Drug Class Detail

Drug Class VEGFR Inhibitor (Pan)

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Drug Name Trade Name Synonyms Drug Classes Drug Description
Vandetanib Caprelsa ZD6474 ABL1 Inhibitor 4 EGFR Inhibitor (Pan) 38 RET Inhibitor 36 SRC Inhibitor 26 VEGFR Inhibitor (Pan) 29 Caprelsa (vandetanib) is a multi-tyrosine kinase inhibitor with activity against VEGFR, EGFR, RET, SRC, and ABL1 kinases, potentially resulting in decreased tumor growth (PMID: 25031937, PMID: 25490448). Caprelsa (vandetanib) is FDA approved for use in medullary thyroid cancer (FDA.gov).
ABT-348 ilorasertib AURK Inhibitor (Pan) 11 PDGFR Inhibitor (Pan) 27 VEGFR Inhibitor (Pan) 29 Ilorasertib (ABT-348) is an ATP-competitive multitargeted kinase inhibitor with activity towards Aurora kinases, and VEGFR, and PDGFR kinase families (PMID: 22935731).
Fruquintinib HMPL-013 VEGFR Inhibitor (Pan) 29 Fruquintinib (HMPL-013) binds and inhibits VEGFR receptors, 1,2 and 3, resulting in reduced cell proliferation and tumor growth (PMID: 25482937).
Bevacizumab Avastin VEGF Antibody 10 VEGFR Inhibitor (Pan) 29 Avastin (bevacizumab) is a monoclonal antibody that binds VEGF and inhibits binding to VEGFR, potentially resulting in decreased tumor growth (PMID: 15136787). Avastin (bevacizumab) is FDA approved for use in colorectal cancer, non-small cell lung cancer, glioblastoma, renal cell carcinoma, cervical carcinoma, and ovarian cancer, and in combination with carboplatin and paclitaxel in epithelial ovarian, fallopian tube, or primary peritoneal cancer (FDA.gov).
Pazopanib Votrient GW-786034 FGFR1 Inhibitor 21 FGFR2 Inhibitor 15 FGFR3 Inhibitor 12 KIT Inhibitor 48 PDGFR Inhibitor (Pan) 27 VEGFR Inhibitor (Pan) 29 Votrient (pazopanib) inhibits VEGFR-1, -2 and -3, KIT, and PDGFR, and FGFR1, 2, and 3, leading to decreased tumor angiogenesis and growth (PMID: 17620431, PMID: 23786770). Votrient (pazopanib) is approved for renal cell carcinoma and soft tissue sarcoma (FDA.gov).
Sulfatinib HMPL-012 FGFR1 Inhibitor 21 VEGFR Inhibitor (Pan) 29 HMPL-012 (Sulfatinib) is a dual VEGFR/FGFR1 inhibitor, which inhibits tumor growth (AACR; Mol Cancer Ther 2015;14(12 Suppl 2):Abstract nr A1).
Ponatinib Iclusig AP24534 BCR-ABL Inhibitor 23 DDR1 Inhibitor 8 DDR2 inhibitor 7 FGFR Inhibitor (Pan) 17 FLT3 Inhibitor 48 KIT Inhibitor 48 PDGFR-alpha Inhibitor 7 RET Inhibitor 36 SRC Inhibitor 26 VEGFR Inhibitor (Pan) 29 Iclusig (ponatinib) inhibits the Bcr-Abl fusion, and other tyrosine kinases, such as RET, DDR, VEGFR, FGFR, KIT, and FLT3 (PMID: 23526464, PMID: 25284748, PMID: 19878872). Iclusig (ponatinib) is FDA approved for chronic myeloid leukemia (CML) and Philadelphia chromosome positive acute lymphoblastic leukemia (Ph positive ALL) as well as ABL1 T315I CML and ABL1 T315I Ph positive ALL (FDA.gov).
Debio 0617B ABL Inhibitor (pan) 8 CSF1R Inhibitor 22 FLT3 Inhibitor 48 JAK Inhibitor (Pan) 8 KIT Inhibitor 48 PDGFR Inhibitor (Pan) 27 SRC Inhibitor 26 VEGFR Inhibitor (Pan) 29 Debio 0617B is a multi-kinase inhibitor of SRC, JAK, and ABL, the class III kinases, CSF1R, FLT3, KIT, and PDGFR, and the class V kinases, VEGFR 1/2/3, which may result in inhibition of Stat3 and Stat5 signaling, leading to inhibition of tumor cell growth and metastasis (PMID: 27439479).
Vorolanib X-82 PDGFR Inhibitor (Pan) 27 VEGFR Inhibitor (Pan) 29 Vorolanib (X-82) is a dual VEGFR/PDGFR inhibitor, which inhibits tumor angiogenesis and cell proliferation in tumors (Journal of Clinical Oncology 34, no. 15_suppl (May 20 2016) 2588-2588).
Tivozanib AV-951 VEGFR Inhibitor (Pan) 29 Tivozanib (AV-951) inhibits VEGFR1-3, which may result in decreased tumor angiogenesis and proliferation and increased cell death (PMID: 23788831).
BMS-690514 EGFR Inhibitor (Pan) 38 HER2 Inhibitor 20 VEGFR Inhibitor (Pan) 29 BMS-690514 is a pan-EGFR/VEGFR inhibitor, which may result in increased tumor cell apoptosis, and decreased tumor cell proliferation and angiogenesis (PMID: 21531814, PMID: 17616683).
Methylnaltrexone Relistor MNTX VEGFR Inhibitor (Pan) 29 Relistor (methylnaltrexone) is a mu-type opioid receptor inhibitor and is approved for constipation, but it has also been shown to inhibit VEGFRs and angiogenesis (PMID: 16820176).
BPR1J373 FLT3 Inhibitor 48 KIT Inhibitor 48 PDGFR Inhibitor (Pan) 27 RET Inhibitor 36 SRC Inhibitor 26 VEGFR Inhibitor (Pan) 29 BPR1J373 is a derivative of 5-phenylthiazol-2-ylamine-pyriminide that inhibits multiple tyrosine kinases including KIT, FLT3, VEGFR1, 2, 3, PDGFR-alpha, PDGFR-beta, RET, and SRC, and may result in anti-tumor activity (PMID: 27512117).
Regorafenib Stivarga BAY 73-4506 BRAF Inhibitor 18 CRAF Inhibitor 10 KIT Inhibitor 48 PDGFR Inhibitor (Pan) 27 RET Inhibitor 36 VEGFR Inhibitor (Pan) 29 VEGFR2 Inhibitor 34 Stivarga (regorafenib) is an inhibitor of several kinases including VEGFR, RET, KIT, PDGFR and RAF, thereby inhibiting tumor angiogenesis and tumor cell proliferation (PMID: 24756792). Stivarga (regorafenib) is FDA approved for colorectal cancer, hepatocellular carcinoma, and GIST (FDA.gov).
Nintedanib Ofev BIBF 1120|Vargatef FGFR Inhibitor (Pan) 17 PDGFR Inhibitor (Pan) 27 RET Inhibitor 36 VEGFR Inhibitor (Pan) 29 Ofev (nintedanib) is a triple angiokinase inhibitor that acts by blocking VEGFR, FGFR, RET, and PDGFR, thereby preventing tumorigenesis (PMID: 24947258, PMID: 24561444). Ofev (nintedanib) is FDA approved for use in patients with idiopathic pulmonary fibrosis (FDA.gov).
Lucitanib E-3810|AL3810 DDR1 Inhibitor 8 DDR2 inhibitor 7 FGFR1 Inhibitor 21 FGFR2 Inhibitor 15 PDGFR-alpha Inhibitor 7 VEGFR Inhibitor (Pan) 29 Lucitanib (E-3810) is a multi-tyrosine kinase receptor inhibitor of VEGFR 1-3, DDR2, PDGFRA, and FGFR1-2, that may inhibit tumor angiogenesis, prevent tumor cell proliferation, and induce tumor cell death (PMID: 27988457, PMID: 24696502).
Lenvatinib Lenvima E7080 FGFR Inhibitor (Pan) 17 KIT Inhibitor 48 PDGFR Inhibitor (Pan) 27 RET Inhibitor 36 VEGFR Inhibitor (Pan) 29 Lenvima (lenvatinib) inhibits VEGFR, FGFR, PDGFR, KIT, and RET, and suppresses cell proliferation and angiogenesis (PMID: 21781317, PMID: 25295214, PMID: 17943726). Lenvima (lenvatinib) is FDA approved for use in patients with radioactive iodine-refractory differentiated thyroid cancer, unresectable hepatocellular carcinoma, and in combination with Afinitor (everolimus) for renal cell carcinoma (FDA.gov).
Motesanib AMG 706 KIT Inhibitor 48 PDGFR Inhibitor (Pan) 27 RET Inhibitor 36 VEGFR Inhibitor (Pan) 29 Motesanib (AMG 706) is a multi-kinase inhibitor, which inhibits vascular endothelial growth factor (VEGFR), platelet-derived growth factor (PDGFR), Kit, and Ret receptors, thereby inhibiting angiogenesis and inducing tumor regression (PMID: 16951187, PMID: 21422803).
ZK 304709 CDK1 Inhibitor 12 CDK2 Inhibitor 16 CDK4 Inhibitor 12 CDK7 Inhibitor 9 CDK9 Inhibitor 11 PDGFR-beta Inhibitor 13 VEGFR Inhibitor (Pan) 29 ZK 304709 is a small molecule kinase inhibitor of CDKs 1, 2, 4, 7, and 9, VEGFR-1,2,3, and PDGFR-beta, which may result in inhibition of both the cell cycle and angiogenesis (PMID: 18653327).
Glesatinib MGCD265 AXL Inhibitor 24 MET Inhibitor 50 RON Inhibitor 10 VEGFR Inhibitor (Pan) 29 Glesatinib (MGCD265) inhibits several tyrosine kinases including MET, MST1R (RON), and AXL, as well as VEGFR1-3, and TIE2, which may result in decreased tumor growth (PMID: 25806189, PMID: 26555154).
Dovitinib TKI258|CHIR-258 CSF1R Inhibitor 22 FGFR Inhibitor (Pan) 17 FLT3 Inhibitor 48 KIT Inhibitor 48 PDGFR Inhibitor (Pan) 27 VEGFR Inhibitor (Pan) 29 Dovitinib (TKI258) targets multiple receptor tyrosine kinases including Flt3, c-Kit, CSF1R, FGFR 1-4, VEGFR 1-3, and PDGFR alpha and beta, potentially resulting in decreased tumor growth (PMID: 15598814, PMID: 25219510, PMID: 23658459, PMID: 16033847).
Aflibercept Zaltrap AVE 0005|Eylea VEGF Antibody 10 VEGFR Inhibitor (Pan) 29 Zaltrap (aflibercept) is comprised of human IgG fused to the extracellular domains of VEGFR1 and VEGFR2, which binds VEGF to inhibit tumor angiogenesis and metastasis (NCI Drug Dictionary). Zaltrap (aflibercept) is FDA approved in patients with metastatic colorectal cancer (FDA.gov).
SU14813 FLT3 Inhibitor 48 KIT Inhibitor 48 PDGFR Inhibitor (Pan) 27 VEGFR Inhibitor (Pan) 29 SU14813 is a multi-kinase inhibitor with activity against VEGFR1-3, PDGFRA, PDGFRB, KIT, and FLT3, which potentially results in decreased tumor angiogenesis and growth (PMID: 16891463, PMID: 20605934).
Axitinib Inlyta AG-013736 KIT Inhibitor 48 PDGFR Inhibitor (Pan) 27 VEGFR Inhibitor (Pan) 29 Inlyta (axitinib) inhibits the VEGFRs, PDGFR, and KIT, potentially resulting in decreased angiogenesis and reduced tumor growth (PMID: 16027439, PMID: 25709499). Inlyta (axitinib) is approved for renal cell carcinoma (FDA.gov).
Linifanib ABT-869|AL-39324 CSF1R Inhibitor 22 FLT3 Inhibitor 48 KIT Inhibitor 48 PDGFR-beta Inhibitor 13 VEGFR Inhibitor (Pan) 29 Linifanib (ABT-869) is a receptor tyrosine kinase inhibitor with specificity against FLT1 (VEGFR1), CSF-1R, KDR (VEGFR2), FLT3, and KIT, which may result in inhibition of cell proliferation and tumor growth, and tumor regression (PMID: 16648571).
SU5402 FGFR1 Inhibitor 21 FGFR2 Inhibitor 15 FGFR3 Inhibitor 12 VEGFR Inhibitor (Pan) 29 SU5402 is an ATP-competitive inhibitor of FGFR1, FGFR2, FGFR3, and VEGFR, which may inhibit cell proliferation and reduce cell migration (PMID: 21119661, PMID: 23420874, PMID: 18852144).
Vatalanib CGP-79787|PTK787|ZK 222584 KIT Inhibitor 48 PDGFR Inhibitor (Pan) 27 VEGFR Inhibitor (Pan) 29 Vatalanib inhibits VEGFR1-3, PDGFRs, and KIT, potentially resulting in decreased tumor angiogenesis and growth (PMID: 23700288, PMID: 12124335).
MGCD516 Sitravatinib AXL Inhibitor 24 DDR1 Inhibitor 8 DDR2 inhibitor 7 KIT Inhibitor 48 MET Inhibitor 50 RET Inhibitor 36 Trk Receptor Inhibitor (Pan) 21 VEGFR Inhibitor (Pan) 29 MGCD516 (Sitravatinib) inhibits several receptor tyrosine kinases including AXL, MET, KIT, VEGFR1-3, RET family members, TRK family members, DDR, and Eph family members, resulting in abrogation of downstream signaling and decreased cell proliferation in tumors overexpressing the target proteins (PMID: 26675259).
Chiauranib CS2164 Aurkb Inhibitors 17 CSF1R Inhibitor 22 KIT Inhibitor 48 PDGFR-alpha Inhibitor 7 VEGFR Inhibitor (Pan) 29 Chiauranib (CS2164) is a multi-kinase inhibitor that inhibits AURKB, CSF-1R, VEGFRs, KIT, and PDGFRA, resulting in decreased tumor growth and angiogenesis (PMID: 28004478).
Molecular Profile Protein Effect Treatment Approaches
KDR Q472H gain of function VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
KDR D717V unknown VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL inact mut loss of function mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL S65W loss of function mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL L116fs loss of function - predicted mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL P86H loss of function mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL L158P loss of function mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL H115R loss of function - predicted mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL Q96* loss of function - predicted mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL R82P loss of function mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL S80I loss of function - predicted mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
KDR act mut gain of function VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL C162W loss of function - predicted mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL P154L loss of function mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL S65L loss of function mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL S183L loss of function mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL D126N loss of function - predicted mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL N90I loss of function - predicted mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL P81S loss of function mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
KDR A1065T gain of function - predicted VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL V62fs loss of function - predicted mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL Y98N loss of function mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL Q132fs loss of function - predicted mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL F148fs loss of function - predicted mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL H110Q unknown mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL R167Q loss of function mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL Y112H loss of function mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL Y98H loss of function - predicted mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL S68fs loss of function - predicted mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL loss loss of function mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL C162F loss of function mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL H115Q loss of function - predicted mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL V155fs loss of function - predicted mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL C77* loss of function - predicted mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL G114R loss of function - predicted mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL S68* loss of function - predicted mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL W117C loss of function mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL L184P loss of function - predicted mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL R167W loss of function - predicted mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL N131fs loss of function - predicted mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL S80R loss of function - predicted mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL N78S loss of function - predicted mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL S111N loss of function mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL R161G loss of function - predicted mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL V130F loss of function - predicted mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL V74G loss of function - predicted mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL R161P loss of function mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL W88* loss of function - predicted mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL L158fs loss of function - predicted mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL R79P loss of function - predicted mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL S111R loss of function mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor