DGIdb - IMATINIB Drug Record

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

(15 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
Rackemann et al., 1990, Uncemented press-fit total knee arthroplasty., J Arthroplasty
Mukherjee et al., 2009, Human schwannomas express activated platelet-derived growth factor receptors and c-kit and are growth inhibited by Gleevec (Imatinib Mesylate)., Cancer Res.
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 SLC22A4

Interaction Score: 2.81

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23127916 22875622

Sources:
PharmGKB
IMATINIB FIP1L1

Interaction Score: 2.81

Interaction Types & Directionality:

n/a

Interaction Info:

Fusion protein FIP1L1:PDGFRA

PMIDs:
24433361

Sources:
PharmGKB FDA
IMATINIB DDR1

Interaction Score: 2.5

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
15972446 16298518 15994946 16401709 16168515

Sources:
TdgClinicalTrial TEND GuideToPharmacology
IMATINIB RCSD1

Interaction Score: 1.88

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
27125982

Sources:
CIViC
IMATINIB UGT2A1

Interaction Score: 1.88

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
30237583

Sources:
PharmGKB
IMATINIB CHST1

Interaction Score: 1.88

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
30237583

Sources:
PharmGKB
IMATINIB CYP2F1

Interaction Score: 1.88

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
30237583

Sources:
PharmGKB
IMATINIB BCL2L11

Interaction Score: 1.88

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
24223824 22426421

Sources:
CIViC PharmGKB
IMATINIB SFN

Interaction Score: 1.88

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
21962576

Sources:
DTC
IMATINIB SLC22A5

Interaction Score: 1.41

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
28762371 23127916

Sources:
PharmGKB
IMATINIB KIT

Interaction Score: 1.29

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 CGI TEND DoCM COSMIC CIViC PharmGKB TTD FDA OncoKB
IMATINIB ULK3

Interaction Score: 0.94

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
15073101

Sources:
PharmGKB
IMATINIB BCR

Interaction Score: 0.78

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 PDGFRA

Interaction Score: 0.57

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 CGI TEND DoCM COSMIC CIViC FDA OncoKB
IMATINIB SLC22A1

Interaction Score: 0.56

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
30713339 30237583 29427770 28762371 24589908 18398725 23223357 19584153

Sources:
PharmGKB
IMATINIB ABL1

Interaction Score: 0.47

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 CGI TEND COSMIC CIViC GuideToPharmacology PharmGKB FDA OncoKB
IMATINIB ABL2

Interaction Score: 0.38

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
25207766

Sources:
CIViC
IMATINIB IKZF1

Interaction Score: 0.31

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
30044693

Sources:
CIViC
IMATINIB ABCB4

Interaction Score: 0.27

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
30237583

Sources:
PharmGKB
IMATINIB SLCO1A2

Interaction Score: 0.27

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
21633340

Sources:
PharmGKB
IMATINIB NF2

Interaction Score: 0.23

Interaction Types & Directionality:

n/a

Interaction Info:

Drug family BCR-ABL inhibitor 1st gen&KIT inhibitor

Alteration NF2:del

Alteration NF2:.

PMIDs:
2290085 19509233

Sources:
CGI
IMATINIB PDGFB

Interaction Score: 0.23

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
OncoKB
IMATINIB PDGFRB

Interaction Score: 0.23

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Drug family BCR-ABL inhibitor 1st gen&KIT inhibitor

Alteration PDGFRB__COL1A1

Trial Name imatinib mesylate, STI 571,Gleevec, Glivec

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

Sources:
DTC MyCancerGenome TdgClinicalTrial CGI TEND CIViC PharmGKB FDA OncoKB
IMATINIB CSF1R

Interaction Score: 0.22

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 CGI TEND DoCM CIViC
IMATINIB GSTT1

Interaction Score: 0.19

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
25188725

Sources:
PharmGKB
IMATINIB SLC19A1

Interaction Score: 0.17

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
30237583

Sources:
PharmGKB
IMATINIB CD40LG

Interaction Score: 0.17

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: 0.13

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
11368438 11234890

Sources:
NCI
IMATINIB NQO2

Interaction Score: 0.13

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22494098

Sources:
DTC
IMATINIB ABCG2

Interaction Score: 0.12

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
15805252 30713339 24322003 24123600 18981009 15155841

Sources:
NCI PharmGKB
IMATINIB DDR2

Interaction Score: 0.12

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
None found

Sources:
GuideToPharmacology
IMATINIB NTRK1

Interaction Score: 0.12

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 CTNNB1

Interaction Score: 0.1

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Clinical Study

Response Type sensitive

PMIDs:
26861905

Sources:
JAX-CKB
IMATINIB PRKCH

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Trametinib;Imatinib

Drug family MEK inhibitor;BCR-ABL inhibitor 1st gen&KIT inhibitor

Alteration PRKCH:amp;ABL1__BCR

PMIDs:
None found

Sources:
CGI
IMATINIB NQO1

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
30237583

Sources:
PharmGKB
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 LYN

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
18191450

Sources:
DTC CIViC
IMATINIB ABCC4

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23127916

Sources:
PharmGKB
IMATINIB RUNX1

Interaction Score: 0.05

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 NF1

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

Drug family BCR-ABL inhibitor 1st gen&KIT inhibitor

Alteration NF1:del

Alteration NF1:.

PMIDs:
None found

Sources:
CGI
IMATINIB SLC2A4

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16707477

Sources:
NCI
IMATINIB RET

Interaction Score: 0.04

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 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: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16970400

Sources:
NCI
IMATINIB FRK

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
IMATINIB MAPK10

Interaction Score: 0.03

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 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 LCK

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
IMATINIB ABCB1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
15155841 15805252

Sources:
NCI
IMATINIB KRAS

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

Drug family BCR-ABL inhibitor 1st gen&KIT inhibitor

Alteration KRAS:G12.

PMIDs:
None found

Sources:
CGI
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

GLEEVEC Trade 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

CGI: Imatinib

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Wasag et al., 2011, Novel, activating KIT-N822I mutation in familial cutaneous mastocytosis., Exp. Hematol.

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.

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.

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.

GuideToPharmacology: 178102314
- Version: 29-September-2020
Alternate Names:

IMATINIB GuideToPharmacology Ligand Name

Drug Info:

Publications:
TTD: Imatinib
- Version: 2020.06.01
Alternate Names:

D0AZ3C TTD Drug ID

Drug Info:

Publications:
TALC: IMATINIB
- Version: 12-May-2016
Alternate Names:

GLEEVEC Drug Trade Name

IMATINIB Drug Generic Name

IMATINIB Primary Drug 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:

Specific Action of the Ligand	Inhibition
Endogenous Drug?	False
Direct Interaction?	False

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

Clinical Status	preclinical
Pathway	activation
Variant Effect	gain-of-function

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

Drug family	BCR-ABL inhibitor 1st gen&KIT inhibitor
Alteration	NF2:del
Alteration	NF2:.

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

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

Evidence Type	Actionable
Approval Status	Clinical Study
Response Type	sensitive

combination therapy	Trametinib;Imatinib
Drug family	MEK inhibitor;BCR-ABL inhibitor 1st gen&KIT inhibitor
Alteration	PRKCH:amp;ABL1__BCR

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

antagonist (inhibitory)
inhibitor (inhibitory)

multitarget
antagonist (inhibitory)
inhibitor (inhibitory)

antagonist (inhibitory)
inhibitor (inhibitory)

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

CGP57148	Development Name
CGP57148B	Development Name
GLEEVEC	Trade Name

GLEEVEC	Drug Trade Name
IMATINIB	Drug Generic Name
IMATINIB	Primary Drug Name

IMATINIB Drug Record

IMATINIB chembl:CHEMBL941 ApprovedAntineoplasticImmunotherapy

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 23127916 22875622

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info: Fusion protein FIP1L1:PDGFRA

PMIDs: 24433361

Sources: PharmGKB FDA

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

Interaction Info: Specific Action of the Ligand Inhibition Endogenous Drug? False Direct Interaction? False

PMIDs: 15972446 16298518 15994946 16401709 16168515

Sources: TdgClinicalTrial TEND GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 27125982

Sources: CIViC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 30237583

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 30237583

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 30237583

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 24223824 22426421

Sources: CIViC PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 21962576

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 28762371 23127916

Sources: PharmGKB

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

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

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

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 15073101

Sources: PharmGKB

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

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 CGI TEND DoCM COSMIC CIViC FDA OncoKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 30713339 30237583 29427770 28762371 24589908 18398725 23223357 19584153

Sources: PharmGKB

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 CGI TEND COSMIC CIViC GuideToPharmacology PharmGKB FDA OncoKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 25207766

Sources: CIViC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 30044693

Sources: CIViC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 30237583

Sources: PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
23127916 22875622

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

Interaction Info:

Fusion protein FIP1L1:PDGFRA

PMIDs:
24433361

Sources:
PharmGKB FDA

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
15972446 16298518 15994946 16401709 16168515

Sources:
TdgClinicalTrial TEND GuideToPharmacology

Interaction Types & Directionality:

n/a

PMIDs:
27125982

Sources:
CIViC

Interaction Types & Directionality:

n/a

PMIDs:
30237583

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
30237583

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
30237583

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
24223824 22426421

Sources:
CIViC PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
21962576

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
28762371 23127916

Sources:
PharmGKB

Interaction Types & Directionality:

multitarget

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Approval Status Guideline

Indication/Tumor Type prostate neuroendocrine neoplasm

Approval Status Phase II

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

Interaction Types & Directionality:

n/a

PMIDs:
15073101

Sources:
PharmGKB

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

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 CGI TEND DoCM COSMIC CIViC FDA OncoKB

Interaction Types & Directionality:

n/a

PMIDs:
30713339 30237583 29427770 28762371 24589908 18398725 23223357 19584153

Sources:
PharmGKB

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 CGI TEND COSMIC CIViC GuideToPharmacology PharmGKB FDA OncoKB

Interaction Types & Directionality:

n/a

PMIDs:
25207766

Sources:
CIViC

Interaction Types & Directionality:

n/a

PMIDs:
30044693

Sources:
CIViC

Interaction Types & Directionality:

n/a

PMIDs:
30237583

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
21633340

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

Interaction Info:

Drug family BCR-ABL inhibitor 1st gen&KIT inhibitor

Alteration NF2:del

Alteration NF2:.

PMIDs:
2290085 19509233

Sources:
CGI

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
OncoKB

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Drug family BCR-ABL inhibitor 1st gen&KIT inhibitor

Alteration PDGFRB__COL1A1

Trial Name imatinib mesylate, STI 571,Gleevec, Glivec

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

Sources:
DTC MyCancerGenome TdgClinicalTrial CGI TEND CIViC PharmGKB FDA OncoKB

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 CGI TEND DoCM CIViC