Drug Class Detail

Drug Class FGFR1 Inhibitor

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Drug Name Trade Name Synonyms Drug Classes Drug Description
AZD4547 FGFR1 Inhibitor 21 FGFR2 Inhibitor 15 FGFR3 Inhibitor 12 AZD4547 selectively binds and inhibits FGFR1, 2, and 3, which may result in the inhibition of FGFR-mediated signal transduction pathways and inhibition of tumor cell proliferation (PMID: 22369928).
Brivanib BMS-540215 FGFR1 Inhibitor 21 VEGFR1 Inhibitor 4 VEGFR2 Inhibitor 34 Brivanib (BMS-540215) selectively binds and inhibits KDR (VEGFR2), while demonstrating moderate activity against VEGFR1 and FGFR1, which inhibits tumor angiogenesis, tumor cell growth, and induces tumor regression (PMID: 18829493, PMID: 16570908).
Lucitanib E-3810|AL3810 DDR1 Inhibitor 8 DDR2 inhibitor 7 FGFR1 Inhibitor 21 FGFR2 Inhibitor 15 PDGFR-alpha Inhibitor 7 VEGFR Inhibitor (Pan) 30 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).
SU11652 FGFR1 Inhibitor 21 KIT Inhibitor 48 PDGFR-beta Inhibitor 13 VEGFR2 Inhibitor 34 SU11652 is an inhibitor of multiple tyrosine kinase receptors including Pdgfr-beta, Kdr (Vegfr2), Fgfr1, and Kit, which blocks pathway activation, promotes cell cycle arrest, and induces apoptosis of tumor cells (PMID: 12091352, PMID: 23216927).
Derazantinib ARQ 087 FGFR1 Inhibitor 21 FGFR2 Inhibitor 15 KIT Inhibitor 48 Derazantinib (ARQ 087) is an ATP-competitive multi-kinase inhibitor with activity against Fgfr 1/2, FGFR fusions, Arg, Lck, and Kit, which prevents cell proliferation and angiogenesis (PMID: 27627808).
Pemigatinib INCB54828|INCB054828 FGFR1 Inhibitor 21 FGFR2 Inhibitor 15 FGFR3 Inhibitor 12 Pemigatinib (INCB054828) is a fibroblast growth factor receptor (FGFR) inhibitor that blocks FGFR1/2/3 signaling, which results in growth inhibition in tumor cells (Ann Oncol, 29 (suppl 8), October 2018, abstract 756P).
Danusertib PHA-739358 ABL1 Inhibitor 4 AURK Inhibitor (Pan) 11 BCR-ABL Inhibitor 23 FGFR1 Inhibitor 21 RET Inhibitor 36 TrkA Receptor Inhibitor 7 Danusertib (PHA-739358) is a pan-Aurora kinase with additional activity against ABL, FGFR1, RET, TRKA, and BCR-ABL, including the T315I mutant (PMID: 20072840, PMID: 18089710).
Pazopanib Votrient GW-786034 FGFR1 Inhibitor 21 FGFR2 Inhibitor 15 FGFR3 Inhibitor 12 KIT Inhibitor 48 PDGFR Inhibitor (Pan) 27 VEGFR Inhibitor (Pan) 30 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).
PD173074 FGFR1 Inhibitor 21 FGFR3 Inhibitor 12 FGFR4 Inhibitor 7 VEGFR2 Inhibitor 34 PD173074 is an ATP-competitive inhibitor of FGFR1, FGFR3, FGFR4, and KDR (VEGFR2), which may reduce proliferation and induce apoptosis in cancer cells (PMID: 9774334, PMID: 24126887, PMID: 14715624).
Orantinib SU6668|TSU-68 FGFR1 Inhibitor 21 KIT Inhibitor 48 PDGFR-beta Inhibitor 13 VEGFR2 Inhibitor 34 Orantinib (SU6668) inhibits several receptor tyrosine kinases KDR, PDGFRB, FGFR1, and KIT, thereby resulting in tumor growth inhibition (PMID: 17367541, PMID: 16144927).
Sulfatinib HMPL-012 FGFR1 Inhibitor 21 VEGFR Inhibitor (Pan) 30 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).
AZ8010 AZ12908010 FGFR1 Inhibitor 21 FGFR2 Inhibitor 15 FGFR3 Inhibitor 12 AZ12908010 (AZ8010) binds and inhibits FGFR1, 2, and 3, which may result in the inhibition of FGFR mediated signal transduction pathways and inhibition of tumor cell proliferation (PMID: 22869148).
ENMD-2076 Aurka Inhibitors 23 FGFR1 Inhibitor 21 FGFR2 Inhibitor 15 FLT3 Inhibitor 48 RET Inhibitor 36 VEGFR2 Inhibitor 34 ENMD-2076 has selective inhibitory activity against Aurora kinase A and FLT3, with reduced potency against RET, KDR (VEGFR2), FGFR1, and FGFR2, preventing angiogenesis and decreasing cell proliferation (PMID: 21177375, PMID: 22921155).
KW-2449 ABL Inhibitor (pan) 8 Aurka Inhibitors 23 FGFR1 Inhibitor 21 FLT3 Inhibitor 48 KW-2449 is a multikinase inhibitor with activity against FLT3, FLT3 D385Y, ABL1, ABL1 T315I, FGFR1, and AURKA, which may inhibit cancer cell proliferation and tumor growth (PMID: 19541823).
SPP86 FGFR1 Inhibitor 21 FGFR2 Inhibitor 15 RET Inhibitor 36 YES Inhibitor 2 SPP86 is a multi-kinase inhibitor with activity against RET, EPHA1, FGFR1, FGFR2, FLT4, LCK, and YES, which may reduce proliferation and induce apoptosis in cancer cells (PMID: 25409876).
SU5402 FGFR1 Inhibitor 21 FGFR2 Inhibitor 15 FGFR3 Inhibitor 12 VEGFR Inhibitor (Pan) 30 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).
E7090 FGFR1 Inhibitor 21 FGFR2 Inhibitor 15 FGFR3 Inhibitor 12 E7090 is a selective inhibitor of FGFR1, FGFR2, and FGFR3, which may result in inhibition of cell proliferation and antitumor activity (PMID: 27535969).
Debio 1347 CH5183284|FF284|debiopharm 1347 FGFR1 Inhibitor 21 FGFR2 Inhibitor 15 FGFR3 Inhibitor 12 Debio 1347 inhibits FGFR-1, -2, and -3, resulting in decreased downstream signaling, and potentially leading to reduced tumor cell proliferation and angiogenesis, and increased cell death in FGFR-overexpressing tumor cells (NCI Drug Dictionary).
S-49076 S49076 AXL Inhibitor 24 FGFR1 Inhibitor 21 FGFR2 Inhibitor 15 FGFR3 Inhibitor 12 MET Inhibitor 50 S-49076 is a multi-kinase inhibitor that inhibits wild-type and mutant forms of MET and FGFR1/2, as well as FGFR3, AXL, and MER, resulting in decreased downstream signaling, and potentially resulting in decreased tumor growth (PMID: 23804704).
XL999 FGFR1 Inhibitor 21 FGFR3 Inhibitor 12 FLT3 Inhibitor 48 KIT Inhibitor 48 PDGFR-beta Inhibitor 13 RET Inhibitor 36 SRC Inhibitor 26 VEGFR2 Inhibitor 34 XL999 inhibits multiple tyrosine kinases including VEGFR2/KDR, FGFR1/3, PDGFR-beta, FLT3, RET, KIT, and SRC, which can result in anti-tumor activity (J Clin Oncol, 25:18s, 2007 (suppl;abstr 3591), PMID: 19581523).
EBI-907 BRAF Inhibitor 18 FGFR1 Inhibitor 21 FGFR2 Inhibitor 15 FGFR3 Inhibitor 12 KIT Inhibitor 48 PDGFR-beta Inhibitor 13 RET Inhibitor 36 EBI-907 is a multi-kinase inhibitor that inhibits BRAF V600E, FGFR1-3, RET, KIT, and PDGFRb, which results in tumor growth inhibition (PMID: 26810733).