DGIdb - SUNITINIB Drug Record

SUNITINIB chembl:CHEMBL535 ApprovedAntineoplasticImmunotherapy

Alternate Names:

SU-11248
SU-011248
SUTENT
SUNITINIB
SU011248
SUNITINIBUM
SUTENT®
SU11248
rxcui:357977
chembl:CHEMBL535
pubchem.compound:5329102
drugbank:01268
chemidplus:557795-19-4

Drug Info:

Drug Class	Kinase Inhibitors
Drug Class	antineoplastic agents, protein kinase inhibitors
Year of Approval	2006
FDA Approval	approved
Drug Class	Small Molecule
Drug Indications	antineoplastic agent

(11 More Sources)

Publications:

Iwata H et al., 2011, Biochemical characterization of a novel type-II VEGFR2 kinase inhibitor: comparison of binding to non-phosphorylated and phosphorylated VEGFR2., Bioorg Med Chem
Perspicace E et al., 2013, Design, synthesis and biological evaluation of new classes of thieno[3,2-d]pyrimidinone and thieno[1,2,3]triazine as inhibitor of vascular endothelial growth factor receptor-2 (VEGFR-2)., Eur J Med Chem
Choi HE et al., 2011, BRN-103, a novel nicotinamide derivative, inhibits VEGF-induced angiogenesis and proliferation in human umbilical vein endothelial cells., Bioorg Med Chem Lett
Maitland ML et al., 2010, Vascular endothelial growth factor pathway., Pharmacogenet Genomics
Quek R et al., 2009, Gastrointestinal stromal tumor: a clinical overview., Hematol Oncol Clin North Am
Mendel et al., 2003, In vivo antitumor activity of SU11248, a novel tyrosine kinase inhibitor targeting vascular endothelial growth factor and platelet-derived growth factor receptors: determination of a pharmacokinetic/pharmacodynamic relationship., Clin. Cancer Res.
Wragg et al., 2017, Sunitinib Treatment Enhances Metastasis of Innately Drug-Resistant Breast Tumors., Cancer Res.
Wang et al., 2016, Recurrent Olfactory Neuroblastoma Treated With Cetuximab and Sunitinib: A Case Report., Medicine (Baltimore)
Gallagher et al., 2010, Phase II study of sunitinib in patients with metastatic urothelial cancer., J. Clin. Oncol.
Antonescu et al., 2009, KDR activating mutations in human angiosarcomas are sensitive to specific kinase inhibitors., Cancer Res.
Schöffski et al., 2006, Emerging role of tyrosine kinase inhibitors in the treatment of advanced renal cell cancer: a review., Ann. Oncol.
Schueneman et al., 2003, SU11248 maintenance therapy prevents tumor regrowth after fractionated irradiation of murine tumor models., Cancer Res.
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Barattè et al., 2004, Quantitation of SU1 1248, an oral multi-target tyrosine kinase inhibitor, and its metabolite in monkey tissues by liquid chromatograph with tandem mass spectrometry following semi-automated liquid-liquid extraction., J Chromatogr A
Amino et al., 2006, YM-359445, an orally bioavailable vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor, has highly potent antitumor activity against established tumors., Clin. Cancer Res.
Silva E et al., 2015, Refractory angiosarcoma of the breast with VEGFR2 upregulation successfully treated with sunitinib., Breast J
Dornbusch J et al., 2016, Evaluation of polymorphisms in angiogenesis-related genes as predictive and prognostic markers for sunitinib-treated metastatic renal cell carcinoma patients., J Cancer Res Clin Oncol
Roskoski, 2007, Sunitinib: a VEGF and PDGF receptor protein kinase and angiogenesis inhibitor., Biochem. Biophys. Res. Commun.
O'Farrell et al., 2003, An innovative phase I clinical study demonstrates inhibition of FLT3 phosphorylation by SU11248 in acute myeloid leukemia patients., Clin. Cancer Res.
Terakawa et al., 2013, Expression level of vascular endothelial growth factor receptor-2 in radical nephrectomy specimens as a prognostic predictor in patients with metastatic renal cell carcinoma treated with sunitinib., Urol. Oncol.
Dornbusch et al., 2013, Analyses of potential predictive markers and survival data for a response to sunitinib in patients with metastatic renal cell carcinoma., PLoS ONE
Chu YH et al., 2015, Association of ABCB1 and FLT3 Polymorphisms with Toxicities and Survival in Asian Patients Receiving Sunitinib for Renal Cell Carcinoma., PLoS One
Kim HR et al., 2013, Pharmacogenetic determinants associated with sunitinib-induced toxicity and ethnic difference in Korean metastatic renal cell carcinoma patients., Cancer Chemother Pharmacol
van Erp NP et al., 2010, Myelosuppression by sunitinib is flt-3 genotype dependent., Br J Cancer
van Erp et al., 2009, Pharmacogenetic pathway analysis for determination of sunitinib-induced toxicity., J. Clin. Oncol.
Griffith et al., 2016, Comprehensive genomic analysis reveals FLT3 activation and a therapeutic strategy for a patient with relapsed adult B-lymphoblastic leukemia., Exp. Hematol.
Gozgit et al., 2011, Potent activity of ponatinib (AP24534) in models of FLT3-driven acute myeloid leukemia and other hematologic malignancies., Mol. Cancer Ther.
O'Farrell et al., 2003, SU11248 is a novel FLT3 tyrosine kinase inhibitor with potent activity in vitro and in vivo., Blood
Yee et al., 2004, Synergistic effect of SU11248 with cytarabine or daunorubicin on FLT3 ITD-positive leukemic cells., Blood
Schmidt-Arras et al., 2004, Flt3 receptor tyrosine kinase as a drug target in leukemia., Curr. Pharm. Des.
Fiedler et al., 2015, A phase I/II study of sunitinib and intensive chemotherapy in patients over 60 years of age with acute myeloid leukaemia and activating FLT3 mutations., Br. J. Haematol.
Albers et al., 2013, The secondary FLT3-ITD F691L mutation induces resistance to AC220 in FLT3-ITD+ AML but retains in vitro sensitivity to PKC412 and Sunitinib., Leukemia
Williams AB et al., 2013, Mutations of FLT3/ITD confer resistance to multiple tyrosine kinase inhibitors., Leukemia
Schittenhelm MM et al., 2006, FLT3 K663Q is a novel AML-associated oncogenic kinase: Determination of biochemical properties and sensitivity to Sunitinib (SU11248)., Leukemia
Xiao W et al., 2018, A favorable outcome of advanced dermatofibrosarcoma protuberans under treatment with sunitinib after imatinib failure., Onco Targets Ther
De Mattia E et al., 2016, Pregnane X receptor, constitutive androstane receptor and hepatocyte nuclear factors as emerging players in cancer precision medicine., Pharmacogenomics
Gollob, 2005, Sorafenib: scientific rationales for single-agent and combination therapy in clear-cell renal cell carcinoma., Clin Genitourin Cancer
Pietras et al., 2005, A multitargeted, metronomic, and maximum-tolerated dose "chemo-switch" regimen is antiangiogenic, producing objective responses and survival benefit in a mouse model of cancer., J. Clin. Oncol.
Abrams et al., 2003, SU11248 inhibits KIT and platelet-derived growth factor receptor beta in preclinical models of human small cell lung cancer., Mol. Cancer Ther.
Gridelli et al., 2007, Sorafenib and sunitinib in the treatment of advanced non-small cell lung cancer., Oncologist
Ahmed et al., 2004, Vascular endothelial growth factor (VEGF) inhibition by small molecules., J Chemother
Katoh et al., 2006, Comparative integromics on VEGF family members., Int. J. Oncol.
Deprimo et al., 2007, Circulating protein biomarkers of pharmacodynamic activity of sunitinib in patients with metastatic renal cell carcinoma: modulation of VEGF and VEGF-related proteins., J Transl Med
Garcia-Donas J et al., 2011, Single nucleotide polymorphism associations with response and toxic effects in patients with advanced renal-cell carcinoma treated with first-line sunitinib: a multicentre, observational, prospective study., Lancet 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.
Girard et al., 2009, Comprehensive genomic analysis reveals clinically relevant molecular distinctions between thymic carcinomas and thymomas., Clin. Cancer Res.
Buti et al., 2011, Impressive response with imatinib in a heavily pretreated patient with metastatic c-KIT mutated thymic carcinoma., J. Clin. Oncol.
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.
Reichardt et al., 2016, Correlation of KIT and PDGFRA mutational status with clinical benefit in patients with gastrointestinal stromal tumor treated with sunitinib in a worldwide treatment-use trial., BMC Cancer
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.
Rutkowski et al., 2012, The outcome and predictive factors of sunitinib therapy in advanced gastrointestinal stromal tumors (GIST) after imatinib failure - one institution study., BMC Cancer
Prenen et al., 2006, Efficacy of the kinase inhibitor SU11248 against gastrointestinal stromal tumor mutants refractory to imatinib mesylate., Clin. Cancer Res.
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.
Joensuu, 2007, Second line therapies for the treatment of gastrointestinal stromal tumor., Curr Opin Oncol
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.
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
Diekstra MH et al., 2015, Association of single nucleotide polymorphisms in IL8 and IL13 with sunitinib-induced toxicity in patients with metastatic renal cell carcinoma., Eur J Clin Pharmacol
Behjati et al., 2014, Recurrent PTPRB and PLCG1 mutations in angiosarcoma., Nat. Genet.
Kim et al., 2006, An orally administered multitarget tyrosine kinase inhibitor, SU11248, is a novel potent inhibitor of thyroid oncogenic RET/papillary thyroid cancer kinases., J. Clin. Endocrinol. Metab.
Gautschi et al., 2017, Targeting RET in Patients With RET-Rearranged Lung Cancers: Results From the Global, Multicenter RET Registry., J. Clin. Oncol.
Jones et al., 2010, Evolution of an adenocarcinoma in response to selection by targeted kinase inhibitors., Genome Biol.
Gupta-Abramson et al., 2008, Phase II trial of sorafenib in advanced thyroid cancer., J. Clin. Oncol.
Santoro et al., 1998, Molecular biology of the MEN2 gene., J. Intern. Med.
Egawa et al., 1998, Genotype-phenotype correlation of patients with multiple endocrine neoplasia type 2 in Japan., Jpn. J. Clin. Oncol.
Carr et al., 2010, Phase II study of daily sunitinib in FDG-PET-positive, iodine-refractory differentiated thyroid cancer and metastatic medullary carcinoma of the thyroid with functional imaging correlation., Clin. Cancer Res.
Kloos et al., 2009, Phase II trial of sorafenib in metastatic thyroid cancer., J. Clin. Oncol.
Elisei et al., 2008, Prognostic significance of somatic RET oncogene mutations in sporadic medullary thyroid cancer: a 10-year follow-up study., J. Clin. Endocrinol. Metab.
Sherman, 2011, Targeted therapies for thyroid tumors., Mod. Pathol.
Lam et al., 2010, Phase II clinical trial of sorafenib in metastatic medullary thyroid cancer., J. Clin. Oncol.
Frisk et al., 2001, CGH alterations in medullary thyroid carcinomas in relation to the RET M918T mutation and clinical outcome., Int. J. Oncol.
Coxon et al., 2012, Anti-tumor activity of motesanib in a medullary thyroid cancer model., J. Endocrinol. Invest.
Verbeek et al., 2011, The effects of four different tyrosine kinase inhibitors on medullary and papillary thyroid cancer cells., J. Clin. Endocrinol. Metab.
Vitagliano et al., 2011, The tyrosine kinase inhibitor ZD6474 blocks proliferation of RET mutant medullary thyroid carcinoma cells., Endocr. Relat. Cancer
Couto et al., 2012, AZD1480 blocks growth and tumorigenesis of RET- activated thyroid cancer cell lines., PLoS ONE
Wells et al., 2012, Vandetanib in patients with locally advanced or metastatic medullary thyroid cancer: a randomized, double-blind phase III trial., J. Clin. Oncol.
Wells et al., 2010, Vandetanib for the treatment of patients with locally advanced or metastatic hereditary medullary thyroid cancer., J. Clin. Oncol.
MacConaill et al., 2014, Prospective enterprise-level molecular genotyping of a cohort of cancer patients., J Mol Diagn
Guo et al., 2006, Inhibition of phosphorylation of the colony-stimulating factor-1 receptor (c-Fms) tyrosine kinase in transfected cells by ABT-869 and other tyrosine kinase inhibitors., Mol. Cancer Ther.
Diekstra MH et al., 2014, Association analysis of genetic polymorphisms in genes related to sunitinib pharmacokinetics, specifically clearance of sunitinib and SU12662., Clin Pharmacol Ther
Adams VR et al., 2007, Sunitinib malate for the treatment of metastatic renal cell carcinoma and gastrointestinal stromal tumors., Clin Ther
Eechoute K et al., 2012, Polymorphisms in endothelial nitric oxide synthase (eNOS) and vascular endothelial growth factor (VEGF) predict sunitinib-induced hypertension., Clin Pharmacol Ther
Montero et al., 2016, A Phase I Clinical, Pharmacokinetic, and Pharmacodynamic Study of Weekly or Every Three Week Ixabepilone and Daily Sunitinib in Patients with Advanced Solid Tumors., Clin. Cancer Res.
Modest et al., 2013, KRAS allel-specific activity of sunitinib in an isogenic disease model of colorectal cancer., J. Cancer Res. Clin. Oncol.
McDermott et al., 2009, Ligand-dependent platelet-derived growth factor receptor (PDGFR)-alpha activation sensitizes rare lung cancer and sarcoma cells to PDGFR kinase inhibitors., Cancer Res.
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.
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
Ramos AH et al., 2009, Amplification of chromosomal segment 4q12 in non-small cell lung cancer., Cancer Biol Ther
Bridgeman et al., 2016, Preclinical Evidence That Trametinib Enhances the Response to Antiangiogenic Tyrosine Kinase Inhibitors in Renal Cell Carcinoma., Mol. Cancer Ther.
Jonasch et al., 2011, Pilot trial of sunitinib therapy in patients with von Hippel-Lindau disease., Ann. Oncol.
Narjoz C et al., 2015, Role of the lean body mass and of pharmacogenetic variants on the pharmacokinetics and pharmacodynamics of sunitinib in cancer patients., Invest New Drugs
Kloth JSL et al., 2018, Genetic polymorphisms as predictive biomarker of survival in patients with gastrointestinal stromal tumors treated with sunitinib., Pharmacogenomics J
Zheng et al., 2015, Heme oxygenase-1 is a predictive biomarker for therapeutic targeting of advanced clear cell renal cell carcinoma treated with sorafenib or sunitinib., Onco Targets Ther
Bachelot et al., 2014, Sunitinib in combination with trastuzumab for the treatment of advanced breast cancer: activity and safety results from a phase II study., BMC Cancer
Numakura K et al., 2017, Clinical effects of single nucleotide polymorphisms on drug-related genes in Japanese metastatic renal cell carcinoma patients treated with sunitinib., Anticancer Drugs
Teo YL et al., 2016, Effect of the CYP3A5 and ABCB1 genotype on exposure, clinical response and manifestation of toxicities from sunitinib in Asian patients., Pharmacogenomics J
Beuselinck B et al., 2014, Efflux pump ABCB1 single nucleotide polymorphisms and dose reductions in patients with metastatic renal cell carcinoma treated with sunitinib., Acta Oncol
Hsieh et al., 2017, Genomic Biomarkers of a Randomized Trial Comparing First-line Everolimus and Sunitinib in Patients with Metastatic Renal Cell Carcinoma., Eur. Urol.
Stacchiotti S et al., 2014, Activity of sunitinib in extraskeletal myxoid chondrosarcoma., Eur J Cancer
Nair A et al., 2018, Combinatorial inhibition of PTPN12-regulated receptors leads to a broadly effective therapeutic strategy in triple-negative breast cancer., Nat Med
Harmon CS et al., 2011, Mechanism-related circulating proteins as biomarkers for clinical outcome in patients with unresectable hepatocellular carcinoma receiving sunitinib., J Transl Med

SUNITINIB EWSR1

Interaction Score: 3.17

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
24703573

Sources:
CIViC
SUNITINIB KDM5C

Interaction Score: 1.59

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
27751729

Sources:
CIViC
SUNITINIB PDGFD

Interaction Score: 1.59

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenomeClinicalTrial
SUNITINIB PTPRB

Interaction Score: 1.59

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
24633157

Sources:
CIViC
SUNITINIB PDGFC

Interaction Score: 1.59

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenomeClinicalTrial
SUNITINIB PDGFB

Interaction Score: 1.19

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
29760553

Sources:
CIViC MyCancerGenomeClinicalTrial
SUNITINIB PTPN12

Interaction Score: 1.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
29578538

Sources:
CIViC
SUNITINIB KIT

Interaction Score: 0.88

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Clinical Status preclinical

Variant Effect gain-of-function

Pathway activation

PMIDs:
22261812 21690468 21642685 18421059 19861435 21969494 23375402 22357254 26772734 25239608 22439647 16638875 18955458 17545799 17367763 12873999 14753710 11752352 12748309 19164557 25594040 23582185 19248971

Sources:
TALC MyCancerGenome TdgClinicalTrial JAX-CKB TEND DoCM COSMIC CIViC MyCancerGenomeClinicalTrial PharmGKB OncoKB
SUNITINIB HMOX1

Interaction Score: 0.79

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
26309414

Sources:
CIViC
SUNITINIB PDGFA

Interaction Score: 0.79

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenomeClinicalTrial
SUNITINIB RET

Interaction Score: 0.77

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

combination therapy Cetuximab + Sunitinib

Indication/Tumor Type olfactory neuroblastoma

Response Type sensitive

PMIDs:
16849418 28447912 27149458 19248971 20696054 18541894 9681850 9839497 20847059 19255327 18073307 21455200 20368568 11351254 21422803 21470995 20943719 23056499 22025146 20065189 25157968

Sources:
TALC MyCancerGenome TdgClinicalTrial JAX-CKB NCI TEND DoCM CIViC PharmGKB
SUNITINIB PDGFRA

Interaction Score: 0.57

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type Advanced Solid Tumor

Response Type resistant

Approval Status Preclinical - Cell culture

PMIDs:
19366796 18955458 16638875 22718859 25157968 14645423 16954519 22745105 18794084 15928335 26130666 15146165 15685537 12949711 21482694 19755855

Sources:
TdgClinicalTrial JAX-CKB TEND DoCM COSMIC CIViC MyCancerGenomeClinicalTrial
SUNITINIB VEGFC

Interaction Score: 0.53

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
21787417

Sources:
CIViC
SUNITINIB BAP1

Interaction Score: 0.53

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
27751729

Sources:
CIViC
SUNITINIB FLT3

Interaction Score: 0.48

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Trial Name Sutent

Novel drug target Established target

PMIDs:
26244574 24013576 20683446 19667267 19248971 27181063 21482694 14654525 12531805 15304385 11752352 14753710 15180525 25818407 23392356 22858906 16990784

Sources:
TALC MyCancerGenome TdgClinicalTrial JAX-CKB TEND COSMIC CIViC MyCancerGenomeClinicalTrial PharmGKB
SUNITINIB POR

Interaction Score: 0.4

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
28117434

Sources:
PharmGKB
SUNITINIB IL13

Interaction Score: 0.4

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
26387812

Sources:
PharmGKB
SUNITINIB PBRM1

Interaction Score: 0.35

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
27751729

Sources:
CIViC
SUNITINIB KDR

Interaction Score: 0.33

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type Advanced Solid Tumor

Response Type sensitive

Approval Status Preclinical

PMIDs:
21885287 23583911 21963305 20124951 19248971 12538485 28011623 27149458 20142593 19723655 16418310 12873999 11752352 14753710 16533791 25639617

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

Interaction Score: 0.32

Interaction Types & Directionality:

n/a

Interaction Info:

Approval Status Preclinical - Pdx

Response Type predicted – sensitive

Indication/Tumor Type kidney cancer

PMIDs:
26487278 22105611

Sources:
JAX-CKB
SUNITINIB PDGFRB

Interaction Score: 0.29

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Trial Name Sutent

Novel drug target Established target

PMIDs:
29760553 16425993 15557593 14753710 12748309 12538485 19248971

Sources:
TALC MyCancerGenome TdgClinicalTrial TEND CIViC PharmGKB
SUNITINIB FLT1

Interaction Score: 0.28

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name Sutent

Novel drug target Established target

Notes

PMIDs:
23583911 26935927 20124951 19248971 17367763 14654525 21478036 24086736

Sources:
TALC DTC TdgClinicalTrial TEND MyCancerGenomeClinicalTrial PharmGKB
SUNITINIB FLT4

Interaction Score: 0.23

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name Sutent

Notes

PMIDs:
17367763 17296815 15688612 16685460 17605814 22015057 19248971

Sources:
TALC TdgClinicalTrial TEND MyCancerGenomeClinicalTrial PharmGKB
SUNITINIB NR1I3

Interaction Score: 0.23

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
27561454

Sources:
PharmGKB
SUNITINIB SLCO1B3

Interaction Score: 0.16

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
28117434

Sources:
PharmGKB
SUNITINIB NOS3

Interaction Score: 0.14

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
21963305

Sources:
DTC
SUNITINIB ABCG2

Interaction Score: 0.1

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
26244574 25344452 24013576

Sources:
PharmGKB
SUNITINIB CSF1R

Interaction Score: 0.1

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
17367763 16648572

Sources:
TEND
SUNITINIB VEGFA

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22948895

Sources:
PharmGKB
SUNITINIB FGFR2

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Cetuximab + Sunitinib

Indication/Tumor Type olfactory neuroblastoma

Response Type sensitive

PMIDs:
27149458

Sources:
JAX-CKB
SUNITINIB CXCL8

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
26387812

Sources:
PharmGKB
SUNITINIB CYP3A5

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
24013576 22015057

Sources:
PharmGKB
SUNITINIB ABCB1

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
27564227 26244574 25778465 24874929 24013576

Sources:
PharmGKB
SUNITINIB KRAS

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

Approval Status Phase I

Response Type predicted – sensitive

combination therapy Ixabepilone + Sunitinib

PMIDs:
26864210 23455880

Sources:
JAX-CKB
SUNITINIB NR1I2

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
25344452

Sources:
PharmGKB
SUNITINIB ERBB2

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Sunitinib + Trastuzumab

Indication/Tumor Type Her2-receptor positive breast cancer

Response Type sensitive

PMIDs:
24606768

Sources:
JAX-CKB
SUNITINIB EGFR

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Cetuximab + Sunitinib

Indication/Tumor Type olfactory neuroblastoma

Response Type sensitive

PMIDs:
27149458

Sources:
JAX-CKB
SUNITINIB YES1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
SUNITINIB CYP3A4

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
24566734 17825686

Sources:
PharmGKB

MyCancerGenome: SUNITINIB
- Version: 20-Jun-2017
Alternate Names:

SU-11248 Development Name

SUNITINIB Generic Name

SUTENT Trade Name

Drug Info:

Drug Class Kinase Inhibitors

Publications:
TEND: SUNITINIB
- Version: 01-August-2011
Alternate Names:

SUNITINIB Primary Drug Name

Drug Info:

Year of Approval 2006

Drug Class antineoplastic agents, protein kinase inhibitors

Publications:
TdgClinicalTrial: SUNITINIB
- Version: January-2014
Alternate Names:

Drug Info:

Drug Indications antineoplastic agent

Drug Class Small Molecule

FDA Approval approved

Publications:

NCI: SU11248

Version: 14-September-2017

Alternate Names:

C26673 NCI drug code

Drug Info:

Publications:

Kim et al., 2006, An orally administered multitarget tyrosine kinase inhibitor, SU11248, is a novel potent inhibitor of thyroid oncogenic RET/papillary thyroid cancer kinases., J. Clin. Endocrinol. Metab.

DTC: SUNITINIB

Version: 02-September-2020

Alternate Names:

CHEMBL535 ChEMBL Drug ID

Drug Info:

Publications:

Perspicace E et al., 2013, Design, synthesis and biological evaluation of new classes of thieno[3,2-d]pyrimidinone and thieno[1,2,3]triazine as inhibitor of vascular endothelial growth factor receptor-2 (VEGFR-2)., Eur J Med Chem

Choi HE et al., 2011, BRN-103, a novel nicotinamide derivative, inhibits VEGF-induced angiogenesis and proliferation in human umbilical vein endothelial cells., Bioorg Med Chem Lett

Iwata H et al., 2011, Biochemical characterization of a novel type-II VEGFR2 kinase inhibitor: comparison of binding to non-phosphorylated and phosphorylated VEGFR2., Bioorg Med Chem

JAX-CKB: Sunitinib

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Jonasch et al., 2011, Pilot trial of sunitinib therapy in patients with von Hippel-Lindau disease., Ann. Oncol.

Bridgeman et al., 2016, Preclinical Evidence That Trametinib Enhances the Response to Antiangiogenic Tyrosine Kinase Inhibitors in Renal Cell Carcinoma., Mol. Cancer Ther.

Fiedler et al., 2015, A phase I/II study of sunitinib and intensive chemotherapy in patients over 60 years of age with acute myeloid leukaemia and activating FLT3 mutations., Br. J. Haematol.

DoCM: SUNITINIB

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Girard et al., 2009, Comprehensive genomic analysis reveals clinically relevant molecular distinctions between thymic carcinomas and thymomas., Clin. Cancer Res.

Buti et al., 2011, Impressive response with imatinib in a heavily pretreated patient with metastatic c-KIT mutated thymic carcinoma., J. Clin. Oncol.

Rossi et al., 2013, When a thymic carcinoma "becomes" a GIST., Lung Cancer

PharmGKB: sunitinib

Version: 18-August-2020

Alternate Names:

Drug Info:

Publications:

Diekstra MH et al., 2015, Association of single nucleotide polymorphisms in IL8 and IL13 with sunitinib-induced toxicity in patients with metastatic renal cell carcinoma., Eur J Clin Pharmacol

Adams VR et al., 2007, Sunitinib malate for the treatment of metastatic renal cell carcinoma and gastrointestinal stromal tumors., Clin Ther

Diekstra MH et al., 2014, Association analysis of genetic polymorphisms in genes related to sunitinib pharmacokinetics, specifically clearance of sunitinib and SU12662., Clin Pharmacol Ther

CIViC: SUNITINIB

Version: 14-September-2020

Alternate Names:

Drug Info:

Publications:

van Erp et al., 2009, Pharmacogenetic pathway analysis for determination of sunitinib-induced toxicity., J. Clin. Oncol.

Gozgit et al., 2011, Potent activity of ponatinib (AP24534) in models of FLT3-driven acute myeloid leukemia and other hematologic malignancies., Mol. Cancer Ther.

Schittenhelm MM et al., 2006, FLT3 K663Q is a novel AML-associated oncogenic kinase: Determination of biochemical properties and sensitivity to Sunitinib (SU11248)., Leukemia

TALC: SUNITINIB
- Version: 12-May-2016
Alternate Names:

SUNITINIB Primary Drug Name

SUNITINIB Drug Generic Name

SUTENT Drug Trade Name

Drug Info:

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

D0R0MW TTD Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL535
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
MyCancerGenomeClinicalTrial: SUNITINIB
- Version: 30-February-2014
Alternate Names:

Drug Info:

Publications:
OncoKB: Sunitinib
- Version: 23-July-2020
Alternate Names:

Drug Info:

Publications:
COSMIC: Sunitinib
- Version: 4-Sep-2020
Alternate Names:

Drug Info:

Publications:

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

combination therapy	Cetuximab + Sunitinib
Indication/Tumor Type	olfactory neuroblastoma
Response Type	sensitive

Indication/Tumor Type	Advanced Solid Tumor
Response Type	resistant
Approval Status	Preclinical - Cell culture

Approval Status	Preclinical - Pdx
Response Type	predicted – sensitive
Indication/Tumor Type	kidney cancer

Approval Status	Phase I
Response Type	predicted – sensitive
combination therapy	Ixabepilone + Sunitinib

combination therapy	Sunitinib + Trastuzumab
Indication/Tumor Type	Her2-receptor positive breast cancer
Response Type	sensitive

SU-11248	Development Name
SUNITINIB	Generic Name
SUTENT	Trade Name

SUNITINIB	Primary Drug Name
SUNITINIB	Drug Generic Name
SUTENT	Drug Trade Name

SUNITINIB Drug Record

SUNITINIB chembl:CHEMBL535 ApprovedAntineoplasticImmunotherapy

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 24703573

Sources: CIViC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 27751729

Sources: CIViC

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: None found

Sources: MyCancerGenomeClinicalTrial

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 24633157

Sources: CIViC

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: None found

Sources: MyCancerGenomeClinicalTrial

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: 29760553

Sources: CIViC MyCancerGenomeClinicalTrial

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 29578538

Sources: CIViC

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: 22261812 21690468 21642685 18421059 19861435 21969494 23375402 22357254 26772734 25239608 22439647 16638875 18955458 17545799 17367763 12873999 14753710 11752352 12748309 19164557 25594040 23582185 19248971

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

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 26309414

Sources: CIViC

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: None found

Sources: MyCancerGenomeClinicalTrial

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: combination therapy Cetuximab + Sunitinib Indication/Tumor Type olfactory neuroblastoma Response Type sensitive

PMIDs: 16849418 28447912 27149458 19248971 20696054 18541894 9681850 9839497 20847059 19255327 18073307 21455200 20368568 11351254 21422803 21470995 20943719 23056499 22025146 20065189 25157968

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

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: 19366796 18955458 16638875 22718859 25157968 14645423 16954519 22745105 18794084 15928335 26130666 15146165 15685537 12949711 21482694 19755855

Sources: TdgClinicalTrial JAX-CKB TEND DoCM COSMIC CIViC MyCancerGenomeClinicalTrial

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 21787417

Sources: CIViC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 27751729

Sources: CIViC

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: 26244574 24013576 20683446 19667267 19248971 27181063 21482694 14654525 12531805 15304385 11752352 14753710 15180525 25818407 23392356 22858906 16990784

Sources: TALC MyCancerGenome TdgClinicalTrial JAX-CKB TEND COSMIC CIViC MyCancerGenomeClinicalTrial PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 28117434

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 26387812

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 27751729

Sources: CIViC

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: 21885287 23583911 21963305 20124951 19248971 12538485 28011623 27149458 20142593 19723655 16418310 12873999 11752352 14753710 16533791 25639617

Interaction Types & Directionality:

n/a

PMIDs:
24703573

Sources:
CIViC

Interaction Types & Directionality:

n/a

PMIDs:
27751729

Sources:
CIViC

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
None found

Sources:
MyCancerGenomeClinicalTrial

Interaction Types & Directionality:

n/a

PMIDs:
24633157

Sources:
CIViC

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
None found

Sources:
MyCancerGenomeClinicalTrial

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
29760553

Sources:
CIViC MyCancerGenomeClinicalTrial

Interaction Types & Directionality:

n/a

PMIDs:
29578538

Sources:
CIViC

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Clinical Status preclinical

Variant Effect gain-of-function

Pathway activation

PMIDs:
22261812 21690468 21642685 18421059 19861435 21969494 23375402 22357254 26772734 25239608 22439647 16638875 18955458 17545799 17367763 12873999 14753710 11752352 12748309 19164557 25594040 23582185 19248971

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

Interaction Types & Directionality:

n/a

PMIDs:
26309414

Sources:
CIViC

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
None found

Sources:
MyCancerGenomeClinicalTrial

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

combination therapy Cetuximab + Sunitinib

Indication/Tumor Type olfactory neuroblastoma

Response Type sensitive

PMIDs:
16849418 28447912 27149458 19248971 20696054 18541894 9681850 9839497 20847059 19255327 18073307 21455200 20368568 11351254 21422803 21470995 20943719 23056499 22025146 20065189 25157968

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

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type Advanced Solid Tumor

Response Type resistant

Approval Status Preclinical - Cell culture

PMIDs:
19366796 18955458 16638875 22718859 25157968 14645423 16954519 22745105 18794084 15928335 26130666 15146165 15685537 12949711 21482694 19755855

Sources:
TdgClinicalTrial JAX-CKB TEND DoCM COSMIC CIViC MyCancerGenomeClinicalTrial

Interaction Types & Directionality:

n/a

PMIDs:
21787417

Sources:
CIViC

Interaction Types & Directionality:

n/a

PMIDs:
27751729

Sources:
CIViC

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Trial Name Sutent

Novel drug target Established target

PMIDs:
26244574 24013576 20683446 19667267 19248971 27181063 21482694 14654525 12531805 15304385 11752352 14753710 15180525 25818407 23392356 22858906 16990784

Sources:
TALC MyCancerGenome TdgClinicalTrial JAX-CKB TEND COSMIC CIViC MyCancerGenomeClinicalTrial PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
28117434

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
26387812

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
27751729

Sources:
CIViC

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type Advanced Solid Tumor

Response Type sensitive

Approval Status Preclinical

PMIDs:
21885287 23583911 21963305 20124951 19248971 12538485 28011623 27149458 20142593 19723655 16418310 12873999 11752352 14753710 16533791 25639617

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

Interaction Types & Directionality:

n/a

Interaction Info:

Approval Status Preclinical - Pdx

Response Type predicted – sensitive

Indication/Tumor Type kidney cancer

PMIDs:
26487278 22105611

Sources:
JAX-CKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Trial Name Sutent

Novel drug target Established target

PMIDs:
29760553 16425993 15557593 14753710 12748309 12538485 19248971

Sources:
TALC MyCancerGenome TdgClinicalTrial TEND CIViC PharmGKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name Sutent

Novel drug target Established target

Notes

PMIDs:
23583911 26935927 20124951 19248971 17367763 14654525 21478036 24086736

Sources:
TALC DTC TdgClinicalTrial TEND MyCancerGenomeClinicalTrial PharmGKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name Sutent

Notes

PMIDs:
17367763 17296815 15688612 16685460 17605814 22015057 19248971

Sources:
TALC TdgClinicalTrial TEND MyCancerGenomeClinicalTrial PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
27561454