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DABRAFENIB Drug Record

  • Summary
  • Interactions
  • Claims
  • DABRAFENIB chembl:CHEMBL2028663 ApprovedAntineoplastic

    Alternate Names:

    GSK2118436A
    DABRAFENIB
    TAFINLAR
    GSK-2118436A
    GSK-2118436
    GSK2118436
    TAFINLAR®
    DRB436
    rxcui:1424911
    pubchem.compound:44462760
    drugbank:08912
    chemidplus:1195765-45-7
    chembl:CHEMBL2028663

    Drug Info:

    Pharmaceutical Developer GlaxoSmithKline
    Source Reported Drug Name(s) Dabrafenib/GSK2118436
    Drug Class RAF Inhibitor
    FDA Approval Melanoma (with BRAF V600 mutation)
    Drug Class Kinase Inhibitors
    FDA Approval not approved
    Drug Class Small molecule
    Drug Indications antineoplastic agent
    (10 More Sources)

    Publications:

    Lu et al., 2017, Engineering and Functional Characterization of Fusion Genes Identifies Novel Oncogenic Drivers of Cancer., Cancer Res.
    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.
    Shen et al., 2016, Loss of cohesin complex components STAG2 or STAG3 confers resistance to BRAF inhibition in melanoma., Nat. Med.
    Horn et al., 2016, High-Order Drug Combinations Are Required to Effectively Kill Colorectal Cancer Cells., Cancer Res.
    2016, Triple Therapy Improves Colorectal Cancer Response., Cancer Discov
    Falchook et al., 2012, Dabrafenib in patients with melanoma, untreated brain metastases, and other solid tumours: a phase 1 dose-escalation trial., Lancet
    Chen et al., 2016, Oncogenic BRAF Deletions That Function as Homodimers and Are Sensitive to Inhibition by RAF Dimer Inhibitor LY3009120., Cancer Discov
    Casadevall et al., 2016, Dabrafenib in an elderly patient with metastatic melanoma and BRAF V600R mutation: a case report., J Med Case Rep
    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
    Van Allen et al., 2014, The genetic landscape of clinical resistance to RAF inhibition in metastatic melanoma., Cancer Discov
    Wagle et al., 2014, MAP kinase pathway alterations in BRAF-mutant melanoma patients with acquired resistance to combined RAF/MEK inhibition., Cancer Discov
    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.
    Klempner et al., 2016, BRAFV600E Mutations in High-Grade Colorectal Neuroendocrine Tumors May Predict Responsiveness to BRAF-MEK Combination Therapy., Cancer Discov
    Agarwal et al., 2016, Response to Targeted Therapy in BRAF Mutant Anaplastic Thyroid Cancer., J Natl Compr Canc Netw
    Drobysheva et al., 2017, Targeted MAPK Pathway Inhibitors in Patients With Disseminated Pilocytic Astrocytomas., J Natl Compr Canc Netw
    Schreuer et al., 2017, Combination of dabrafenib plus trametinib for BRAF and MEK inhibitor pretreated patients with advanced BRAF(V600)-mutant melanoma: an open-label, single arm, dual-centre, phase 2 clinical trial., Lancet Oncol.
    Hauschild et al., 2012, Dabrafenib in BRAF-mutated metastatic melanoma: a multicentre, open-label, phase 3 randomised controlled trial., Lancet
    Hirschi et al., 2014, Genetic targeting of B-RafV600E affects survival and proliferation and identifies selective agents against BRAF-mutant colorectal cancer cells., Mol. Cancer
    Oddo et al., 2016, Molecular Landscape of Acquired Resistance to Targeted Therapy Combinations in BRAF-Mutant Colorectal Cancer., Cancer Res.
    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.
    Gibson et al., 2017, Genomic Heterogeneity and Exceptional Response to Dual Pathway Inhibition in Anaplastic Thyroid Cancer., Clin. Cancer Res.
    Carlino et al., 2015, Preexisting MEK1P124 mutations diminish response to BRAF inhibitors in metastatic melanoma patients., Clin. Cancer Res.
    Karoulia et al., 2016, An Integrated Model of RAF Inhibitor Action Predicts Inhibitor Activity against Oncogenic BRAF Signaling., Cancer Cell
    Shi H et al., 2014, Acquired resistance and clonal evolution in melanoma during BRAF inhibitor therapy., Cancer Discov
    Long GV et al., 2014, Increased MAPK reactivation in early resistance to dabrafenib/trametinib combination therapy of BRAF-mutant metastatic melanoma., Nat Commun
    Ahronian et al., 2015, Clinical Acquired Resistance to RAF Inhibitor Combinations in BRAF-Mutant Colorectal Cancer through MAPK Pathway Alterations., Cancer Discov
    Larkin et al., 2014, Combined vemurafenib and cobimetinib in BRAF-mutated melanoma., N. Engl. J. Med.
    Ponti et al., 2012, Overwhelming response to Dabrafenib in a patient with double BRAF mutation (V600E; V600M) metastatic malignant melanoma., J Hematol Oncol
    Subbiah V et al., 2018, Dabrafenib and Trametinib Treatment in Patients With Locally Advanced or Metastatic BRAF V600-Mutant Anaplastic Thyroid Cancer., J Clin Oncol
    Flaherty et al., 2012, Combined BRAF and MEK inhibition in melanoma with BRAF V600 mutations., N. Engl. J. Med.
    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
    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
    Robert et al., 2015, Improved overall survival in melanoma with combined dabrafenib and trametinib., N. Engl. J. Med.
    Planchard et al., 2016, Dabrafenib plus trametinib in patients with previously treated BRAF(V600E)-mutant metastatic non-small cell lung cancer: an open-label, multicentre phase 2 trial., Lancet Oncol.
    Menzies et al., 2014, Dabrafenib and trametinib, alone and in combination for BRAF-mutant metastatic melanoma., Clin. Cancer Res.
    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
    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.
    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.
    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
    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
    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.
    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
    Garner et al., 1975, Effect of pH on substrate and inhibitor kinetic constants of human liver alanine aminopeptidase. Evidence for two ionizable active center groups., Biochemistry
    Poole-Wilson et al., 1975, Effect of pH on ionic exchange and function in rat and rabbit myocardium., Am. J. Physiol.
    Fioravanti et al., 1976, Pyridine nucleotide transhydrogenases of parasitic helminths., Arch. Biochem. Biophys.
    Bland et al., 1976, Rapid infusion of sodium bicarbonate and albumin into high-risk premature infants soon after birth: a controlled, prospective trial., Am. J. Obstet. Gynecol.
    Sakaguchi et al., 1976, Microbiological oxidation of synthetic chalcocite and covellite by Thiobacillus ferrooxidans., Appl. Environ. Microbiol.
    Silen et al., 1975, Acid-base balance in amphibian gastric mucosa., Am. J. Physiol.
    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
    Noeparast A et al., 2016, Non-V600 BRAF mutations recurrently found in lung cancer predict sensitivity to the combination of Trametinib and Dabrafenib., Oncotarget
    Watson et al., 2014, The RAC1 P29S hotspot mutation in melanoma confers resistance to pharmacological inhibition of RAF., Cancer Res.
    Kulkarni D et al., 2016, Pyrexia in dabrafenib-treated melanoma patients is not associated with common genetic variation or HLA polymorphisms., Pharmacogenomics
    Rizos et al., 2014, BRAF inhibitor resistance mechanisms in metastatic melanoma: spectrum and clinical impact., Clin. Cancer Res.
    Maertens et al., 2013, Elucidating distinct roles for NF1 in melanomagenesis., Cancer Discov
    Souroullas et al., 2016, An oncogenic Ezh2 mutation induces tumors through global redistribution of histone 3 lysine 27 trimethylation., Nat. Med.
    Wang et al., 2017, ATXN1L, CIC, and ETS Transcription Factors Modulate Sensitivity to MAPK Pathway Inhibition., Cell Rep
  • 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

  • DABRAFENIB   ATXN1L

    Interaction Score: 2.17

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    28178529


    Sources:
    CIViC

  • DABRAFENIB   RAC1

    Interaction Score: 1.22

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    25056119 24265153


    Sources:
    CIViC

  • DABRAFENIB   EZH2

    Interaction Score: 0.93

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    27135738


    Sources:
    CIViC

  • DABRAFENIB   NF1

    Interaction Score: 0.81

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    23171796


    Sources:
    CIViC

  • DABRAFENIB   STAG2

    Interaction Score: 0.81

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Trametinib + Dabrafenib
    Indication/Tumor Type melanoma
    Response Type decreased response

    PMIDs:
    27500726


    Sources:
    JAX-CKB

  • DABRAFENIB   MAP2K1

    Interaction Score: 0.59

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Dabrafenib + SCH772984
    Indication/Tumor Type colorectal cancer
    Response Type sensitive

    PMIDs:
    24463458 25370473 22389471 24265154 24265153 27312529 25673644


    Sources:
    JAX-CKB CIViC

  • DABRAFENIB   NRAS

    Interaction Score: 0.42

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    27523909 22389471 25452114


    Sources:
    JAX-CKB CIViC PharmGKB

  • DABRAFENIB   CDKN2A

    Interaction Score: 0.31

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    24265155


    Sources:
    CIViC

  • DABRAFENIB   MAP2K2

    Interaction Score: 0.24

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    25452114 24265153


    Sources:
    CIViC

  • DABRAFENIB   HLA-DRB1

    Interaction Score: 0.21

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    27023328


    Sources:
    PharmGKB

  • DABRAFENIB   MITF

    Interaction Score: 0.12

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    24265153


    Sources:
    CIViC

  • DABRAFENIB   HRAS

    Interaction Score: 0.1

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • DABRAFENIB   G6PD

    Interaction Score: 0.09

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB FDA

  • DABRAFENIB   AKT1

    Interaction Score: 0.09

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    24265155


    Sources:
    CIViC

  • DABRAFENIB   KRAS

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    27312529


    Sources:
    JAX-CKB PharmGKB

  • DABRAFENIB   PIK3CA

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Dabrafenib + Everolimus + Trametinib
    Indication/Tumor Type thyroid carcinoma
    Response Type sensitive

    PMIDs:
    27797976


    Sources:
    JAX-CKB

  • DABRAFENIB   EGFR

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    27312529


    Sources:
    JAX-CKB

  • DABRAFENIB   TP53

    Interaction Score: 0.02

    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

  • CancerCommons: DABRAFENIB

    • Version: 25-July-2013

    Alternate Names:
    44462760 PubChem Drug ID
    Dabrafenib Drug Trade Name
    Dabrafenib Drug Development Name

    Drug Info:
    Drug Class RAF Inhibitor
    Source Reported Drug Name(s) Dabrafenib/GSK2118436
    Pharmaceutical Developer GlaxoSmithKline

    Publications:

  • MyCancerGenome: DABRAFENIB

    • Version: 20-Jun-2017

    Alternate Names:
    DABRAFENIB Generic Name

    Drug Info:
    Drug Class Kinase Inhibitors
    FDA Approval Melanoma (with BRAF V600 mutation)

    Publications:

  • TdgClinicalTrial: GSK2118436

    • Version: January-2014

    Alternate Names:

    Drug Info:
    Drug Indications antineoplastic agent
    Drug Class Small molecule
    FDA Approval not approved

    Publications:

  • JAX-CKB: Dabrafenib

    • Version: 27-September-2017

    Alternate Names:

    Drug Info:

    Publications:
    Carlino et al., 2015, Preexisting MEK1P124 mutations diminish response to BRAF inhibitors in metastatic melanoma patients., Clin. Cancer Res.
    Van Allen et al., 2014, The genetic landscape of clinical resistance to RAF inhibition in metastatic melanoma., Cancer Discov
    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.

  • DoCM: DABRAFENIB

    • Version: 27-September-2017

    Alternate Names:

    Drug 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.

  • PharmGKB: dabrafenib

    • Version: 18-August-2020

    Alternate Names:

    Drug Info:

    Publications:
    Kulkarni D et al., 2016, Pyrexia in dabrafenib-treated melanoma patients is not associated with common genetic variation or HLA polymorphisms., Pharmacogenomics

  • CIViC: DABRAFENIB

    • Version: 14-September-2020

    Alternate Names:

    Drug Info:

    Publications:
    Van Allen et al., 2014, The genetic landscape of clinical resistance to RAF inhibition in metastatic melanoma., Cancer Discov
    Ahronian et al., 2015, Clinical Acquired Resistance to RAF Inhibitor Combinations in BRAF-Mutant Colorectal Cancer through MAPK Pathway Alterations., Cancer Discov
    Shi H et al., 2014, Acquired resistance and clonal evolution in melanoma during BRAF inhibitor therapy., Cancer Discov

  • TALC: DABRAFENIB

    • Version: 12-May-2016

    Alternate Names:
    DABRAFENIB Primary Drug Name
    DABRAFENIB Drug Generic Name
    TAFINLAR Drug Trade Name

    Drug Info:

    Publications:

  • TTD: Dabrafenib

    • Version: 2020.06.01

    Alternate Names:
    D05ROI TTD Drug ID

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL2028663

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

  • MyCancerGenomeClinicalTrial: GSK2118436

    • Version: 30-February-2014

    Alternate Names:

    Drug Info:

    Publications:

  • OncoKB: Dabrafenib

    • Version: 23-July-2020

    Alternate Names:

    Drug Info:

    Publications:

  • FDA: Dabrafenib

    • Version: 04-September-2020

    Alternate Names:

    Drug Info:

    Publications:

  • COSMIC: Dabrafenib

    • Version: 4-Sep-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