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IMATINIB Drug Record

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  • IMATINIB chembl:CHEMBL941 ApprovedAntineoplasticImmunotherapy

    Alternate Names:

    STI-571
    IMATINIB
    GLEEVEC
    CGP 57148
    STI 571
    ALPHA-(4-METHYL-1-PIPERAZINYL)-3'-{[4-(3-PYRIDYL)-2-PYRIMIDINYL]AMINO}-P-TOLUIDIDE
    QTI571
    STI571
    4-(4-METHYL-PIPERAZIN-1-YLMETHYL)-N-[4-METHYL-3-(4-PYRIDIN-3-YL-PYRIMIDIN-2-YLAMINO)-PHENYL]-BENZAMIDE
    chembl:CHEMBL941
    chemidplus:152459-95-5
    drugbank:00619
    pubchem.compound:5291
    rxcui:282388

    Drug Info:

    Drug Class Small Molecule
    Drug Indications antineoplastic agent
    FDA Approval approved
    Drug Class antineoplastic agents, protein kinase inhibitors
    Year of Approval 2001
    Drug Class Kinase Inhibitor
    FDA Approval GI stromal tumor (KIT+), Dermatofibrosarcoma protuberans, Multiple hematologic malignancies including Philadelphia chromosome-positive ALL and CML
    Drug Class Kinase Inhibitors
    (13 More Sources)

    Publications:

    MacConaill et al., 2014, Prospective enterprise-level molecular genotyping of a cohort of cancer patients., J Mol Diagn
    Heinrich et al., 2003, Kinase mutations and imatinib response in patients with metastatic gastrointestinal stromal tumor., J. Clin. Oncol.
    Heinrich et al., 2006, Molecular correlates of imatinib resistance in gastrointestinal stromal tumors., J. Clin. Oncol.
    Heinrich et al., 2012, Crenolanib inhibits the drug-resistant PDGFRA D842V mutation associated with imatinib-resistant gastrointestinal stromal tumors., Clin. Cancer Res.
    Dewaele et al., 2008, Activity of dasatinib, a dual SRC/ABL kinase inhibitor, and IPI-504, a heat shock protein 90 inhibitor, against gastrointestinal stromal tumor-associated PDGFRAD842V mutation., Clin. Cancer Res.
    Corless et al., 2005, PDGFRA mutations in gastrointestinal stromal tumors: frequency, spectrum and in vitro sensitivity to imatinib., J. Clin. Oncol.
    Yoo et al., 2016, Efficacy of Imatinib in Patients with Platelet-Derived Growth Factor Receptor Alpha-Mutated Gastrointestinal Stromal Tumors., Cancer Res Treat
    Lasota et al., 2004, A great majority of GISTs with PDGFRA mutations represent gastric tumors of low or no malignant potential., Lab. Invest.
    Debiec-Rychter et al., 2005, Mechanisms of resistance to imatinib mesylate in gastrointestinal stromal tumors and activity of the PKC412 inhibitor against imatinib-resistant mutants., Gastroenterology
    Hirota et al., 2003, Gain-of-function mutations of platelet-derived growth factor receptor alpha gene in gastrointestinal stromal tumors., Gastroenterology
    Cassier et al., 2012, Outcome of patients with platelet-derived growth factor receptor alpha-mutated gastrointestinal stromal tumors in the tyrosine kinase inhibitor era., Clin. Cancer Res.
    Prenen et al., 2006, Efficacy of the kinase inhibitor SU11248 against gastrointestinal stromal tumor mutants refractory to imatinib mesylate., Clin. Cancer Res.
    Dai et al., 2013, Large-scale analysis of PDGFRA mutations in melanomas and evaluation of their sensitivity to tyrosine kinase inhibitors imatinib and crenolanib., Clin. Cancer Res.
    Yi et al., 2005, Epithelioid gastrointestinal stromal tumor with PDGFRA activating mutation and immunoreactivity., Appl. Immunohistochem. Mol. Morphol.
    Borbényi, 2005, [Disorders with eosinophilia, treatment of hypereosinophilic syndrome]., Orv Hetil
    Tefferi, 2005, Modern diagnosis and treatment of primary eosinophilia., Acta Haematol.
    Chen et al., 2005, Imatinib resistance in gastrointestinal stromal tumors., Curr Oncol Rep
    Trempat et al., 2003, Chronic myeloproliferative disorders with rearrangement of the platelet-derived growth factor alpha receptor: a new clinical target for STI571/Glivec., Oncogene
    Chalmers et al., 2015, Comprehensive genomic profiling identifies a novel TNKS2-PDGFRA fusion that defines a myeloid neoplasm with eosinophilia that responded dramatically to imatinib therapy., Blood Cancer J
    Metzgeroth G et al., 2012, Limited clinical activity of nilotinib and sorafenib in FIP1L1-PDGFRA positive chronic eosinophilic leukemia with imatinib-resistant T674I mutation., Leukemia
    Srinivas et al., 2014, Complete response of monoblastic myeloid sarcoma with FIP1L1- PDGFRA rearrangement to imatinib monotherapy., Br. J. Haematol.
    Cools et al., 2003, A tyrosine kinase created by fusion of the PDGFRA and FIP1L1 genes as a therapeutic target of imatinib in idiopathic hypereosinophilic syndrome., N. Engl. J. Med.
    Klion et al., 2004, Molecular remission and reversal of myelofibrosis in response to imatinib mesylate treatment in patients with the myeloproliferative variant of hypereosinophilic syndrome., Blood
    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)
    Hammerman et al., 2011, Mutations in the DDR2 kinase gene identify a novel therapeutic target in squamous cell lung cancer., Cancer Discov
    Holtkamp et al., 2006, Mutation and expression of PDGFRA and KIT in malignant peripheral nerve sheath tumors, and its implications for imatinib sensitivity., Carcinogenesis
    Szerlip et al., 2012, Intratumoral heterogeneity of receptor tyrosine kinases EGFR and PDGFRA amplification in glioblastoma defines subpopulations with distinct growth factor response., Proc. Natl. Acad. Sci. U.S.A.
    Elling et al., 2011, Novel imatinib-sensitive PDGFRA-activating point mutations in hypereosinophilic syndrome induce growth factor independence and leukemia-like disease., Blood
    Ramos AH et al., 2009, Amplification of chromosomal segment 4q12 in non-small cell lung cancer., Cancer Biol Ther
    de Groot et al., 2006, Cellular effects of imatinib on medullary thyroid cancer cells harboring multiple endocrine neoplasia Type 2A and 2B associated RET mutations., Surgery
    David et al., 2007, Durable responses to imatinib in patients with PDGFRB fusion gene-positive and BCR-ABL-negative chronic myeloproliferative disorders., Blood
    Sakurai Y et al., 2020, B-Cell Precursor-Acute Lymphoblastic Leukemia With EBF1-PDGFRB Fusion Treated With Hematopoietic Stem Cell Transplantation and Imatinib: A Case Report and Literature Review., J Pediatr Hematol Oncol
    Lengline E et al., 2013, Successful tyrosine kinase inhibitor therapy in a refractory B-cell precursor acute lymphoblastic leukemia with EBF1-PDGFRB fusion., Haematologica
    Weston et al., 2013, Tyrosine kinase inhibitor therapy induces remission in a patient with refractory EBF1-PDGFRB-positive acute lymphoblastic leukemia., J. Clin. Oncol.
    Jones et al., 2005, The development and application of imatinib., Expert Opin Drug Saf
    Modi et al., 2005, A phase II trial of imatinib mesylate monotherapy in patients with metastatic breast cancer., Breast Cancer Res. Treat.
    Johnson et al., 2005, Induction of heparin-binding EGF-like growth factor and activation of EGF receptor in imatinib mesylate-treated squamous carcinoma cells., J. Cell. Physiol.
    Basciani et al., 2005, Imatinib mesylate inhibits Leydig cell tumor growth: evidence for in vitro and in vivo activity., Cancer Res.
    Chen et al., 2006, The tyrosine kinase inhibitor imatinib fails to inhibit pancreatic cancer progression., Cancer Lett.
    Ishibashi T et al., 2016, Ph-like ALL-related novel fusion kinase ATF7IP-PDGFRB exhibits high sensitivity to tyrosine kinase inhibitors in murine cells., Exp Hematol
    Delbaldo, [Pharmacokinetic-pharmacodynamics relationships of imatinib (Glivec)]., Therapie
    de Groot et al., 2007, A phase II trial of imatinib therapy for metastatic medullary thyroid carcinoma., J. Clin. Endocrinol. Metab.
    Catani et al., [New orientations in the management of advanced, metastatic gastrointestinal stromal tumors (GIST): combination of surgery and systemic therapy with imatinib in a case of primary gastric location]., Chir Ital
    Kovács et al., 2005, [Gastrointestinal stromal tumors (GISTs): clinical and pathological features]., Orv Hetil
    Tuveson DA et al., 2001, STI571 inactivation of the gastrointestinal stromal tumor c-KIT oncoprotein: biological and clinical implications., Oncogene
    Joensuu et al., 2017, Effect of KIT and PDGFRA Mutations on Survival in Patients With Gastrointestinal Stromal Tumors Treated With Adjuvant Imatinib: An Exploratory Analysis of a Randomized Clinical Trial., JAMA Oncol
    Jachetti et al., 2017, Imatinib Spares cKit-Expressing Prostate Neuroendocrine Tumors, whereas Kills Seminal Vesicle Epithelial-Stromal Tumors by Targeting PDGFR-β., Mol. Cancer Ther.
    Dagher et al., 2002, Approval summary: imatinib mesylate in the treatment of metastatic and/or unresectable malignant gastrointestinal stromal tumors., Clin. Cancer Res.
    Einhorn et al., 2006, Phase II study of imatinib mesylate in chemotherapy refractory germ cell tumors expressing KIT., Am. J. Clin. Oncol.
    Foster et al., 2008, Association of paediatric mastocytosis with a polymorphism resulting in an amino acid substitution (M541L) in the transmembrane domain of c-KIT., Br. J. Dermatol.
    Iurlo et al., 2014, Identification of kit(M541L) somatic mutation in chronic eosinophilic leukemia, not otherwise specified and its implication in low-dose imatinib response., Oncotarget
    Tamborini et al., 2006, Functional analyses and molecular modeling of two c-Kit mutations responsible for imatinib secondary resistance in GIST patients., Oncogene
    Pectasides et al., Complete response after imatinib mesylate administration in a patient with chemoresistant stage IV seminoma., Anticancer Res.
    Ströbel et al., 2004, Thymic carcinoma with overexpression of mutated KIT and the response to imatinib., N. Engl. J. Med.
    Growney et al., 2005, Activation mutations of human c-KIT resistant to imatinib mesylate are sensitive to the tyrosine kinase inhibitor PKC412., Blood
    Frost et al., 2002, Juxtamembrane mutant V560GKit is more sensitive to Imatinib (STI571) compared with wild-type c-kit whereas the kinase domain mutant D816VKit is resistant., Mol. Cancer Ther.
    Terheyden et al., 2010, Response to imatinib mesylate depends on the presence of the V559A-mutated KIT oncogene., J. Invest. Dermatol.
    Wasag et al., 2011, Novel, activating KIT-N822I mutation in familial cutaneous mastocytosis., Exp. Hematol.
    Buti et al., 2011, Impressive response with imatinib in a heavily pretreated patient with metastatic c-KIT mutated thymic carcinoma., J. Clin. Oncol.
    Spitaleri et al., 2015, Inactivity of imatinib in gastrointestinal stromal tumors (GISTs) harboring a KIT activation-loop domain mutation (exon 17 mutation pN822K)., Onco Targets Ther
    Conca et al., 2013, Are two better than one? A novel double-mutant KIT in GIST that responds to Imatinib., Mol Oncol
    Tamborini et al., 2004, A new mutation in the KIT ATP pocket causes acquired resistance to imatinib in a gastrointestinal stromal tumor patient., Gastroenterology
    Hagemann et al., 2014, Stabilization of disease after targeted therapy in a thymic carcinoma with KIT mutation detected by clinical next-generation sequencing., J Thorac Oncol
    Heinrich et al., 2017, Correlation of Long-term Results of Imatinib in Advanced Gastrointestinal Stromal Tumors With Next-Generation Sequencing Results: Analysis of Phase 3 SWOG Intergroup Trial S0033., JAMA Oncol
    Patrikidou et al., 2016, Long-term outcome of molecular subgroups of GIST patients treated with standard-dose imatinib in the BFR14 trial of the French Sarcoma Group., Eur. J. Cancer
    Zeng S et al., 2017 Sep, Wnt/β-catenin Signaling Contributes to Tumor Malignancy and Is Targetable in Gastrointestinal Stromal Tumor., Mol Cancer Ther
    Handolias et al., 2010, Clinical responses observed with imatinib or sorafenib in melanoma patients expressing mutations in KIT., Br. J. Cancer
    Goemans et al., 2005, Mutations in KIT and RAS are frequent events in pediatric core-binding factor acute myeloid leukemia., Leukemia
    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.
    Carlino et al., 2014, Resistance to c-Kit inhibitors in melanoma: insights for future therapies., Oncoscience
    Todd et al., 2013, Secondary c-Kit mutations confer acquired resistance to RTK inhibitors in c-Kit mutant melanoma cells., Pigment Cell Melanoma Res
    Zook et al., 2017, Combination of Imatinib Mesylate and AKT Inhibitor Provides Synergistic Effects in Preclinical Study of Gastrointestinal Stromal Tumor., Clin. Cancer Res.
    Gebreyohannes et al., 2016, Cabozantinib Is Active against Human Gastrointestinal Stromal Tumor Xenografts Carrying Different KIT Mutations., Mol. Cancer Ther.
    Garner et al., 2014, Ponatinib inhibits polyclonal drug-resistant KIT oncoproteins and shows therapeutic potential in heavily pretreated gastrointestinal stromal tumor (GIST) patients., Clin. Cancer Res.
    Rapisuwon et al., 2014, Novel somatic KIT exon 8 mutation with dramatic response to imatinib in a patient with mucosal melanoma: a case report., Melanoma Res.
    Girard et al., 2009, Comprehensive genomic analysis reveals clinically relevant molecular distinctions between thymic carcinomas and thymomas., Clin. Cancer Res.
    Li et al., 2015, FGFR-Mediated Reactivation of MAPK Signaling Attenuates Antitumor Effects of Imatinib in Gastrointestinal Stromal Tumors., Cancer Discov
    Nakagomi et al., 2007, Juxtamembrane-type c-kit gene mutation found in aggressive systemic mastocytosis induces imatinib-resistant constitutive KIT activation., Lab. Invest.
    Debiec-Rychter et al., 2006, KIT mutations and dose selection for imatinib in patients with advanced gastrointestinal stromal tumours., Eur. J. Cancer
    Heinrich et al., 2008, Correlation of kinase genotype and clinical outcome in the North American Intergroup Phase III Trial of imatinib mesylate for treatment of advanced gastrointestinal stromal tumor: CALGB 150105 Study by Cancer and Leukemia Group B and Southwest Oncology Group., J. Clin. Oncol.
    Heinrich et al., 2008, Primary and secondary kinase genotypes correlate with the biological and clinical activity of sunitinib in imatinib-resistant gastrointestinal stromal tumor., J. Clin. Oncol.
    Minor et al., 2012, Sunitinib therapy for melanoma patients with KIT mutations., Clin. Cancer Res.
    Guo et al., 2011, Phase II, open-label, single-arm trial of imatinib mesylate in patients with metastatic melanoma harboring c-Kit mutation or amplification., J. Clin. Oncol.
    Carvajal et al., 2011, KIT as a therapeutic target in metastatic melanoma., JAMA
    Hodi et al., 2008, Major response to imatinib mesylate in KIT-mutated melanoma., J. Clin. Oncol.
    Dy et al., 2005, A phase II trial of imatinib (ST1571) in patients with c-kit expressing relapsed small-cell lung cancer: a CALGB and NCCTG study., Ann. Oncol.
    Rutkowski et al., 2007, Predictive factors for long-term effects of imatinib therapy in patients with inoperable/metastatic CD117(+) gastrointestinal stromal tumors (GISTs)., J. Cancer Res. Clin. Oncol.
    Posadas et al., 2007, A prospective analysis of imatinib-induced c-KIT modulation in ovarian cancer: a phase II clinical study with proteomic profiling., Cancer
    Lee et al., 2006, Response to imatinib in KIT- and PDGFRA-wild type gastrointestinal stromal associated with neurofibromatosis type 1., Dig. Dis. Sci.
    De Giorgi, 2007, KIT mutations and imatinib dose effects in patients with gastrointestinal stromal tumors., J. Clin. Oncol.
    Cameron et al., 2011, Ten Years of Treatment with 400 mg Imatinib per Day in a Case of Advanced Gastrointestinal Stromal Tumor., Case Rep Oncol
    Antonescu et al., 2007, L576P KIT mutation in anal melanomas correlates with KIT protein expression and is sensitive to specific kinase inhibition., Int. J. Cancer
    Woodman et al., 2009, Activity of dasatinib against L576P KIT mutant melanoma: molecular, cellular, and clinical correlates., Mol. Cancer Ther.
    Hodi et al., 2013, Imatinib for melanomas harboring mutationally activated or amplified KIT arising on mucosal, acral, and chronically sun-damaged skin., J. Clin. Oncol.
    McDonnell et al., 2011, V559A and N822I double KIT mutant melanoma with predictable response to imatinib?, Pigment Cell Melanoma Res
    Handolias et al., 2010, Mutations in KIT occur at low frequency in melanomas arising from anatomical sites associated with chronic and intermittent sun exposure., Pigment Cell Melanoma Res
    Cairoli et al., 2006, Prognostic impact of c-KIT mutations in core binding factor leukemias: an Italian retrospective study., Blood
    Gleixner et al., 2007, Synergistic growth-inhibitory effects of two tyrosine kinase inhibitors, dasatinib and PKC412, on neoplastic mast cells expressing the D816V-mutated oncogenic variant of KIT., Haematologica
    Pan et al., 2007, EXEL-0862, a novel tyrosine kinase inhibitor, induces apoptosis in vitro and ex vivo in human mast cells expressing the KIT D816V mutation., Blood
    Gotlib et al., 2005, Activity of the tyrosine kinase inhibitor PKC412 in a patient with mast cell leukemia with the D816V KIT mutation., 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
    Ustun et al., 2009, Chemotherapy and dasatinib induce long-term hematologic and molecular remission in systemic mastocytosis with acute myeloid leukemia with KIT D816V., Leuk. Res.
    Gajiwala et al., 2009, KIT kinase mutants show unique mechanisms of drug resistance to imatinib and sunitinib in gastrointestinal stromal tumor patients., Proc. Natl. Acad. Sci. U.S.A.
    Smith et al., 2012, Validation of ITD mutations in FLT3 as a therapeutic target in human acute myeloid leukaemia., Nature
    Johnson et al., 2013, Hidden mastocytosis in acute myeloid leukemia with t(8;21)(q22;q22)., Am. J. Clin. Pathol.
    Serrano et al., 2015, KRAS and KIT Gatekeeper Mutations Confer Polyclonal Primary Imatinib Resistance in GI Stromal Tumors: Relevance of Concomitant Phosphatidylinositol 3-Kinase/AKT Dysregulation., J. Clin. Oncol.
    Hong et al., 2012, [Secondary mutation of c-kit/PDGFRα genotypes after imatinib mesylate therapy and its relationship with efficacy of sunitinib]., Zhonghua Bing Li Xue Za Zhi
    Roberts et al., 2007, Resistance to c-KIT kinase inhibitors conferred by V654A mutation., Mol. Cancer Ther.
    Tutone et al., 2011, Study of the role of "gatekeeper" mutations V654A and T670I of c-kit kinase in the interaction with inhibitors by means mixed molecular dynamics/docking approach., Bioinformation
    Antonescu et al., 2005, Acquired resistance to imatinib in gastrointestinal stromal tumor occurs through secondary gene mutation., Clin. Cancer Res.
    Hirota et al., 1998, Gain-of-function mutations of c-kit in human gastrointestinal stromal tumors., Science
    Curtin et al., 2006, Somatic activation of KIT in distinct subtypes of melanoma., J. Clin. Oncol.
    Tornillo et al., 2006, An update on molecular genetics of gastrointestinal stromal tumours., J. Clin. Pathol.
    Hirota et al., 2001, Gain-of-function mutation at the extracellular domain of KIT in gastrointestinal stromal tumours., J. Pathol.
    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
    Carter et al., 2005, Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinases., Proc. Natl. Acad. Sci. U.S.A.
    Beadling et al., 2008, KIT gene mutations and copy number in melanoma subtypes., Clin. Cancer Res.
    Kitayama et al., 1995, Constitutively activating mutations of c-kit receptor tyrosine kinase confer factor-independent growth and tumorigenicity of factor-dependent hematopoietic cell lines., Blood
    Tefferi, 2009, Molecular drug targets in myeloproliferative neoplasms: mutant ABL1, JAK2, MPL, KIT, PDGFRA, PDGFRB and FGFR1., J. Cell. Mol. Med.
    Rossi et al., 2013, When a thymic carcinoma "becomes" a GIST., Lung Cancer
    Schirosi et al., 2012, Activating c-KIT mutations in a subset of thymic carcinoma and response to different c-KIT inhibitors., Ann. Oncol.
    Shah et al., 2006, Dasatinib (BMS-354825) inhibits KITD816V, an imatinib-resistant activating mutation that triggers neoplastic growth in most patients with systemic mastocytosis., Blood
    Hartmann et al., 2005, Novel germline mutation of KIT associated with familial gastrointestinal stromal tumors and mastocytosis., Gastroenterology
    Guo et al., 2007, Sorafenib inhibits the imatinib-resistant KITT670I gatekeeper mutation in gastrointestinal stromal tumor., Clin. Cancer Res.
    Emile et al., 2012, Frequencies of KIT and PDGFRA mutations in the MolecGIST prospective population-based study differ from those of advanced GISTs., Med. Oncol.
    Agirre et al., 2005, Coexistence of different clonal populations harboring the b3a2 (p210) and e1a2 (p190) BCR-ABL1 fusion transcripts in chronic myelogenous leukemia resistant to imatinib., Cancer Genet. Cytogenet.
    Haberler et al., 2006, Immunohistochemical analysis of platelet-derived growth factor receptor-alpha, -beta, c-kit, c-abl, and arg proteins in glioblastoma: possible implications for patient selection for imatinib mesylate therapy., J. Neurooncol.
    Brueggemeier et al., Protein-acrylamide copolymer hydrogels for array-based detection of tyrosine kinase activity from cell lysates., Biomacromolecules
    Dewar et al., 2005, Inhibition of c-fms by imatinib: expanding the spectrum of treatment., Cell Cycle
    Hoerth et al., 2004, Involvment of c-Abl in the radiation-induced inhibition of myoblast differentiation., Int. J. Radiat. Biol.
    Mojzych M et al., 2014, Synthesis and kinase inhibitory activity of new sulfonamide derivatives of pyrazolo[4,3-e][1,2,4]triazines., Eur J Med Chem
    Page BD et al., 2012, Small molecule STAT5-SH2 domain inhibitors exhibit potent antileukemia activity., J Med Chem
    Perwein T et al., 2016, Imatinib-induced long-term remission in a relapsed RCSD1-ABL1-positive acute lymphoblastic leukemia., Haematologica
    Roberts et al., 2014, Targetable kinase-activating lesions in Ph-like acute lymphoblastic leukemia., N. Engl. J. Med.
    Tomita O et al., 2014, Sensitivity of SNX2-ABL1 toward tyrosine kinase inhibitors distinct from that of BCR-ABL1., Leuk Res
    Testoni et al., 2016, Somatically mutated ABL1 is an actionable and essential NSCLC survival gene., EMBO Mol Med
    Khoury HJ et al., 2012, Bosutinib is active in chronic phase chronic myeloid leukemia after imatinib and dasatinib and/or nilotinib therapy failure., Blood
    O'Hare et al., 2005, In vitro activity of Bcr-Abl inhibitors AMN107 and BMS-354825 against clinically relevant imatinib-resistant Abl kinase domain mutants., Cancer Res.
    Pemovska T et al., 2015, Axitinib effectively inhibits BCR-ABL1(T315I) with a distinct binding conformation., Nature
    Branford et al., 2003, Detection of BCR-ABL mutations in patients with CML treated with imatinib is virtually always accompanied by clinical resistance, and mutations in the ATP phosphate-binding loop (P-loop) are associated with a poor prognosis., Blood
    Redaelli et al., 2009, Activity of bosutinib, dasatinib, and nilotinib against 18 imatinib-resistant BCR/ABL mutants., J. Clin. Oncol.
    Yamamoto et al., 2004, The two major imatinib resistance mutations E255K and T315I enhance the activity of BCR/ABL fusion kinase., Biochem. Biophys. Res. Commun.
    An et al., 2010, BCR-ABL tyrosine kinase inhibitors in the treatment of Philadelphia chromosome positive chronic myeloid leukemia: a review., Leuk. Res.
    Nimmanapalli et al., 2002, Novel targeted therapies for Bcr-Abl positive acute leukemias: beyond STI571., Oncogene
    Ivan et al., 2006, Analysis of protein tyrosine kinases expression in the melanoma metastases of patients treated with Imatinib Mesylate (STI571, Gleevec)., J. Cutan. Pathol.
    Deguchi Y et al., 2008, Comparison of imatinib, dasatinib, nilotinib and INNO-406 in imatinib-resistant cell lines., Leuk Res
    Talpaz M et al., 2006, Dasatinib in imatinib-resistant Philadelphia chromosome-positive leukemias., N Engl J Med
    Ravegnini G et al., 2019, An exploratory study by DMET array identifies a germline signature associated with imatinib response in gastrointestinal stromal tumor., Pharmacogenomics J
    Chase et al., 2009, Imatinib sensitivity as a consequence of a CSF1R-Y571D mutation and CSF1/CSF1R signaling abnormalities in the cell line GDM1., Leukemia
    Lilljebjörn et al., 2014, RNA-seq identifies clinically relevant fusion genes in leukemia including a novel MEF2D/CSF1R fusion responsive to imatinib., Leukemia
    El Hajj Dib et al., 2006, Imatinib mesylate (Gleevec) enhances mature osteoclast apoptosis and suppresses osteoclast bone resorbing activity., Eur. J. Pharmacol.
    Ando et al., 2006, Imatinib mesylate inhibits osteoclastogenesis and joint destruction in rats with collagen-induced arthritis (CIA)., J. Bone Miner. Metab.
    Dewar et al., 2006, Imatinib as a potential antiresorptive therapy for bone disease., Blood
    Taylor et al., 2006, FMS receptor for M-CSF (CSF-1) is sensitive to the kinase inhibitor imatinib and mutation of Asp-802 to Val confers resistance., Oncogene
    Croom et al., 2003, Imatinib mesylate: in the treatment of gastrointestinal stromal tumours., Drugs
    Waller, 2010, Imatinib mesylate., Recent Results Cancer Res.
    Nadal et al., 2004, Imatinib mesylate (Gleevec/Glivec) a molecular-targeted therapy for chronic myeloid leukaemia and other malignancies., Int. J. Clin. Pract.
    Reddy EP et al., 2012, The ins and outs of bcr-abl inhibition., Genes Cancer
    Davies A et al., 2014, Dual glutathione-S-transferase-θ1 and -μ1 gene deletions determine imatinib failure in chronic myeloid leukemia., Clin Pharmacol Ther
    Verboom MC et al., 2019, Genetic polymorphisms in ABCG2 and CYP1A2 are associated with imatinib dose reduction in patients treated for gastrointestinal stromal tumors., Pharmacogenomics J
    Cargnin S et al., 2018, Impact of SLC22A1 and CYP3A5 genotypes on imatinib response in chronic myeloid leukemia: A systematic review and meta-analysis., Pharmacol Res
    Qiu HB et al., 2018, Imatinib-induced ophthalmological side-effects in GIST patients are associated with the variations of EGFR, SLC22A1, SLC22A5 and ABCB1., Pharmacogenomics J
    Di Paolo A et al., 2014, The c.480C>G polymorphism of hOCT1 influences imatinib clearance in patients affected by chronic myeloid leukemia., Pharmacogenomics J
    Clark RE et al., 2008, Pharmacologic markers and predictors of responses to imatinib therapy in patients with chronic myeloid leukemia., Leuk Lymphoma
    Giannoudis A et al., 2013, The hOCT1 SNPs M420del and M408V alter imatinib uptake and M420del modifies clinical outcome in imatinib-treated chronic myeloid leukemia., Blood
    Kim DH et al., 2009, Clinical relevance of a pharmacogenetic approach using multiple candidate genes to predict response and resistance to imatinib therapy in chronic myeloid leukemia., Clin Cancer Res
    Breedveld et al., 2005, The effect of Bcrp1 (Abcg2) on the in vivo pharmacokinetics and brain penetration of imatinib mesylate (Gleevec): implications for the use of breast cancer resistance protein and P-glycoprotein inhibitors to enable the brain penetration of imatinib in patients., Cancer Res.
    Skoglund K et al., 2014, Single-nucleotide polymorphisms of ABCG2 increase the efficacy of tyrosine kinase inhibitors in the K562 chronic myeloid leukemia cell line., Pharmacogenet Genomics
    Delord M et al., 2013, High imatinib dose overcomes insufficient response associated with ABCG2 haplotype in chronic myelogenous leukemia patients., Oncotarget
    Petain A et al., 2008, Population pharmacokinetics and pharmacogenetics of imatinib in children and adults., Clin Cancer Res
    Ozvegy-Laczka et al., 2004, High-affinity interaction of tyrosine kinase inhibitors with the ABCG2 multidrug transporter., Mol. Pharmacol.
    Kindler et al., 2005, Identification of a novel activating mutation (Y842C) within the activation loop of FLT3 in patients with acute myeloid leukemia (AML)., Blood
    Corradi V et al., 2011, Computational techniques are valuable tools for the discovery of protein-protein interaction inhibitors: the 14-3-3σ case., Bioorg Med Chem Lett
    Porosnicu et al., 2001, Co-treatment with As2O3 enhances selective cytotoxic effects of STI-571 against Brc-Abl-positive acute leukemia cells., Leukemia
    Nimmanapalli et al., 2001, Cotreatment with STI-571 enhances tumor necrosis factor alpha-related apoptosis-inducing ligand (TRAIL or apo-2L)-induced apoptosis of Bcr-Abl-positive human acute leukemia cells., Clin. Cancer Res.
    Augis V et al., 2013, A single nucleotide polymorphism in cBIM is associated with a slower achievement of major molecular response in chronic myeloid leukaemia treated with imatinib., PLoS One
    Ng et al., 2012, A common BIM deletion polymorphism mediates intrinsic resistance and inferior responses to tyrosine kinase inhibitors in cancer., Nat. Med.
    Ehmann F et al., 2014, European Medicines Agency initiatives and perspectives on pharmacogenomics., Br J Clin Pharmacol
    van Erp et al., 2007, Influence of CYP3A4 inhibition on the steady-state pharmacokinetics of imatinib., Clin. Cancer Res.
    Dressman MA et al., 2004, Correlation of major cytogenetic response with a pharmacogenetic marker in chronic myeloid leukemia patients treated with imatinib (STI571)., Clin Cancer Res
    Angelini S et al., 2013, Polymorphisms in OCTN1 and OCTN2 transporters genes are associated with prolonged time to progression in unresectable gastrointestinal stromal tumours treated with imatinib therapy., Pharmacol Res
    Angelini S et al., 2013, Association between imatinib transporters and metabolizing enzymes genotype and response in newly diagnosed chronic myeloid leukemia patients receiving imatinib therapy., Haematologica
    Gunby et al., 2006, Structural insights into the ATP binding pocket of the anaplastic lymphoma kinase by site-directed mutagenesis, inhibitor binding analysis, and homology modeling., J. Med. Chem.
    Kasper et al., 2016, Correlation of CTNNB1 Mutation Status with Progression Arrest Rate in RECIST Progressive Desmoid-Type Fibromatosis Treated with Imatinib: Translational Research Results from a Phase 2 Study of the German Interdisciplinary Sarcoma Group (GISG-01)., Ann. Surg. Oncol.
    Kawano et al., Depsipeptide enhances imatinib mesylate-induced apoptosis of Bcr-Abl-positive cells and ectopic expression of cyclin D1, c-Myc or active MEK abrogates this effect., Anticancer Res.
    Jubert et al., 2006, [Targeted therapies in pediatric oncology: a new therapeutic approach?]., Arch Pediatr
    Xu et al., 2005, Blocking platelet-derived growth factor-D/platelet-derived growth factor receptor beta signaling inhibits human renal cell carcinoma progression in an orthotopic mouse model., Cancer Res.
    Benjamin et al., 2006, Management of gastrointestinal stromal tumors in the imatinib era: selected case studies., Oncologist
    Neef et al., 2006, Oral imatinib treatment reduces early fibrogenesis but does not prevent progression in the long term., J. Hepatol.
    Dicker et al., 2006, CD154 induces p73 to overcome the resistance to apoptosis of chronic lymphocytic leukemia cells lacking functional p53., Blood
    Yamakawa Y et al., 2011, Pharmacokinetic impact of SLCO1A2 polymorphisms on imatinib disposition in patients with chronic myeloid leukemia., Clin Pharmacol Ther
    Michaelis S et al., 2012, Dabigatran and dabigatran ethyl ester: potent inhibitors of ribosyldihydronicotinamide dehydrogenase (NQO2)., J Med Chem
    Curtis et al., 2007, Two novel imatinib-responsive PDGFRA fusion genes in chronic eosinophilic leukaemia., Br. J. Haematol.
    Tarn et al., 2006, Therapeutic effect of imatinib in gastrointestinal stromal tumors: AKT signaling dependent and independent mechanisms., Cancer Res.
    Kassogue Y et al., 2014, Functional polymorphism of CYP2B6 G15631T is associated with hematologic and cytogenetic response in chronic myeloid leukemia patients treated with imatinib., Med Oncol
    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
    Wang et al., 2005, AML1-ETO and C-KIT mutation/overexpression in t(8;21) leukemia: implication in stepwise leukemogenesis and response to Gleevec., Proc. Natl. Acad. Sci. U.S.A.
    Carter et al., 2006, Regulation of survivin expression through Bcr-Abl/MAPK cascade: targeting survivin overcomes imatinib resistance and increases imatinib sensitivity in imatinib-responsive CML cells., Blood
    Adeagbo BA et al., 2016, Influence of CYP3A5*3 and ABCB1 C3435T on clinical outcomes and trough plasma concentrations of imatinib in Nigerians with chronic myeloid leukaemia., J Clin Pharm Ther
    Yeoh AEJ et al., 2018, Intensifying Treatment of Childhood B-Lymphoblastic Leukemia With IKZF1 Deletion Reduces Relapse and Improves Overall Survival: Results of Malaysia-Singapore ALL 2010 Study., J Clin Oncol
  • IMATINIB   DDR1

    Interaction Score: 6.87

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

    Interaction Info:
    Trial Name imatinib mesylate, STI 571,Gleevec, Glivec
    Novel drug target Established target

    PMIDs:
    15972446 16298518 15994946 16401709 16168515


    Sources:
    TdgClinicalTrial TEND

  • IMATINIB   SLC22A4

    Interaction Score: 2.94

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    23127916 22875622


    Sources:
    PharmGKB

  • IMATINIB   FIP1L1

    Interaction Score: 2.94

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Fusion protein FIP1L1:PDGFRA

    PMIDs:
    24433361


    Sources:
    PharmGKB FDA

  • IMATINIB   RCSD1

    Interaction Score: 1.96

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    27125982


    Sources:
    CIViC

  • IMATINIB   UGT2A1

    Interaction Score: 1.96

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    30237583


    Sources:
    PharmGKB

  • IMATINIB   CHST1

    Interaction Score: 1.96

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    30237583


    Sources:
    PharmGKB

  • IMATINIB   CYP2F1

    Interaction Score: 1.96

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    30237583


    Sources:
    PharmGKB

  • IMATINIB   BCL2L11

    Interaction Score: 1.96

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    24223824 22426421


    Sources:
    CIViC PharmGKB

  • IMATINIB   SFN

    Interaction Score: 1.96

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    21962576


    Sources:
    DTC

  • IMATINIB   KIT

    Interaction Score: 1.58

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

    Interaction Info:
    Approval Status Guideline
    Indication/Tumor Type prostate neuroendocrine neoplasm
    Approval Status Phase II

    PMIDs:
    11526490 28334365 27980106 12374669 16462496 18795925 25015329 16751810 18751412 15201427 15790786 12481435 19812602 21689725 21969494 26316776 23567324 15236194 24419427 16954519 28196207 26687836 28611108 20372153 16015387 24317392 25594040 23582185 27370604 27777285 25239608 25003536 19861435 25673643 17259998 16624552 18955451 18955458 22261812 21690468 21642685 18421059 16087693 17458563 17559139 16865565 17369583 22114577 17372901 19671763 14645423 23775962 21159146 20088873 16384925 18024392 16912224 15972446 23714533 18986703 19164557 22504184 24045550 24687822 22932406 17363509 22355224 16638875 15685537 15930355 9438854 16908931 16731599 11276010 18936790 16046538 18980976 7530509 19175693 25157968 23375402 22357254 16434489 16143141 17699867 21953054


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

  • IMATINIB   SLC22A5

    Interaction Score: 1.47

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    28762371 23127916


    Sources:
    PharmGKB

  • IMATINIB   ULK3

    Interaction Score: 0.98

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15073101


    Sources:
    PharmGKB

  • IMATINIB   BCR

    Interaction Score: 0.82

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Fusion protein BCR:ABL1
    Notes Targets BCR-ABL fusion protein

    PMIDs:
    24681986 22148584 12600228 20072827 15206509 23226582


    Sources:
    TALC DTC PharmGKB FDA

  • IMATINIB   SLC22A1

    Interaction Score: 0.63

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    30713339 30237583 29427770 28762371 24589908 18398725 23223357 19584153


    Sources:
    PharmGKB

  • IMATINIB   PDGFRA

    Interaction Score: 0.6

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

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

    PMIDs:
    25157968 14645423 16954519 22745105 18794084 15928335 26130666 15146165 15685537 12949711 22718859 16638875 24132921 15894928 15921304 15995325 15946589 12944919 25658984 21818111 24456122 12660384 14504092 28514312 22328973 16357008 22323597 21224473 19755855


    Sources:
    DTC MyCancerGenome TdgClinicalTrial JAX-CKB TEND DoCM COSMIC CIViC FDA OncoKB

  • IMATINIB   ABL1

    Interaction Score: 0.5

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Fusion protein BCR:ABL1
    Trial Name imatinib mesylate, STI 571,Gleevec, Glivec
    Novel drug target Established target

    PMIDs:
    15949566 16205964 16153117 15917650 15799618 24681986 22148584 27125982 25207766 24367893 26758680 22371878 15930265 25686603 12623848 19075254 15194504 20537386 12476305 16630177 18191450 16775234


    Sources:
    DTC MyCancerGenome TdgClinicalTrial JAX-CKB NCI TEND COSMIC CIViC PharmGKB FDA OncoKB

  • IMATINIB   ABL2

    Interaction Score: 0.49

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    25207766


    Sources:
    CIViC

  • IMATINIB   SLCO1A2

    Interaction Score: 0.39

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    21633340


    Sources:
    PharmGKB

  • IMATINIB   IKZF1

    Interaction Score: 0.33

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    30044693


    Sources:
    CIViC

  • IMATINIB   ABCB4

    Interaction Score: 0.28

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    30237583


    Sources:
    PharmGKB

  • IMATINIB   CSF1R

    Interaction Score: 0.27

    Interaction Types & Directionality:
    antagonist (inhibitory)

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

    PMIDs:
    18971950 24186003 17049513 16816921 16449525 15917650 16170366


    Sources:
    DTC TdgClinicalTrial JAX-CKB TEND DoCM CIViC

  • IMATINIB   PDGFRB

    Interaction Score: 0.25

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

    Interaction Info:
    Trial Name imatinib mesylate, STI 571,Gleevec, Glivec
    Novel drug target Established target

    PMIDs:
    16960151 32068648 24186319 23835704 15794712 15803362 15887238 15753388 15893416 26703895


    Sources:
    DTC MyCancerGenome TdgClinicalTrial TEND CIViC PharmGKB FDA OncoKB

  • IMATINIB   PDGFB

    Interaction Score: 0.25

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    OncoKB

  • IMATINIB   GSTT1

    Interaction Score: 0.2

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    25188725


    Sources:
    PharmGKB

  • IMATINIB   SLC19A1

    Interaction Score: 0.18

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    30237583


    Sources:
    PharmGKB

  • IMATINIB   CD40LG

    Interaction Score: 0.18

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    16741250


    Sources:
    NCI

  • IMATINIB   SMAD4

    Interaction Score: 0.16

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Imatinib + Carboplatin + Paclitaxel
    Indication/Tumor Type melanoma
    Response Type sensitive

    PMIDs:
    28514312


    Sources:
    JAX-CKB

  • IMATINIB   ETV6

    Interaction Score: 0.16

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type chronic leukemia
    Response Type sensitive
    Approval Status Clinical Study

    PMIDs:
    17555450


    Sources:
    JAX-CKB

  • IMATINIB   XIAP

    Interaction Score: 0.15

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    11368438 11234890


    Sources:
    NCI

  • IMATINIB   NTRK1

    Interaction Score: 0.13

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Novel drug target Established target
    Trial Name imatinib mesylate, STI 571,Gleevec, Glivec

    PMIDs:
    17582306 17579194 15832750 16782438 16052979


    Sources:
    TdgClinicalTrial TEND

  • IMATINIB   NQO2

    Interaction Score: 0.13

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22494098


    Sources:
    DTC

  • IMATINIB   ABCG2

    Interaction Score: 0.13

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15805252 30713339 24322003 24123600 18981009 15155841


    Sources:
    NCI PharmGKB

  • IMATINIB   CTNNB1

    Interaction Score: 0.12

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    26861905


    Sources:
    JAX-CKB

  • IMATINIB   CDKN2A

    Interaction Score: 0.09

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    28514312


    Sources:
    JAX-CKB

  • IMATINIB   NQO1

    Interaction Score: 0.09

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    30237583


    Sources:
    PharmGKB

  • IMATINIB   LYN

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    18191450


    Sources:
    DTC CIViC

  • IMATINIB   ABCC4

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    23127916


    Sources:
    PharmGKB

  • IMATINIB   RUNX1

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15650049


    Sources:
    NCI

  • IMATINIB   BIRC5

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    16254145


    Sources:
    NCI

  • IMATINIB   IRAK1

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • IMATINIB   MYC

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15517875


    Sources:
    NCI

  • IMATINIB   RET

    Interaction Score: 0.05

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name imatinib mesylate, STI 571,Gleevec, Glivec
    Novel drug target Established target

    PMIDs:
    16782438


    Sources:
    TdgClinicalTrial TEND

  • IMATINIB   SLC2A4

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    16707477


    Sources:
    NCI

  • IMATINIB   CYP2B6

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    24293093


    Sources:
    PharmGKB

  • IMATINIB   ABCC2

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    30237583


    Sources:
    PharmGKB

  • IMATINIB   ALK

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    16970400


    Sources:
    NCI

  • IMATINIB   MAPK10

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • IMATINIB   FRK

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • IMATINIB   EYA2

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • IMATINIB   TAOK1

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • IMATINIB   JAK2

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type myeloid leukemia
    Response Type resistant
    Approval Status Preclinical - Cell culture

    PMIDs:
    21224473


    Sources:
    JAX-CKB

  • IMATINIB   EGFR

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    22323597 28762371


    Sources:
    JAX-CKB PharmGKB

  • IMATINIB   FLT3

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    15345593


    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

  • IMATINIB   CLK4

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • IMATINIB   CYP3A5

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    27426203


    Sources:
    PharmGKB

  • IMATINIB   LCK

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • IMATINIB   MET

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Imatinib + Carboplatin + Paclitaxel
    Indication/Tumor Type melanoma
    Response Type sensitive

    PMIDs:
    28514312


    Sources:
    JAX-CKB

  • IMATINIB   ABCB1

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15155841 15805252


    Sources:
    NCI

  • IMATINIB   YES1

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • IMATINIB   SMAD3

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • IMATINIB   CYP1A2

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    30713339


    Sources:
    PharmGKB

  • IMATINIB   CYP3A4

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    18094422


    Sources:
    NCI PharmGKB

  • MyCancerGenome: IMATINIB

    • Version: 20-Jun-2017

    Alternate Names:
    CGP57148 Development Name
    CGP57148B Development Name
    IMATINIB Generic Name

    Drug Info:
    Drug Class Kinase Inhibitors
    FDA Approval GI stromal tumor (KIT+), Dermatofibrosarcoma protuberans, Multiple hematologic malignancies including Philadelphia chromosome-positive ALL and CML
    Drug Class Kinase Inhibitor

    Publications:

  • TEND: IMATINIB

    • Version: 01-August-2011

    Alternate Names:
    IMATINIB Primary Drug Name

    Drug Info:
    Year of Approval 2001
    Drug Class antineoplastic agents, protein kinase inhibitors

    Publications:

  • TdgClinicalTrial: IMATINIB

    • Version: January-2014

    Alternate Names:

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

    Publications:

  • NCI: IMATINIB

    • Version: 14-September-2017

    Alternate Names:
    C1687 NCI drug code

    Drug Info:

    Publications:
    Breedveld et al., 2005, The effect of Bcrp1 (Abcg2) on the in vivo pharmacokinetics and brain penetration of imatinib mesylate (Gleevec): implications for the use of breast cancer resistance protein and P-glycoprotein inhibitors to enable the brain penetration of imatinib in patients., Cancer Res.
    Gunby et al., 2006, Structural insights into the ATP binding pocket of the anaplastic lymphoma kinase by site-directed mutagenesis, inhibitor binding analysis, and homology modeling., J. Med. Chem.
    van Erp et al., 2007, Influence of CYP3A4 inhibition on the steady-state pharmacokinetics of imatinib., Clin. Cancer Res.

  • DTC: IMATINIB

    • Version: 02-September-2020

    Alternate Names:
    CHEMBL941 ChEMBL Drug ID

    Drug Info:

    Publications:
    Corradi V et al., 2011, Computational techniques are valuable tools for the discovery of protein-protein interaction inhibitors: the 14-3-3σ case., Bioorg Med Chem Lett
    Michaelis S et al., 2012, Dabigatran and dabigatran ethyl ester: potent inhibitors of ribosyldihydronicotinamide dehydrogenase (NQO2)., J Med Chem
    Page BD et al., 2012, Small molecule STAT5-SH2 domain inhibitors exhibit potent antileukemia activity., J Med Chem

  • NCI: STI-571

    • Version: 14-September-2017

    Alternate Names:
    C1687 NCI drug code

    Drug Info:

    Publications:
    Porosnicu et al., 2001, Co-treatment with As2O3 enhances selective cytotoxic effects of STI-571 against Brc-Abl-positive acute leukemia cells., Leukemia
    Nimmanapalli et al., 2001, Cotreatment with STI-571 enhances tumor necrosis factor alpha-related apoptosis-inducing ligand (TRAIL or apo-2L)-induced apoptosis of Bcr-Abl-positive human acute leukemia cells., Clin. Cancer Res.

  • NCI: GLEEVEC

    • Version: 14-September-2017

    Alternate Names:
    C1687 NCI drug code

    Drug Info:

    Publications:
    Wang et al., 2005, AML1-ETO and C-KIT mutation/overexpression in t(8;21) leukemia: implication in stepwise leukemogenesis and response to Gleevec., Proc. Natl. Acad. Sci. U.S.A.
    Breedveld et al., 2005, The effect of Bcrp1 (Abcg2) on the in vivo pharmacokinetics and brain penetration of imatinib mesylate (Gleevec): implications for the use of breast cancer resistance protein and P-glycoprotein inhibitors to enable the brain penetration of imatinib in patients., Cancer Res.
    Ozvegy-Laczka et al., 2004, High-affinity interaction of tyrosine kinase inhibitors with the ABCG2 multidrug transporter., Mol. Pharmacol.

  • JAX-CKB: Imatinib

    • Version: 27-September-2017

    Alternate Names:

    Drug Info:

    Publications:
    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)
    Curtis et al., 2007, Two novel imatinib-responsive PDGFRA fusion genes in chronic eosinophilic leukaemia., Br. J. Haematol.
    Hammerman et al., 2011, Mutations in the DDR2 kinase gene identify a novel therapeutic target in squamous cell lung cancer., Cancer Discov

  • DoCM: IMATINIB

    • Version: 27-September-2017

    Alternate Names:

    Drug Info:

    Publications:
    Corless et al., 2005, PDGFRA mutations in gastrointestinal stromal tumors: frequency, spectrum and in vitro sensitivity to imatinib., J. Clin. Oncol.
    Debiec-Rychter et al., 2005, Mechanisms of resistance to imatinib mesylate in gastrointestinal stromal tumors and activity of the PKC412 inhibitor against imatinib-resistant mutants., Gastroenterology
    Cassier et al., 2012, Outcome of patients with platelet-derived growth factor receptor alpha-mutated gastrointestinal stromal tumors in the tyrosine kinase inhibitor era., Clin. Cancer Res.

  • PharmGKB: imatinib

    • Version: 18-August-2020

    Alternate Names:

    Drug Info:

    Publications:
    Tuveson DA et al., 2001, STI571 inactivation of the gastrointestinal stromal tumor c-KIT oncoprotein: biological and clinical implications., Oncogene
    Ravegnini G et al., 2019, An exploratory study by DMET array identifies a germline signature associated with imatinib response in gastrointestinal stromal tumor., Pharmacogenomics J
    Ehmann F et al., 2014, European Medicines Agency initiatives and perspectives on pharmacogenomics., Br J Clin Pharmacol

  • CIViC: IMATINIB

    • Version: 14-September-2020

    Alternate Names:

    Drug Info:

    Publications:
    An et al., 2010, BCR-ABL tyrosine kinase inhibitors in the treatment of Philadelphia chromosome positive chronic myeloid leukemia: a review., Leuk. Res.
    Testoni et al., 2016, Somatically mutated ABL1 is an actionable and essential NSCLC survival gene., EMBO Mol Med
    Redaelli et al., 2009, Activity of bosutinib, dasatinib, and nilotinib against 18 imatinib-resistant BCR/ABL mutants., J. Clin. Oncol.

  • TTD: Imatinib

    • Version: 2020.06.01

    Alternate Names:
    D0AZ3C TTD Drug ID

    Drug Info:

    Publications:

  • TALC: IMATINIB

    • Version: 12-May-2016

    Alternate Names:
    IMATINIB Primary Drug Name
    IMATINIB Drug Generic Name
    GLEEVEC Drug Trade Name

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL941

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

  • OncoKB: Imatinib

    • Version: 23-July-2020

    Alternate Names:

    Drug Info:

    Publications:

  • FDA: Imatinib

    • Version: 04-September-2020

    Alternate Names:

    Drug Info:

    Publications:

  • COSMIC: Imatinib

    • Version: 4-Sep-2020

    Alternate Names:

    Drug Info:

    Publications:

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