984

    PMIDs:
    26287849 28363909 28783719 22270724 22281684 24523613 26208524 26916115 27312529 25838391 27002107 25714871 23325582 21163703 20619739 22038996 19773371 23845441 14679157 22180495 21156289 21663470 22356324 12460918 18541894 23406027 21129611 22536370 23470635 23251002 24594804 19018267 22586120 24388723 19010912 24508103 20857202 19537845 21975775 26678033 22448344 25024077 20350999 24163374 19561230 19255327 23031422 22351686 22048237 23833300 24576830 22389471 23020132 22997239 19238210 23524406 22735384 19404918 25370471 24570209 23612012 20630094 23489023 21426297 21639808 20413299 23812671 23614898 22649091 22972589 24396464 24583796 20368568 19001320 24107445 22241789 26619011 24586605 23918947 24354346 21594703 15035987 22663011 23549875 21683865 22805292 23934108 25157968 25989278 20818844 22773810 22608338 21483012 12460919 22743296 12068308 26989027 19603024 27729313 19603018 31566309 19571295 31515458 28972961


    Sources:
    JAX-CKB DoCM CIViC OncoKB

  • ENCORAFENIB   BRAF

    Interaction Score: 1.59

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    combination therapy Cetuximab + Encorafenib
    Indication/Tumor Type colorectal cancer
    Response Type resistant

    PMIDs:
    27307593 28363909 28351928 27312529 26577700 29573941 31566309 29356698 25769717 26586345


    Sources:
    TALC MyCancerGenome JAX-CKB ChemblInteractions CIViC CancerCommons PharmGKB TTD FDA OncoKB

  • PLX-4720   BRAF

    Interaction Score: 1.42

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Indication/Tumor Type melanoma
    Response Type resistant
    Approval Status Preclinical - Cell line xenograft

    PMIDs:
    26351322 21383288 24265153 19915144 22281684 27217440 23242808 27523909 24983357 27924459 26461489 26573800 20538618 18287029 23845441 31937621 23533272 10592235


    Sources:
    JAX-CKB CIViC

  • CHEMBL525191   BRAF

    Interaction Score: 1.27

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    23549875


    Sources:
    CIViC

  • RG-7256   BRAF

    Interaction Score: 1.27

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Serine/threonine-protein kinase B-raf inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions TTD

  • RAF-265   BRAF

    Interaction Score: 1.12

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Indication/Tumor Type Advanced Solid Tumor
    Response Type predicted – sensitive
    Response Type resistant

    PMIDs:
    20538618 22351689


    Sources:
    MyCancerGenome TdgClinicalTrial JAX-CKB ChemblInteractions CancerCommons

  • CEP-32496   BRAF

    Interaction Score: 0.85

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Serine/threonine-protein kinase B-raf inhibitor
    Direct Interaction yes
    Indication/Tumor Type melanoma

    PMIDs:
    22319199


    Sources:
    JAX-CKB ChemblInteractions TTD

  • PLX-8394   BRAF

    Interaction Score: 0.64

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Serine/threonine-protein kinase B-raf inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • CHEMBL2144069   BRAF

    Interaction Score: 0.64

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    23398453


    Sources:
    DTC

  • XL-281   BRAF

    Interaction Score: 0.64

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Serine/threonine-protein kinase B-raf inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    MyCancerGenome ChemblInteractions TTD

  • DABRAFENIB MESYLATE   BRAF

    Interaction Score: 0.64

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Serine/threonine-protein kinase B-raf inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • CHEMBL217354   BRAF

    Interaction Score: 0.64

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Vemurafenib + TW-37
    Indication/Tumor Type non-small cell lung carcinoma
    Evidence Type Actionable

    PMIDs:
    25665005


    Sources:
    JAX-CKB

  • ZELBORAF   BRAF

    Interaction Score: 0.64

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Reported Cancer Type Melanoma

    PMIDs:
    None found


    Sources:
    CancerCommons

  • COBIMETINIB   BRAF

    Interaction Score: 0.55

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Approval Status FDA approved
    Approval Status Phase Ib/II
    combination therapy Atezolizumab + Vemurafenib + Cobimetinib

    PMIDs:
    25037139 27480103 25265494 23934108 22084396 28649441


    Sources:
    ClearityFoundationBiomarkers JAX-CKB CIViC PharmGKB FDA OncoKB

  • LY-3009120   BRAF

    Interaction Score: 0.53

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Indication/Tumor Type melanoma
    Response Type sensitive
    Approval Status Preclinical

    PMIDs:
    22798288 26732095 26343583


    Sources:
    JAX-CKB ChemblInteractions

  • LIFIRAFENIB   BRAF

    Interaction Score: 0.51

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Serine/threonine-protein kinase B-raf inhibitor
    Indication/Tumor Type Advanced Solid Tumor

    PMIDs:
    26208524


    Sources:
    JAX-CKB ChemblInteractions TTD

  • PF-04217903   BRAF

    Interaction Score: 0.42

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy ABT-263 + CGM097 + Dabrafenib + PF-04217903
    Indication/Tumor Type colorectal cancer
    Response Type sensitive

    PMIDs:
    27659046


    Sources:
    JAX-CKB

  • PAC-1   BRAF

    Interaction Score: 0.42

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    27297867


    Sources:
    JAX-CKB

  • BINIMETINIB   BRAF

    Interaction Score: 0.42

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Encorafenib + Binimetinib
    combination therapy Encorafenib + Binimetinib + Cetuximab
    Evidence Type Actionable

    PMIDs:
    26577700 29573941 28152546 23414587 27307593 31566309


    Sources:
    ClearityFoundationBiomarkers JAX-CKB CIViC PharmGKB FDA OncoKB

  • SELUMETINIB   BRAF

    Interaction Score: 0.36

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type melanoma
    Response Type decreased response
    Approval Status Preclinical

    PMIDs:
    24265152 27196754 26351322 23406027 27655129 26137449 22197931 24448821 23942066 26461489 27222538 27312529 19915144 27217440 22048237 26343583 31151904


    Sources:
    ClearityFoundationBiomarkers JAX-CKB CIViC

  • PD-0325901   BRAF

    Interaction Score: 0.35

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type colorectal cancer
    Response Type resistant
    Approval Status Preclinical

    PMIDs:
    26272063 27488531 26573800 16273091 26267534


    Sources:
    JAX-CKB

  • XL-888   BRAF

    Interaction Score: 0.32

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type melanoma
    Response Type sensitive
    Approval Status Preclinical

    PMIDs:
    22351686


    Sources:
    JAX-CKB

  • SAR-260301   BRAF

    Interaction Score: 0.32

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy SAR260301 + Selumetinib
    Indication/Tumor Type melanoma
    Response Type sensitive

    PMIDs:
    27196754


    Sources:
    JAX-CKB

  • IDELALISIB   BRAF

    Interaction Score: 0.32

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type melanoma
    Response Type no benefit
    Approval Status Preclinical

    PMIDs:
    26137449


    Sources:
    JAX-CKB

  • DEL-22379   BRAF

    Interaction Score: 0.32

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type colorectal cancer
    Response Type sensitive
    Approval Status Preclinical - Cell culture

    PMIDs:
    26267534


    Sources:
    JAX-CKB

  • ARQ-736   BRAF

    Interaction Score: 0.32

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Serine/threonine-protein kinase B-raf inhibitor

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • TAK-733   BRAF

    Interaction Score: 0.32

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type melanoma
    Response Type sensitive
    Approval Status Phase I

    PMIDs:
    26439693 24398428 22798288


    Sources:
    JAX-CKB

  • CAPMATINIB   BRAF

    Interaction Score: 0.32

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type collecting duct carcinoma
    Response Type sensitive
    Approval Status Preclinical - Pdx

    PMIDs:
    28783719


    Sources:
    JAX-CKB

  • VORUCICLIB   BRAF

    Interaction Score: 0.32

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Vemurafenib + Voruciclib
    Indication/Tumor Type melanoma
    Response Type sensitive

    PMIDs:
    None found


    Sources:
    JAX-CKB

  • DOXIL   BRAF

    Interaction Score: 0.32

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Evidence Type Actionable
    Approval Status Clinical Study
    Response Type sensitive

    PMIDs:
    21216929


    Sources:
    JAX-CKB

  • LGX-806   BRAF

    Interaction Score: 0.32

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Serine/threonine-protein kinase B-raf inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • SORAFENIB   BRAF

    Interaction Score: 0.29

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name Nexavar
    Novel drug target Established target
    Clinical Status preclinical

    PMIDs:
    20812347 16609060 17575107 11752352 16901402 16880785 18794803 19001320 24727320 20526349 18186519 25157968 22310681 20350999 19537845 12068308 20619739 14679157 21129611 26619011 28362716 24885690 23792568 22394203 23629727 27388325 20538618 28002790


    Sources:
    MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial JAX-CKB TEND DoCM CIViC MyCancerGenomeClinicalTrial PharmGKB

  • E-6201   BRAF

    Interaction Score: 0.27

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type melanoma
    Response Type sensitive
    Approval Status Preclinical

    PMIDs:
    23039341 24448821


    Sources:
    JAX-CKB

  • OBATOCLAX   BRAF

    Interaction Score: 0.25

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Evidence Type Actionable
    Approval Status Preclinical
    Response Type sensitive

    PMIDs:
    22460902


    Sources:
    JAX-CKB

  • GANETESPIB   BRAF

    Interaction Score: 0.21

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type skin melanoma
    Response Type sensitive
    Approval Status Preclinical - Cell line xenograft

    PMIDs:
    25077897 24398428


    Sources:
    JAX-CKB

  • MLN-2480   BRAF

    Interaction Score: 0.21

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction RAF serine/threonine protein kinase inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • TIVOZANIB   BRAF

    Interaction Score: 0.21

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy PLX4720 + Tivozanib
    Indication/Tumor Type melanoma
    Response Type sensitive

    PMIDs:
    26461489


    Sources:
    JAX-CKB

  • NAVITOCLAX   BRAF

    Interaction Score: 0.21

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy ABT-263 + Alpelisib + Dabrafenib + Erlotinib
    Indication/Tumor Type colorectal cancer
    Response Type sensitive

    PMIDs:
    27659046 24983357 25665005


    Sources:
    JAX-CKB

  • AEW-541   BRAF

    Interaction Score: 0.21

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy AZD6482 + NVP-AEW541
    Indication/Tumor Type melanoma
    Response Type no benefit

    PMIDs:
    26577700


    Sources:
    JAX-CKB

  • PF-00477736   BRAF

    Interaction Score: 0.21

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Approval Status Preclinical - Cell culture
    Indication/Tumor Type Advanced Solid Tumor
    Indication/Tumor Type colon cancer

    PMIDs:
    26140595


    Sources:
    JAX-CKB

  • UPROSERTIB   BRAF

    Interaction Score: 0.21

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    24265152


    Sources:
    JAX-CKB

  • CGM-097   BRAF

    Interaction Score: 0.21

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Approval Status Preclinical - Cell culture
    Indication/Tumor Type colorectal cancer
    combination therapy ABT-263 + CGM097 + Dabrafenib + PF-04217903

    PMIDs:
    27659046


    Sources:
    JAX-CKB

  • PIMASERTIB   BRAF

    Interaction Score: 0.21

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Pimasertib + Sorafenib
    Indication/Tumor Type colorectal cancer
    Response Type sensitive

    PMIDs:
    23629727


    Sources:
    ClearityFoundationBiomarkers JAX-CKB

  • PEXIDARTINIB   BRAF

    Interaction Score: 0.21

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy PLX3397 + Vemurafenib
    Indication/Tumor Type melanoma
    Response Type sensitive

    PMIDs:
    25939769


    Sources:
    JAX-CKB

  • REFAMETINIB   BRAF

    Interaction Score: 0.18

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type melanoma
    Response Type sensitive
    Approval Status Preclinical - Cell line xenograft

    PMIDs:
    19706763


    Sources:
    JAX-CKB

  • RO-4987655   BRAF

    Interaction Score: 0.18

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type melanoma
    Response Type sensitive
    Approval Status Preclinical - Cell culture

    PMIDs:
    26438159


    Sources:
    JAX-CKB

  • DASATINIB   BRAF

    Interaction Score: 0.18

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Clinical Status preclinical
    Variant Effect reduced kinase activity
    Pathway activation

    PMIDs:
    20350999 21129611 22310681 25157968 19537845 18186519 26619011 12460919 12460918 21483012 19238210 22649091 12068308 23833300 19010912 23242808 27222538


    Sources:
    JAX-CKB DoCM MyCancerGenomeClinicalTrial

  • PERTUZUMAB   BRAF

    Interaction Score: 0.16

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    29320312


    Sources:
    CIViC

  • REGORAFENIB   BRAF

    Interaction Score: 0.16

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Serine/threonine-protein kinase B-raf inhibitor
    Indication/Tumor Type colorectal cancer

    PMIDs:
    21170960 23629727 25838391


    Sources:
    MyCancerGenome JAX-CKB ChemblInteractions MyCancerGenomeClinicalTrial

  • ALPELISIB   BRAF

    Interaction Score: 0.14

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Alpelisib + PLX4720
    Indication/Tumor Type melanoma
    Response Type sensitive

    PMIDs:
    27659046 27924459 28363909 26577700 27312529


    Sources:
    JAX-CKB CIViC

  • EVEROLIMUS   BRAF

    Interaction Score: 0.13

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Everolimus + Selumetinib
    Indication/Tumor Type malignant glioma
    Response Type predicted – sensitive

    PMIDs:
    20664172 20664174 23629727 27797976 27217440 29156677


    Sources:
    JAX-CKB CIViC

  • AFATINIB   BRAF

    Interaction Score: 0.13

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Evidence Type Actionable
    Approval Status Preclinical
    Response Type sensitive

    PMIDs:
    26916115


    Sources:
    JAX-CKB

  • TEMSIROLIMUS   BRAF

    Interaction Score: 0.13

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    combination therapy Bevacizumab + Temsirolimus + Doxil
    Indication/Tumor Type ovarian carcinoma
    Response Type sensitive

    PMIDs:
    21216929


    Sources:
    JAX-CKB MyCancerGenomeClinicalTrial

  • BEVACIZUMAB   BRAF

    Interaction Score: 0.12

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Bevacizumab + Temsirolimus + Doxil
    Indication/Tumor Type ovarian carcinoma
    Response Type sensitive

    PMIDs:
    21216929 19603024 22180495 19571295


    Sources:
    JAX-CKB CIViC

  • IRINOTECAN   BRAF

    Interaction Score: 0.12

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Cetuximab + Irinotecan
    Indication/Tumor Type colorectal cancer
    Response Type resistant

    PMIDs:
    28783719 26989027 22180495 26687137 19603024 27729313 25714871 19603018


    Sources:
    JAX-CKB CIViC

  • GSK-2636771   BRAF

    Interaction Score: 0.12

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy GSK2636771 + Pembrolizumab
    combination therapy GSK2636771 + unspecified IGF-1R antibody
    combination therapy BYL719 + GSK2636771 + LGX818

    PMIDs:
    26577700 26645196


    Sources:
    JAX-CKB

  • NERATINIB   BRAF

    Interaction Score: 0.12

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type colorectal cancer
    Response Type sensitive
    Approval Status Preclinical

    PMIDs:
    26243863


    Sources:
    JAX-CKB

  • PEMBROLIZUMAB   BRAF

    Interaction Score: 0.12

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type melanoma
    Response Type no benefit
    Approval Status Preclinical

    PMIDs:
    26645196


    Sources:
    JAX-CKB PharmGKB FDA

  • VENETOCLAX   BRAF

    Interaction Score: 0.12

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Evidence Type Actionable
    Approval Status Preclinical - Cell culture
    Response Type no benefit

    PMIDs:
    27974663


    Sources:
    JAX-CKB

  • CI-1040   BRAF

    Interaction Score: 0.11

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type Advanced Solid Tumor
    Response Type sensitive
    Approval Status Preclinical

    PMIDs:
    19018267 19915144 20538618


    Sources:
    JAX-CKB

  • AZD-6482   BRAF

    Interaction Score: 0.11

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy AZD6482 + NVP-AEW541
    Indication/Tumor Type melanoma
    Response Type no benefit

    PMIDs:
    26577700


    Sources:
    JAX-CKB

  • PA-799   BRAF

    Interaction Score: 0.11

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type breast cancer
    Response Type decreased response
    Approval Status Preclinical - Cell line xenograft

    PMIDs:
    21558396


    Sources:
    JAX-CKB

  • LENVATINIB   BRAF

    Interaction Score: 0.11

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Evidence Type Actionable
    Approval Status Phase I
    Response Type sensitive

    PMIDs:
    26169970


    Sources:
    JAX-CKB

  • SARACATINIB   BRAF

    Interaction Score: 0.11

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type melanoma
    Response Type sensitive
    Approval Status Preclinical

    PMIDs:
    23242808


    Sources:
    JAX-CKB

  • SAPANISERTIB   BRAF

    Interaction Score: 0.09

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy MLN0128 + PD-0325901
    Indication/Tumor Type colorectal cancer
    Response Type sensitive

    PMIDs:
    26272063 25261369


    Sources:
    JAX-CKB

  • GEDATOLISIB   BRAF

    Interaction Score: 0.09

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type colon cancer
    Response Type sensitive
    Approval Status Preclinical

    PMIDs:
    17314276 21325073 24042735


    Sources:
    JAX-CKB

  • OXALIPLATIN   BRAF

    Interaction Score: 0.09

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    26637369 19603024 19571295


    Sources:
    JAX-CKB CIViC

  • NIVOLUMAB   BRAF

    Interaction Score: 0.08

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB FDA

  • PICTILISIB   BRAF

    Interaction Score: 0.08

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy GDC0879 + GDC-0941
    Indication/Tumor Type melanoma
    Response Type sensitive

    PMIDs:
    26577700 24265153 19276360


    Sources:
    JAX-CKB

  • RIBOCICLIB   BRAF

    Interaction Score: 0.08

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Encorafenib + Ribociclib
    Indication/Tumor Type melanoma
    Response Type sensitive

    PMIDs:
    28351928


    Sources:
    JAX-CKB

  • ERLOTINIB   BRAF

    Interaction Score: 0.08

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Erlotinib + PLX4720
    Indication/Tumor Type melanoma
    Response Type sensitive

    PMIDs:
    27659046 22448344 27924459 22180495


    Sources:
    JAX-CKB CIViC

  • BUPARLISIB   BRAF

    Interaction Score: 0.08

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Binimetinib + BKM120
    Indication/Tumor Type melanoma
    Response Type sensitive

    PMIDs:
    24265152 27307593


    Sources:
    JAX-CKB

  • PANOBINOSTAT   BRAF

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    21464044


    Sources:
    JAX-CKB

  • MK-2206   BRAF

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Evidence Type Actionable
    combination therapy MK2206 + Trametinib
    Indication/Tumor Type melanoma

    PMIDs:
    24265152


    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

  • OMIPALISIB   BRAF

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Dabrafenib + GSK2126458
    Indication/Tumor Type melanoma
    Response Type sensitive

    PMIDs:
    22389471


    Sources:
    JAX-CKB

  • PILARALISIB   BRAF

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type melanoma
    Response Type sensitive
    Approval Status Preclinical - Cell line xenograft

    PMIDs:
    25637314


    Sources:
    JAX-CKB

  • TRASTUZUMAB   BRAF

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Fluorouracil + Leucovorin + Trastuzumab
    Indication/Tumor Type rectum adenocarcinoma
    Response Type no benefit

    PMIDs:
    27626067


    Sources:
    JAX-CKB

  • PONATINIB   BRAF

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    31937621


    Sources:
    CIViC

  • DACTOLISIB   BRAF

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy BEZ235 + Vemurafenib
    Indication/Tumor Type melanoma
    Response Type sensitive

    PMIDs:
    23549875 26137449


    Sources:
    JAX-CKB CIViC

  • GEFITINIB   BRAF

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type melanoma
    combination therapy Gefitinib + PLX4720
    Evidence Type Actionable

    PMIDs:
    27312529 23242808 22448344 22281684


    Sources:
    JAX-CKB CIViC

  • CAPECITABINE   BRAF

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22180495 19571295


    Sources:
    CIViC

  • ATEZOLIZUMAB   BRAF

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Atezolizumab + Vemurafenib + Cobimetinib
    Indication/Tumor Type melanoma
    Response Type sensitive

    PMIDs:
    None found


    Sources:
    JAX-CKB

  • LEUCOVORIN   BRAF

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Fluorouracil + Leucovorin + Trastuzumab
    Indication/Tumor Type rectum adenocarcinoma
    Response Type no benefit

    PMIDs:
    27626067


    Sources:
    JAX-CKB

  • PALBOCICLIB   BRAF

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type melanoma
    Response Type sensitive
    Approval Status Preclinical - Cell culture

    PMIDs:
    26369631 27488531


    Sources:
    JAX-CKB

  • SORAFENIB TOSYLATE   BRAF

    Interaction Score: 0.04

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Serine/threonine-protein kinase B-raf inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • VORINOSTAT   BRAF

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    27924459


    Sources:
    JAX-CKB

  • CEDIRANIB   BRAF

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Response Type sensitive
    combination therapy Cediranib + Selumetinib + PLX4720
    Indication/Tumor Type melanoma

    PMIDs:
    26461489


    Sources:
    JAX-CKB

  • IMATINIB   BRAF

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Approval Status Preclinical - Cell line xenograft
    combination therapy Imatinib + PLX4720
    Evidence Type Actionable

    PMIDs:
    27924459


    Sources:
    JAX-CKB

  • FLUOROURACIL   BRAF

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Fluorouracil + Leucovorin + Trastuzumab
    Indication/Tumor Type rectum adenocarcinoma
    Response Type no benefit

    PMIDs:
    26637369 27626067


    Sources:
    JAX-CKB

  • DOXORUBICIN   BRAF

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy PLX4720 + Doxorubicin
    Indication/Tumor Type melanoma
    Response Type sensitive

    PMIDs:
    27924459


    Sources:
    JAX-CKB

  • Ensembl: ENSG00000157764

    • Version: 101_38

    Alternate Names:
    BRAF Ensembl Gene Name

    Gene Info:
    Gene Biotype PROTEIN_CODING

    Publications:

  • TdgClinicalTrial: P15056

    • Version: January-2014

    Alternate Names:
    BRAF Gene Symbol

    Gene Info:
    Target Class Enzymes
    Target Subclass EC:2.7.11.1

    Publications:

  • RussLampel: ENSG00000157764

    • Version: 26-July-2011

    Alternate Names:
    ENSG00000157764 Ensembl Gene Id
    BRAF Display Id
    B-RAF PROTO-ONCOGENE SERINE/THREONINE-PROTEIN KINASE (EC 2.7.1.37) (P94) (V-RAF MURINE SARCOMA VIRAL ONCOGENE HOMOLOG B1). [SOURCE:UNIPROT/SWISSPROT;ACC:P15056] Description

    Gene Info:
    Human Readable Name DRUGGABLE GENOME

    Gene Categories:
    DRUGGABLE GENOME

    Publications:

  • TEND: P15056

    • Version: 01-August-2011

    Alternate Names:
    BRAF1_HUMAN Uniprot Id
    ENSG00000157764 Ensembl Gene Id
    P15056 Uniprot Accession

    Gene Info:
    Target Subclass 2.7.11.1
    Target Main Class Enzymes

    Publications:

  • CancerCommons: BRAF

    • Version: 25-July-2013

    Alternate Names:
    673 Entrez Gene ID

    Gene Info:
    CancerCommons Reported Gene Name BRAF (V660) E/K
    CancerCommons Reported Gene Name BRAF
    CancerCommons Reported Gene Name Pan-RAF

    Publications:

  • HopkinsGroom: P15056

    • Version: 11-September-2012

    Alternate Names:
    SERINE/THREONINE-PROTEIN KINASE B-RAF Uniprot Protein Name
    BRAF_HUMAN Uniprot Id
    673 Entrez Gene Id

    Gene Info:
    Interpro Short Name Ser-Thr/Tyr_kinase_cat_dom
    Interpro Name Serine-threonine/tyrosine-protein kinase catalytic domain
    Uniprot Evidence 1: Evidence at protein level

    Gene Categories:
    KINASE, DRUGGABLE GENOME

    Publications:

  • JAX-CKB: BRAF

    • Version: 27-September-2017

    Alternate Names:
    673 CKB Entrez Id
    BRAF CKB Gene Synonym
    B-raf CKB Gene Synonym

    Gene Info:

    Publications:
    Mok et al., 2015, Inhibition of colony stimulating factor-1 receptor improves antitumor efficacy of BRAF inhibition., BMC Cancer
    Martinelli et al., 2013, Antitumor activity of pimasertib, a selective MEK 1/2 inhibitor, in combination with PI3K/mTOR inhibitors or with multi-targeted kinase inhibitors in pimasertib-resistant human lung and colorectal cancer cells., Int. J. Cancer
    Okimoto RA et al., 2016 Nov 22, Preclinical efficacy of a RAF inhibitor that evades paradoxical MAPK pathway activation in protein kinase BRAF-mutant lung cancer., Proc Natl Acad Sci U S A

  • PharmGKB: BRAF

    • Version: 18-August-2020

    Alternate Names:
    PA25408 PharmGKB ID

    Gene Info:

    Publications:
    Gong L et al., 2017, PharmGKB summary: sorafenib pathways., Pharmacogenet Genomics

  • CIViC: BRAF

    • Version: 14-September-2020

    Alternate Names:
    673 Entrez Gene ID
    5 CIViC Gene ID

    Gene Info:

    Gene Categories:
    DRUG RESISTANCE, CLINICALLY ACTIONABLE

    Publications:
    Rad et al., 2013, A genetic progression model of Braf(V600E)-induced intestinal tumorigenesis reveals targets for therapeutic intervention., Cancer Cell
    Loaiza-Bonilla A et al., 2014, Dramatic response to dabrafenib and trametinib combination in a BRAF V600E-mutated cholangiocarcinoma: implementation of a molecular tumour board and next-generation sequencing for personalized medicine., Ecancermedicalscience
    Kocsis J et al., 2017, Combined dabrafenib and trametinib treatment in a case of chemotherapy-refractory extrahepatic BRAF V600E mutant cholangiocarcinoma: dramatic clinical and radiological response with a confusing synchronic new liver lesion., J Gastrointest Oncol

  • DoCM: BRAF

    • Version: 27-September-2017

    Alternate Names:

    Gene Info:

    Publications:
    Flaherty et al., 2012, Combined BRAF and MEK inhibition in melanoma with BRAF V600 mutations., N. Engl. J. Med.
    Falchook et al., 2012, Dabrafenib in patients with melanoma, untreated brain metastases, and other solid tumours: a phase 1 dose-escalation trial., Lancet
    Chang et al., 2016, Identifying recurrent mutations in cancer reveals widespread lineage diversity and mutational specificity., Nat. Biotechnol.

  • DTC: BRAF

    • Version: 02-September-2020

    Alternate Names:

    Gene Info:

    Publications:
    Yang W et al., 2015, Design, synthesis and biological evaluation of bis-aryl ureas and amides based on 2-amino-3-purinylpyridine scaffold as DFG-out B-Raf kinase inhibitors., Eur J Med Chem
    Vasbinder MM et al., 2013, Discovery and optimization of a novel series of potent mutant B-Raf(V600E) selective kinase inhibitors., J Med Chem

  • HingoraniCasas: ENSG00000157764

    • Version: 31-May-2017

    Alternate Names:
    ENSG00000157764 Gene Symbol
    BRAF Ensembl Id

    Gene Info:

    Gene Categories:
    DRUGGABLE GENOME

    Publications:

  • TALC: BRAF

    • Version: 12-May-2016

    Alternate Names:
    BRAF Gene Symbol

    Gene Info:

    Publications:

  • MyCancerGenome: BRAF

    • Version: 20-Jun-2017

    Alternate Names:
    673 Entrez Gene Id
    BRAF MyCancerGenome Gene Symbol
    BRAF MyCancerGenome Reported Gene Name

    Gene Info:

    Publications:

  • ChemblInteractions: BRAF1

    • Version: chembl_23

    Alternate Names:
    RAFB1 GENE_SYMBOL
    BRAF GENE_SYMBOL
    Serine/threonine-protein kinase B-raf UNIPROT

    Gene Info:

    Publications:

  • OncoKB: BRAF

    • Version: 23-July-2020

    Alternate Names:
    673 OncoKB Entrez Id
    NS7 OncoKB Gene Synonym
    B-raf OncoKB Gene Synonym

    Gene Info:

    Publications:

  • GO: BRAF

    • Version: 01-February-2022

    Alternate Names:
    BRAF1 GO Gene Synonym
    RAFB1 GO Gene Synonym

    Gene Info:

    Gene Categories:
    SERINE THREONINE KINASE

    Publications:

  • Tempus: BRAF

    • Version: 11-November-2018

    Alternate Names:
    BRAF Gene Symbol

    Gene Info:

    Gene Categories:
    CLINICALLY ACTIONABLE

    Publications:

  • dGene: BRAF

    • Version: 27-Jun-2013

    Alternate Names:
    673 Gene ID
    B-RAF1 dGene Synonym
    BRAF1 dGene Synonym

    Gene Info:

    Gene Categories:
    KINASE, SERINE THREONINE KINASE

    Publications:

  • TTD: Serine/threonine-protein kinase B-raf

    • Version: 2020.06.01

    Alternate Names:
    BRAF TTD Gene Abbreviation
    T99089 TTD Target ID

    Gene Info:

    Publications:

  • Pharos: BRAF

    • Version: 01-February-2022

    Alternate Names:
    Serine/threonine-protein kinase B-raf Gene Name
    P15056 UniProt ID

    Gene Info:

    Gene Categories:
    KINASE

    Publications:

  • ClearityFoundationBiomarkers: BRAF

    • Version: 26-July-2013

    Alternate Names:

    Gene Info:

    Publications:

  • ClearityFoundationClinicalTrial: BRAF

    • Version: 15-June-2013

    Alternate Names:

    Gene Info:

    Publications:

  • MyCancerGenomeClinicalTrial: BRAF

    • Version: 30-February-2014

    Alternate Names:

    Gene Info:

    Publications:

  • MskImpact: BRAF

    • Version: May-2015

    Alternate Names:

    Gene Info:

    Gene Categories:
    CLINICALLY ACTIONABLE

    Publications:

  • FoundationOneGenes: BRAF

    • Version: 03-September-2020

    Alternate Names:

    Gene Info:

    Gene Categories:
    CLINICALLY ACTIONABLE

    Publications:

  • CarisMolecularIntelligence: BRAF

    • Version: 04-September-2020

    Alternate Names:

    Gene Info:

    Gene Categories:
    CLINICALLY ACTIONABLE

    Publications:

  • FDA: BRAF

    • Version: 04-September-2020

    Alternate Names:

    Gene Info:

    Publications:

  • Oncomine: BRAF

    • Version: v3

    Alternate Names:

    Gene Info:

    Gene Categories:
    CLINICALLY ACTIONABLE

    Publications:

  • COSMIC: BRAF

    • Version: 4-Sep-2020

    Alternate Names:

    Gene Info:

    Gene Categories:
    DRUG RESISTANCE

    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.

The dgidb.org website does not provide any medical or healthcare products, services or advice, and is not for medical emergencies or urgent situations. IF YOU THINK YOU MAY HAVE A MEDICAL EMERGENCY, CALL YOUR DOCTOR OR 911 IMMEDIATELY. Information contained on this website is not a substitute for a doctor's medical judgment or advice. We recommend that you discuss your specific, individual health concerns with your doctor or health care professional.

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