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SORAFENIB Drug Record

  • Summary
  • Interactions
  • Claims
  • SORAFENIB chembl:CHEMBL1336 ApprovedAntineoplasticImmunotherapy

    Alternate Names:

    NEXAVAR
    SORAFENIB
    BAY-43-9006
    N-(4-CHLORO-3-(TRIFLUOROMETHYL)PHENYL)-N'-(4-(2-(N-METHYLCARBAMOYL)-4-PYRIDYLOXY)PHENYL)UREA
    SORAFENIBUM
    NEXAVAR®
    4-(4-((((4-CHLORO-3-(TRIFLUOROMETHYL)PHENYL)AMINO)CARBONYL)AMINO)PHENOXY)-N-METHYL-2-PYRIDINECARBOXAMIDE
    BAY 43-9006
    chemidplus:284461-73-0
    pubchem.compound:216239
    chembl:CHEMBL1336
    drugbank:00398
    rxcui:495881

    Drug Info:

    FDA Approval approved
    Drug Class Small Molecule
    Drug Indications antineoplastic agent
    Drug Class antineoplastic agents, protein kinase inhibitors
    Year of Approval 2005
    FDA Approval Hepatocellular carcinoma, Renal cell carcinoma, Thyroid carcinoma
    Drug Class Kinase Inhibitors
    (11 More Sources)

    Publications:

    Handolias et al., 2010, Clinical responses observed with imatinib or sorafenib in melanoma patients expressing mutations in KIT., Br. J. Cancer
    Quintás-Cardama et al., 2008, Complete response of stage IV anal mucosal melanoma expressing KIT Val560Asp to the multikinase inhibitor sorafenib., Nat Clin Pract Oncol
    Bisagni et al., 2009, Long lasting response to the multikinase inhibitor bay 43-9006 (Sorafenib) in a heavily pretreated metastatic thymic carcinoma., J Thorac Oncol
    Guo et al., 2007, Sorafenib inhibits the imatinib-resistant KITT670I gatekeeper mutation in gastrointestinal stromal tumor., Clin. Cancer Res.
    Schirosi et al., 2012, Activating c-KIT mutations in a subset of thymic carcinoma and response to different c-KIT inhibitors., Ann. Oncol.
    Woodman et al., 2009, Activity of dasatinib against L576P KIT mutant melanoma: molecular, cellular, and clinical correlates., Mol. Cancer Ther.
    Cascone et al., 2007, Combined targeted therapies in non-small cell lung cancer: a winner strategy?, Curr Opin Oncol
    Koch et al., 2006, Does the expression of c-kit (CD117) in neuroendocrine tumors represent a target for therapy?, Ann. N. Y. Acad. Sci.
    Liu et al., 2006, Sorafenib blocks the RAF/MEK/ERK pathway, inhibits tumor angiogenesis, and induces tumor cell apoptosis in hepatocellular carcinoma model PLC/PRF/5., Cancer Res.
    Guida et al., 2007, Sorafenib inhibits imatinib-resistant KIT and platelet-derived growth factor receptor beta gatekeeper mutants., Clin. Cancer Res.
    Lierman et al., 2007, The ability of sorafenib to inhibit oncogenic PDGFRbeta and FLT3 mutants and overcome resistance to other small molecule inhibitors., Haematologica
    Heinrich et al., 2012, Sorafenib inhibits many kinase mutations associated with drug-resistant gastrointestinal stromal tumors., Mol. Cancer Ther.
    Dişel et al., 2011, Promising efficacy of sorafenib in a relapsed thymic carcinoma with C-KIT exon 11 deletion mutation., Lung Cancer
    Huynh et al., 2009, Sorafenib induces growth suppression in mouse models of gastrointestinal stromal tumor., Mol. Cancer Ther.
    Falchook et al., 2015, Dual antiangiogenic inhibition: a phase I dose escalation and expansion trial targeting VEGF-A and VEGFR in patients with advanced solid tumors., Invest New Drugs
    Allegra et al., 2014, A new KIT mutation (N505I) in acral melanoma confers constitutive signaling, favors tumorigenic properties, and is sensitive to imatinib., J. Invest. Dermatol.
    Gong L et al., 2017, PharmGKB summary: sorafenib pathways., Pharmacogenet Genomics
    Escudier B et al., 2015, Genotype Correlations With Blood Pressure and Efficacy From a Randomized Phase III Trial of Second-Line Axitinib Versus Sorafenib in Metastatic Renal Cell Carcinoma., Clin Genitourin Cancer
    Zheng YB et al., 2014, The relationship of kinase insert domain receptor gene polymorphisms and clinical outcome in advanced hepatocellular carcinoma patients treated with sorafenib., Med Oncol
    Scartozzi M et al., 2014, VEGF and VEGFR genotyping in the prediction of clinical outcome for HCC patients receiving sorafenib: the ALICE-1 study., Int J Cancer
    Jain L et al., 2010, Hypertension and hand-foot skin reactions related to VEGFR2 genotype and improved clinical outcome following bevacizumab and sorafenib., J Exp Clin Cancer Res
    Maitland ML et al., 2010, Vascular endothelial growth factor pathway., Pharmacogenet Genomics
    Antonescu et al., 2009, KDR activating mutations in human angiosarcomas are sensitive to specific kinase inhibitors., Cancer Res.
    Schöffski et al., 2006, Emerging role of tyrosine kinase inhibitors in the treatment of advanced renal cell cancer: a review., Ann. Oncol.
    Adnane et al., 2006, Sorafenib (BAY 43-9006, Nexavar), a dual-action inhibitor that targets RAF/MEK/ERK pathway in tumor cells and tyrosine kinases VEGFR/PDGFR in tumor vasculature., Meth. Enzymol.
    Veronese et al., 2006, Mechanisms of hypertension associated with BAY 43-9006., J. Clin. Oncol.
    Rini, 2006, Sorafenib., Expert Opin Pharmacother
    Lacouture et al., 2006, Inflammation of actinic keratoses subsequent to therapy with sorafenib, a multitargeted tyrosine-kinase inhibitor., Clin. Exp. Dermatol.
    Machado VA et al., 2015, Synthesis, antiangiogenesis evaluation and molecular docking studies of 1-aryl-3-[(thieno[3,2-b]pyridin-7-ylthio)phenyl]ureas: Discovery of a new substitution pattern for type II VEGFR-2 Tyr kinase inhibitors., Bioorg Med Chem
    Li GB et al., 2015, LEADOPT: an automatic tool for structure-based lead optimization, and its application in structural optimizations of VEGFR2 and SYK inhibitors., Eur J Med Chem
    Imielinski et al., 2014, Oncogenic and sorafenib-sensitive ARAF mutations in lung adenocarcinoma., J. Clin. Invest.
    Doff et al., 1977, Root surface caries in the molar teeth of Rice rats. I. A method for quantitative scoring., J. Dent. Res.
    Chang et al., 2016, Identifying recurrent mutations in cancer reveals widespread lineage diversity and mutational specificity., Nat. Biotechnol.
    Unnithan et al., 2007, The role of targeted therapy in metastatic renal cell carcinoma., ScientificWorldJournal
    Gollob, 2005, Sorafenib: scientific rationales for single-agent and combination therapy in clear-cell renal cell carcinoma., Clin Genitourin Cancer
    Lu et al., 2010, Sorafenib induces growth inhibition and apoptosis of human chondrosarcoma cells by blocking the RAF/ERK/MEK pathway., J Surg Oncol
    Gridelli et al., 2007, Sorafenib and sunitinib in the treatment of advanced non-small cell lung cancer., Oncologist
    Huether et al., 2007, Sorafenib alone or as combination therapy for growth control of cholangiocarcinoma., Biochem. Pharmacol.
    Wilhelm et al., 2008, Preclinical overview of sorafenib, a multikinase inhibitor that targets both Raf and VEGF and PDGF receptor tyrosine kinase signaling., Mol. Cancer Ther.
    Gollob et al., 2006, Role of Raf kinase in cancer: therapeutic potential of targeting the Raf/MEK/ERK signal transduction pathway., Semin. Oncol.
    Smalley et al., 2009, CRAF inhibition induces apoptosis in melanoma cells with non-V600E BRAF mutations., Oncogene
    Carlomagno et al., 2006, BAY 43-9006 inhibition of oncogenic RET mutants., J. Natl. Cancer Inst.
    Wilhelm et al., 2004, BAY 43-9006 exhibits broad spectrum oral antitumor activity and targets the RAF/MEK/ERK pathway and receptor tyrosine kinases involved in tumor progression and angiogenesis., Cancer Res.
    Wilhelm et al., 2006, Discovery and development of sorafenib: a multikinase inhibitor for treating cancer., Nat Rev Drug Discov
    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
    Paz-Ares et al., 2015, Monotherapy Administration of Sorafenib in Patients With Non-Small Cell Lung Cancer (MISSION) Trial: A Phase III, Multicenter, Placebo-Controlled Trial of Sorafenib in Patients with Relapsed or Refractory Predominantly Nonsquamous Non-Small-Cell Lung Cancer after 2 or 3 Previous Treatment Regimens., J Thorac Oncol
    Dingemans et al., 2013, A phase II study of sorafenib in patients with platinum-pretreated, advanced (Stage IIIb or IV) non-small cell lung cancer with a KRAS mutation., Clin. Cancer Res.
    Wilson et al., 2016, Copy Number Changes Are Associated with Response to Treatment with Carboplatin, Paclitaxel, and Sorafenib in Melanoma., Clin. Cancer Res.
    Lim et al., 2014, A phase II study of the efficacy and safety of the combination therapy of the MEK inhibitor refametinib (BAY 86-9766) plus sorafenib for Asian patients with unresectable hepatocellular carcinoma., Clin. Cancer Res.
    Papadimitrakopoulou et al., 2016, The BATTLE-2 Study: A Biomarker-Integrated Targeted Therapy Study in Previously Treated Patients With Advanced Non-Small-Cell Lung Cancer., J. Clin. Oncol.
    Auclair et al., 2007, Antitumor activity of sorafenib in FLT3-driven leukemic cells., Leukemia
    Ravandi et al., 2013, Phase 2 study of azacytidine plus sorafenib in patients with acute myeloid leukemia and FLT-3 internal tandem duplication mutation., Blood
    Moreira et al., Clinical Response to Sorafenib in a Patient with Metastatic Colorectal Cancer and FLT3 Amplification., Case Rep Oncol
    Albers et al., 2013, The secondary FLT3-ITD F691L mutation induces resistance to AC220 in FLT3-ITD+ AML but retains in vitro sensitivity to PKC412 and Sunitinib., Leukemia
    Kancha et al., 2007, Sensitivity toward sorafenib and sunitinib varies between different activating and drug-resistant FLT3-ITD mutations., Exp. Hematol.
    Wang et al., 2012, MicroRNAs in liver disease., Gastroenterology
    Piloto et al., 2007, Prolonged exposure to FLT3 inhibitors leads to resistance via activation of parallel signaling pathways., Blood
    Mathews et al., 2007, Impact of FLT3 mutations and secondary cytogenetic changes on the outcome of patients with newly diagnosed acute promyelocytic leukemia treated with a single agent arsenic trioxide regimen., Haematologica
    Zimmerman et al., 2013, Crenolanib is active against models of drug-resistant FLT3-ITD-positive acute myeloid leukemia., Blood
    Bagrintseva et al., 2004, Mutations in the tyrosine kinase domain of FLT3 define a new molecular mechanism of acquired drug resistance to PTK inhibitors in FLT3-ITD-transformed hematopoietic cells., Blood
    Smith et al., 2013, Activity of ponatinib against clinically-relevant AC220-resistant kinase domain mutants of FLT3-ITD., Blood
    Yamamoto et al., 2001, Activating mutation of D835 within the activation loop of FLT3 in human hematologic malignancies., Blood
    MacConaill et al., 2014, Prospective enterprise-level molecular genotyping of a cohort of cancer patients., J Mol Diagn
    Mardis et al., 2009, Recurring mutations found by sequencing an acute myeloid leukemia genome., N. Engl. J. Med.
    Martelli et al., 2013, Mutational landscape of AML with normal cytogenetics: biological and clinical implications., Blood Rev.
    Allen et al., 2013, The importance of relative mutant level for evaluating impact on outcome of KIT, FLT3 and CBL mutations in core-binding factor acute myeloid leukemia., Leukemia
    Knapper et al., 2006, A phase 2 trial of the FLT3 inhibitor lestaurtinib (CEP701) as first-line treatment for older patients with acute myeloid leukemia not considered fit for intensive chemotherapy., Blood
    Man et al., 2012, Sorafenib treatment of FLT3-ITD(+) acute myeloid leukemia: favorable initial outcome and mechanisms of subsequent nonresponsiveness associated with the emergence of a D835 mutation., Blood
    Brown et al., 2005, FLT3 inhibition selectively kills childhood acute lymphoblastic leukemia cells with high levels of FLT3 expression., Blood
    Eisenhoffer et al., 2012, Crowding induces live cell extrusion to maintain homeostatic cell numbers in epithelia., Nature
    Clark et al., 2004, Variable sensitivity of FLT3 activation loop mutations to the small molecule tyrosine kinase inhibitor MLN518., Blood
    Smith et al., 2013, The role of kinase inhibitors in the treatment of patients with acute myeloid leukemia., Am Soc Clin Oncol Educ Book
    Jourdan et al., 2013, Prospective evaluation of gene mutations and minimal residual disease in patients with core binding factor acute myeloid leukemia., Blood
    Smith et al., 2012, Validation of ITD mutations in FLT3 as a therapeutic target in human acute myeloid leukaemia., Nature
    Fischer et al., 2010, Phase IIB trial of oral Midostaurin (PKC412), the FMS-like tyrosine kinase 3 receptor (FLT3) and multi-targeted kinase inhibitor, in patients with acute myeloid leukemia and high-risk myelodysplastic syndrome with either wild-type or mutated FLT3., J. Clin. Oncol.
    Baker et al., 2013, Emergence of polyclonal FLT3 tyrosine kinase domain mutations during sequential therapy with sorafenib and sunitinib in FLT3-ITD-positive acute myeloid leukemia., Clin. Cancer Res.
    Gozgit et al., 2011, Potent activity of ponatinib (AP24534) in models of FLT3-driven acute myeloid leukemia and other hematologic malignancies., Mol. Cancer Ther.
    Zhang et al., 2008, Mutant FLT3: a direct target of sorafenib in acute myelogenous leukemia., J. Natl. Cancer Inst.
    Williams AB et al., 2013, Mutations of FLT3/ITD confer resistance to multiple tyrosine kinase inhibitors., Leukemia
    Lam et al., 2010, Phase II clinical trial of sorafenib in metastatic medullary thyroid cancer., J. Clin. Oncol.
    Apsel B et al., 2008, Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases., Nat Chem Biol
    Plaza-Menacho et al., 2007, Sorafenib functions to potently suppress RET tyrosine kinase activity by direct enzymatic inhibition and promoting RET lysosomal degradation independent of proteasomal targeting., J. Biol. Chem.
    Flaherty, 2006, Chemotherapy and targeted therapy combinations in advanced melanoma., Clin. Cancer Res.
    Kim et al., 2007, Sorafenib inhibits the angiogenesis and growth of orthotopic anaplastic thyroid carcinoma xenografts in nude mice., Mol. Cancer Ther.
    Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
    Haluska et al., 2006, Therapeutic targets in melanoma: map kinase pathway., Curr Oncol Rep
    Eisen et al., 2006, Sorafenib in advanced melanoma: a Phase II randomised discontinuation trial analysis., Br. J. Cancer
    Di Nicolantonio et al., 2008, Wild-type BRAF is required for response to panitumumab or cetuximab in metastatic colorectal cancer., J. Clin. Oncol.
    Nakaoku et al., 2014, Druggable oncogene fusions in invasive mucinous lung adenocarcinoma., Clin. Cancer Res.
    Palanisamy et al., 2010, Rearrangements of the RAF kinase pathway in prostate cancer, gastric cancer and melanoma., Nat. Med.
    Bentivegna et al., 2008, Rapid identification of somatic mutations in colorectal and breast cancer tissues using mismatch repair detection (MRD)., Hum. Mutat.
    Bardelli et al., 2012, The road to resistance: EGFR mutation and cetuximab., Nat. Med.
    Tejpar et al., 2010, Prognostic and predictive biomarkers in resected colon cancer: current status and future perspectives for integrating genomics into biomarker discovery., Oncologist
    De Roock et al., 2009, Clinical biomarkers in oncology: focus on colorectal cancer., Mol Diagn Ther
    Davies et al., 2002, Mutations of the BRAF gene in human cancer., Nature
    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.
    Maldonado et al., 2003, Determinants of BRAF mutations in primary melanomas., J. Natl. Cancer Inst.
    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.
    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
    Al-Marrawi et al., 2013, Off-label use of cetuximab plus sorafenib and panitumumab plus regorafenib to personalize therapy for a patient with V600E BRAF-mutant metastatic colon cancer., Cancer Biol. Ther.
    Mangana et al., 2012, Sorafenib in melanoma., Expert Opin Investig Drugs
    Casadei Gardini et al., 2016, Efficacy of sorafenib in BRAF-mutated non-small-cell lung cancer (NSCLC) and no response in synchronous BRAF wild type-hepatocellular carcinoma: a case report., BMC Cancer
    Whittaker et al., 2010, Gatekeeper mutations mediate resistance to BRAF-targeted therapies., Sci Transl Med
    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
    Reddy et al., 2006, Sorafenib: recent update on activity as a single agent and in combination with interferon-alpha2 in patients with advanced-stage renal cell carcinoma., Clin Genitourin Cancer
    Lathia et al., 2006, Lack of effect of ketoconazole-mediated CYP3A inhibition on sorafenib clinical pharmacokinetics., Cancer Chemother. Pharmacol.
    Strumberg, 2005, Preclinical and clinical development of the oral multikinase inhibitor sorafenib in cancer treatment., Drugs Today
    Lee JH et al., 2013, Genetic predisposition of hand-foot skin reaction after sorafenib therapy in patients with hepatocellular carcinoma., Cancer
    Ho et al., 2015, The impact of FGFR1 and FRS2α expression on sorafenib treatment in metastatic renal cell carcinoma., BMC Cancer
    Boudou-Rouquette P et al., 2012, Early sorafenib-induced toxicity is associated with drug exposure and UGTIA9 genetic polymorphism in patients with solid tumors: a preliminary study., PLoS One
    Casadei Gardini A et al., 2016, eNOS polymorphisms and clinical outcome in advanced HCC patients receiving sorafenib: final results of the ePHAS study., Oncotarget
    Blumenschein et al., 2013, Comprehensive biomarker analysis and final efficacy results of sorafenib in the BATTLE trial., Clin. Cancer Res.
    Diez-Cecilia E et al., 2015, Probing a 3,4'-bis-guanidinium diaryl derivative as an allosteric inhibitor of the Ras pathway., Bioorg Med Chem Lett
    Ullrich et al., 2011, BAY 43-9006/Sorafenib blocks CSF1R activity and induces apoptosis in various classical Hodgkin lymphoma cell lines., Br. J. Haematol.
    Pan et al., 2015, Development and Characterization of Bladder Cancer Patient-Derived Xenografts for Molecularly Guided Targeted Therapy., PLoS ONE
    Lin CC et al., 2020, A GALNT14 rs9679162 genotype-guided therapeutic strategy for advanced hepatocellular carcinoma: systemic or hepatic arterial infusion chemotherapy., Pharmacogenomics J
    Zheng et al., 2015, Heme oxygenase-1 is a predictive biomarker for therapeutic targeting of advanced clear cell renal cell carcinoma treated with sorafenib or sunitinib., Onco Targets Ther
    Chen KF et al., 2012, Blockade of STAT3 activation by sorafenib derivatives through enhancing SHP-1 phosphatase activity., Eur J Med Chem
    Ferrario et al., 2016, Phase I/II Trial of Sorafenib in Combination with Vinorelbine as First-Line Chemotherapy for Metastatic Breast Cancer., PLoS ONE
    Herraez E et al., 2013, Expression of SLC22A1 variants may affect the response of hepatocellular carcinoma and cholangiocarcinoma to sorafenib., Hepatology
    Poklepovic et al., 2016, Phase I study of pemetrexed with sorafenib in advanced solid tumors., Oncotarget
    Bins S et al., 2016, Polymorphisms in SLCO1B1 and UGT1A1 are associated with sorafenib-induced toxicity., Pharmacogenomics
    Tsuchiya N et al., 2013, Risk factors for sorafenib-induced high-grade skin rash in Japanese patients with advanced renal cell carcinoma., Anticancer Drugs
    Arao et al., 2013, FGF3/FGF4 amplification and multiple lung metastases in responders to sorafenib in hepatocellular carcinoma., Hepatology
    Hu C et al., 2018, Arid1a regulates response to anti-angiogenic therapy in advanced hepatocellular carcinoma., J Hepatol
  • SORAFENIB   FGF3

    Interaction Score: 1.53

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22890726


    Sources:
    CIViC

  • SORAFENIB   MAPK4

    Interaction Score: 1.53

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20124951


    Sources:
    PharmGKB

  • SORAFENIB   MAPK6

    Interaction Score: 1.53

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20124951


    Sources:
    PharmGKB

  • SORAFENIB   SLC15A2

    Interaction Score: 0.76

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • SORAFENIB   MAPK7

    Interaction Score: 0.76

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20124951


    Sources:
    PharmGKB

  • SORAFENIB   ARAF

    Interaction Score: 0.76

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    24569458 72763 26619011


    Sources:
    MyCancerGenome DoCM CIViC PharmGKB OncoKB

  • SORAFENIB   RAF1

    Interaction Score: 0.6

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name Nexavar
    Novel drug target Established target

    PMIDs:
    28362716 20124951 20812347 17296815 17266941 16757355 18852116 17272980 16890795 18794803


    Sources:
    MyCancerGenome TdgClinicalTrial TEND MyCancerGenomeClinicalTrial PharmGKB

  • SORAFENIB   PTPN6

    Interaction Score: 0.38

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22871485


    Sources:
    DTC

  • SORAFENIB   HMOX1

    Interaction Score: 0.38

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    26309414


    Sources:
    CIViC

  • SORAFENIB   GALNT14

    Interaction Score: 0.38

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    31611591


    Sources:
    PharmGKB

  • SORAFENIB   FLT3

    Interaction Score: 0.36

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

    Interaction Info:
    Notes
    Novel drug target Established target
    Trial Name Nexavar

    PMIDs:
    17205056 17229632 23613521 25848357 23392356 28362716 17889720 22504185 17047150 17606455 24046014 14604974 23430109 11290608 25157968 19657110 23261068 23783394 16857985 22368270 15374878 22504183 15256420 23714533 23321257 22504184 20733134 23969938 21482694 18230792 22858906


    Sources:
    TALC TdgClinicalTrial JAX-CKB TEND DoCM COSMIC CIViC PharmGKB OncoKB

  • SORAFENIB   KIT

    Interaction Score: 0.34

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

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

    PMIDs:
    20372153 18936790 19461405 17699867 22357254 19671763 17272980 17102120 17178882 17545544 17229632 22665524 20970876 19139124 25363205 24317392 28362716


    Sources:
    TALC MyCancerGenome TdgClinicalTrial JAX-CKB TEND DoCM CIViC PharmGKB TTD OncoKB

  • SORAFENIB   ARID1A

    Interaction Score: 0.31

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    29113912


    Sources:
    CIViC

  • 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

  • SORAFENIB   KDR

    Interaction Score: 0.15

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

    Interaction Info:
    Notes
    Evidence Type Actionable
    Approval Status Preclinical

    PMIDs:
    28362716 25816720 25182707 24510746 20630084 20124951 19723655 16418310 16757355 16446323 16503817 16824050 26344591 25743214


    Sources:
    TALC DTC MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial JAX-CKB TEND CIViC MyCancerGenomeClinicalTrial PharmGKB TTD

  • SORAFENIB   RET

    Interaction Score: 0.15

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Indication/Tumor Type thyroid medullary carcinoma
    Response Type predicted – sensitive
    Approval Status Phase II

    PMIDs:
    28362716 16507829 15466206 17016424 20368568 18849971 17664273


    Sources:
    DTC MyCancerGenome JAX-CKB CIViC PharmGKB

  • SORAFENIB   PDGFRB

    Interaction Score: 0.14

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

    Interaction Info:
    Trial Name Nexavar
    Novel drug target Established target
    Notes

    PMIDs:
    17619763 16425993 17545544 28362716


    Sources:
    TALC DTC MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial TEND MyCancerGenomeClinicalTrial PharmGKB TTD

  • SORAFENIB   UGT1A9

    Interaction Score: 0.13

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    28362716 22912756


    Sources:
    PharmGKB

  • SORAFENIB   FLT4

    Interaction Score: 0.11

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

    Interaction Info:
    Trial Name Nexavar
    Novel drug target Established target
    Notes

    PMIDs:
    16729906 16133532 16474853 16757355 17296815 28362716


    Sources:
    TALC DTC TdgClinicalTrial TEND MyCancerGenomeClinicalTrial PharmGKB

  • SORAFENIB   SLC22A1

    Interaction Score: 0.11

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    23532667


    Sources:
    PharmGKB

  • SORAFENIB   FLT1

    Interaction Score: 0.08

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    16507829 15466206 17016424 28362716


    Sources:
    DTC MyCancerGenome MyCancerGenomeClinicalTrial PharmGKB

  • SORAFENIB   NOS3

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    27058899


    Sources:
    PharmGKB

  • SORAFENIB   DYRK3

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • SORAFENIB   MAPK13

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20124951


    Sources:
    PharmGKB

  • SORAFENIB   MAPK11

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20124951


    Sources:
    PharmGKB

  • SORAFENIB   SRPK1

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • SORAFENIB   FGFR1

    Interaction Score: 0.06

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Evidence Type Emerging
    Approval Status Phase II
    Response Type not applicable

    PMIDs:
    25900027 28362716 16507829 15466206 17016424


    Sources:
    JAX-CKB PharmGKB

  • SORAFENIB   CYP2C8

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    28362716


    Sources:
    PharmGKB

  • SORAFENIB   VEGFA

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    24510746 22736425


    Sources:
    PharmGKB

  • SORAFENIB   MAPK12

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20124951


    Sources:
    PharmGKB

  • SORAFENIB   MAPK10

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20124951


    Sources:
    PharmGKB

  • SORAFENIB   HIPK4

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • SORAFENIB   MAPK9

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20124951


    Sources:
    PharmGKB

  • SORAFENIB   CSF1R

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type Hodgkin's lymphoma
    Response Type sensitive
    Approval Status Preclinical

    PMIDs:
    21517818


    Sources:
    DTC JAX-CKB

  • SORAFENIB   HIPK2

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • SORAFENIB   MAP3K20

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • SORAFENIB   PDGFRA

    Interaction Score: 0.05

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    21482694


    Sources:
    DTC CIViC MyCancerGenomeClinicalTrial

  • SORAFENIB   MKNK2

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • SORAFENIB   KRAS

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    23629727 26743856 23224737 26307133 25294897 27480147 25363205


    Sources:
    JAX-CKB

  • SORAFENIB   EPHA2

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • SORAFENIB   CAMK2B

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • SORAFENIB   IRAK1

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • SORAFENIB   MAPK3

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20124951


    Sources:
    PharmGKB

  • SORAFENIB   CDK8

    Interaction Score: 0.04

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • SORAFENIB   MAPK8

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20124951


    Sources:
    PharmGKB

  • SORAFENIB   FGFR3

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Sorafenib + BEZ235
    Indication/Tumor Type urinary bladder cancer
    Response Type sensitive

    PMIDs:
    26270481


    Sources:
    DTC JAX-CKB

  • SORAFENIB   LIMK1

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • SORAFENIB   NRAS

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Pimasertib + Sorafenib
    Indication/Tumor Type non-small cell lung carcinoma
    Response Type sensitive

    PMIDs:
    23629727


    Sources:
    JAX-CKB

  • SORAFENIB   CYP2B6

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    28362716


    Sources:
    PharmGKB

  • SORAFENIB   MAPK14

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20124951


    Sources:
    DTC PharmGKB

  • SORAFENIB   EGFR

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Pimasertib + Sorafenib
    Approval Status Preclinical - Cell line xenograft
    Indication/Tumor Type non-small cell lung carcinoma

    PMIDs:
    23629727 26743856 24166906 26318998


    Sources:
    DTC JAX-CKB TTD

  • SORAFENIB   AXL

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • SORAFENIB   SLCO1B1

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    27533851


    Sources:
    PharmGKB

  • SORAFENIB   ABCC2

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    23237922


    Sources:
    PharmGKB

  • SORAFENIB   MINK1

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • SORAFENIB   PLK4

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • SORAFENIB   SLK

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • SORAFENIB   TAOK1

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • SORAFENIB   NTRK3

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • SORAFENIB   RPS6KB1

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • SORAFENIB   MAP4K5

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • SORAFENIB   BLK

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • SORAFENIB   TNF

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22736425


    Sources:
    PharmGKB

  • SORAFENIB   LYN

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • SORAFENIB   NTRK2

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • SORAFENIB   PIK3CA

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    23629727 25363205


    Sources:
    JAX-CKB

  • SORAFENIB   AURKA

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • SORAFENIB   PTEN

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Pemetrexed + Sorafenib
    Indication/Tumor Type Advanced Solid Tumor
    Response Type predicted – sensitive

    PMIDs:
    27213589


    Sources:
    JAX-CKB

  • SORAFENIB   NTRK1

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • SORAFENIB   MET

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Bevacizumab + Sorafenib
    Indication/Tumor Type gastrointestinal stromal tumor
    Response Type sensitive

    PMIDs:
    25363205


    Sources:
    JAX-CKB

  • SORAFENIB   AURKB

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • SORAFENIB   ABL1

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • SORAFENIB   HIF1A

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    25816720


    Sources:
    PharmGKB

  • SORAFENIB   AKT1

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Cisplatin + Gemcitabine + Sorafenib
    Indication/Tumor Type invasive bladder transitional cell carcinoma
    Response Type predicted – resistant

    PMIDs:
    None found


    Sources:
    JAX-CKB

  • SORAFENIB   ERBB2

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Approval Status Phase Ib/II
    Indication/Tumor Type Her2-receptor negative breast cancer
    combination therapy Sorafenib + Vinorelbine

    PMIDs:
    27992451


    Sources:
    JAX-CKB

  • SORAFENIB   MAPK1

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20124951


    Sources:
    PharmGKB

  • SORAFENIB   YES1

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • SORAFENIB   CYP2C9

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    28362716


    Sources:
    PharmGKB

  • SORAFENIB   ABCB1

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • SORAFENIB   CYP3A4

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    28362716


    Sources:
    PharmGKB

  • SORAFENIB   GMNN

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • MyCancerGenome: SORAFENIB

    • Version: 20-Jun-2017

    Alternate Names:
    SORAFENIB Generic Name
    NEXAVAR Trade Name

    Drug Info:
    Drug Class Kinase Inhibitors
    FDA Approval Hepatocellular carcinoma, Renal cell carcinoma, Thyroid carcinoma

    Publications:

  • TEND: SORAFENIB

    • Version: 01-August-2011

    Alternate Names:
    SORAFENIB Primary Drug Name

    Drug Info:
    Year of Approval 2005
    Drug Class antineoplastic agents, protein kinase inhibitors

    Publications:

  • TdgClinicalTrial: SORAFENIB

    • Version: January-2014

    Alternate Names:

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

    Publications:

  • DTC: SORAFENIB

    • Version: 02-September-2020

    Alternate Names:
    CHEMBL1336 ChEMBL Drug ID

    Drug Info:

    Publications:
    Chen KF et al., 2012, Blockade of STAT3 activation by sorafenib derivatives through enhancing SHP-1 phosphatase activity., Eur J Med Chem
    Machado VA et al., 2015, Synthesis, antiangiogenesis evaluation and molecular docking studies of 1-aryl-3-[(thieno[3,2-b]pyridin-7-ylthio)phenyl]ureas: Discovery of a new substitution pattern for type II VEGFR-2 Tyr kinase inhibitors., Bioorg Med Chem
    Li GB et al., 2015, LEADOPT: an automatic tool for structure-based lead optimization, and its application in structural optimizations of VEGFR2 and SYK inhibitors., Eur J Med Chem

  • JAX-CKB: Sorafenib

    • Version: 27-September-2017

    Alternate Names:

    Drug Info:

    Publications:
    Antonescu et al., 2009, KDR activating mutations in human angiosarcomas are sensitive to specific kinase inhibitors., Cancer Res.
    Pan et al., 2015, Development and Characterization of Bladder Cancer Patient-Derived Xenografts for Molecularly Guided Targeted Therapy., PLoS ONE
    Whittaker et al., 2010, Gatekeeper mutations mediate resistance to BRAF-targeted therapies., Sci Transl Med

  • DoCM: SORAFENIB

    • Version: 27-September-2017

    Alternate Names:

    Drug Info:

    Publications:
    Schirosi et al., 2012, Activating c-KIT mutations in a subset of thymic carcinoma and response to different c-KIT inhibitors., Ann. Oncol.
    Guo et al., 2007, Sorafenib inhibits the imatinib-resistant KITT670I gatekeeper mutation in gastrointestinal stromal tumor., Clin. Cancer Res.
    Bisagni et al., 2009, Long lasting response to the multikinase inhibitor bay 43-9006 (Sorafenib) in a heavily pretreated metastatic thymic carcinoma., J Thorac Oncol

  • PharmGKB: sorafenib

    • Version: 18-August-2020

    Alternate Names:

    Drug Info:

    Publications:
    Imielinski et al., 2014, Oncogenic and sorafenib-sensitive ARAF mutations in lung adenocarcinoma., J. Clin. Invest.
    Maitland ML et al., 2010, Vascular endothelial growth factor pathway., Pharmacogenet Genomics
    Gong L et al., 2017, PharmGKB summary: sorafenib pathways., Pharmacogenet Genomics

  • CIViC: SORAFENIB

    • Version: 14-September-2020

    Alternate Names:

    Drug Info:

    Publications:
    Di Nicolantonio et al., 2008, Wild-type BRAF is required for response to panitumumab or cetuximab in metastatic colorectal cancer., J. Clin. Oncol.
    Smalley et al., 2009, CRAF inhibition induces apoptosis in melanoma cells with non-V600E BRAF mutations., Oncogene
    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

  • TTD: Sorafenib

    • Version: 2020.06.01

    Alternate Names:
    D0W5HK TTD Drug ID

    Drug Info:

    Publications:

  • TALC: SORAFENIB

    • Version: 12-May-2016

    Alternate Names:
    SORAFENIB Primary Drug Name
    SORAFENIB Drug Generic Name
    NEXAVAR Drug Trade Name

    Drug Info:

    Publications:

  • OncoKB: Sorafenib

    • Version: 23-July-2020

    Alternate Names:

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL1336

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

  • MyCancerGenomeClinicalTrial: SORAFENIB

    • Version: 30-February-2014

    Alternate Names:

    Drug Info:

    Publications:

  • ClearityFoundationClinicalTrial: SORAFENIB

    • Version: 15-June-2013

    Alternate Names:

    Drug Info:

    Publications:

  • COSMIC: Sorafenib

    • 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.

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