Drug Class Detail

Drug Class FGFR2 Inhibitor

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Drug Name Trade Name Synonyms Drug Classes Drug Description
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).
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).
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).
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).
TAK-901 Aurkb Inhibitors 17 FGFR2 Inhibitor 15 FLT3 Inhibitor 48 TAK-901 is a selective inhibitor of Aurora B kinase, FLT3, and FGFR2, and has demonstrated anti-tumor activity in several cancer models (PMID: 23358665).
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).
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).
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).
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).
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).
PHM16 FAK inhibitor 14 FGFR2 Inhibitor 15 PHM16 is an ATP competitive inhibitor of PTK2 (FAK) and FGFR2, which may result in decreased cell adhesion, inhibition of cell growth, and induction of apoptosis (PMID: 24657306).
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).
Molecular Profile Protein Effect Treatment Approaches
FGFR2 E566G gain of function FGFR Inhibitor (Pan) FGFR2 Inhibitor
FGFR2-AHCYL1 gain of function FGFR Inhibitor (Pan) FGFR2 Inhibitor
FGFR2 L618M gain of function FGFR Inhibitor (Pan) FGFR2 Inhibitor
FGFR2-CCDC6 gain of function FGFR Inhibitor (Pan) FGFR2 Inhibitor
FGFR2 K641N gain of function FGFR Inhibitor (Pan) FGFR2 Inhibitor
FGFR2 I548V gain of function FGFR Inhibitor (Pan) FGFR2 Inhibitor
FGFR2 K641R gain of function FGFR Inhibitor (Pan) FGFR2 Inhibitor
FGFR2 G663E gain of function FGFR Inhibitor (Pan) FGFR2 Inhibitor
FGFR2 V564F gain of function - predicted FGFR Inhibitor (Pan) FGFR2 Inhibitor
FGFR2 K660N gain of function FGFR Inhibitor (Pan) FGFR2 Inhibitor
FGFR2 N549K gain of function FGFR Inhibitor (Pan) FGFR2 Inhibitor
FGFR2 W290C gain of function FGFR Inhibitor (Pan) FGFR2 Inhibitor
FGFR2 K659E gain of function FGFR Inhibitor (Pan) FGFR2 Inhibitor
FGFR2 Y375C gain of function FGFR Inhibitor (Pan) FGFR2 Inhibitor
FGFR2 C342Y gain of function FGFR Inhibitor (Pan) FGFR2 Inhibitor
FGFR2 amp no effect FGFR Inhibitor (Pan) FGFR2 Antibody FGFR2 Inhibitor
FGFR2 T341P gain of function FGFR Inhibitor (Pan) FGFR2 Inhibitor
FGFR2 N550K gain of function FGFR Inhibitor (Pan) FGFR2 Inhibitor
FGFR2 S267_D273dup gain of function FGFR Inhibitor (Pan) FGFR2 Inhibitor
FGFR2 D101Y gain of function - predicted FGFR Inhibitor (Pan) FGFR2 Inhibitor
FGFR2 E565A gain of function FGFR Inhibitor (Pan) FGFR2 Inhibitor
FGFR2 V565I gain of function FGFR Inhibitor (Pan) FGFR2 Inhibitor
FGFR2-BICC1 gain of function FGFR Inhibitor (Pan) FGFR2 Inhibitor
FGFR2 P253R gain of function FGFR Inhibitor (Pan) FGFR2 Inhibitor
FGFR2 E565G gain of function FGFR Inhibitor (Pan) FGFR2 Inhibitor
FGFR2 L617F gain of function - predicted FGFR Inhibitor (Pan) FGFR2 Inhibitor
FGFR2 R203C gain of function FGFR Inhibitor (Pan) FGFR2 Inhibitor
FGFR2 C383R gain of function - predicted FGFR Inhibitor (Pan) FGFR2 Inhibitor
FGFR2 C382R gain of function FGFR Inhibitor (Pan) FGFR2 Inhibitor
FGFR2 L761Tfs*55 unknown FGFR Inhibitor (Pan) FGFR2 Inhibitor
FGFR2 S372C gain of function - predicted FGFR Inhibitor (Pan) FGFR2 Inhibitor
FGFR2 N549H gain of function FGFR Inhibitor (Pan) FGFR2 Inhibitor
FGFR2 M536I gain of function FGFR Inhibitor (Pan) FGFR2 Inhibitor
FGFR2 over exp no effect FGFR Inhibitor (Pan) FGFR2 Inhibitor GSK3052230
FGFR2 N550H gain of function FGFR Inhibitor (Pan) FGFR2 Inhibitor
FGFR2 V564I gain of function - predicted FGFR Inhibitor (Pan) FGFR2 Inhibitor
FGFR2 E566A gain of function - predicted FGFR Inhibitor (Pan) FGFR2 Inhibitor
FGFR2 K659N gain of function FGFR Inhibitor (Pan) FGFR2 Inhibitor
FGFR2 K526E gain of function - predicted FGFR Inhibitor (Pan) FGFR2 Inhibitor
FGFR2 R678G gain of function FGFR Inhibitor (Pan) FGFR2 Inhibitor
FGFR2 K660E gain of function FGFR Inhibitor (Pan) FGFR2 Inhibitor
FGFR2 N550S gain of function FGFR Inhibitor (Pan) FGFR2 Inhibitor
FGFR2 - TACC3 gain of function FGFR Inhibitor (Pan) FGFR2 Inhibitor
FGFR2 K525E gain of function FGFR Inhibitor (Pan) FGFR2 Inhibitor
FGFR2 N550T gain of function FGFR Inhibitor (Pan) FGFR2 Inhibitor
FGFR2 N549T gain of function FGFR Inhibitor (Pan) FGFR2 Inhibitor
FGFR2 F276C gain of function FGFR Inhibitor (Pan) FGFR2 Inhibitor
FGFR2 Y376C gain of function - predicted FGFR Inhibitor (Pan) FGFR2 Inhibitor
FGFR2 M538I gain of function FGFR Inhibitor (Pan) FGFR2 Inhibitor
FGFR2 V564L gain of function - predicted FGFR Inhibitor (Pan) FGFR2 Inhibitor
FGFR2 W290_I291delinsC gain of function FGFR Inhibitor (Pan) FGFR2 Inhibitor
FGFR2 act mut gain of function FGFR Inhibitor (Pan) FGFR2 Inhibitor
FGFR2 S252W gain of function FGFR Inhibitor (Pan) FGFR2 Inhibitor GSK3052230