Drug Class Detail

Drug Class FGFR3 Inhibitor

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Drug Name Trade Name Synonyms Drug Classes Drug Description
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).
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).
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).
R3Mab FGFR3 Inhibitor 12 R3Mab is a monoclonal antibody, which specifically targets FGFR3 to block signaling and tumor growth (PMID: 23657946, PMID: 19381019)
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).
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).
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).
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).
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).
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).
Molecular Profile Protein Effect Treatment Approaches
FGFR3 K650N gain of function - predicted FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 G382D gain of function - predicted FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 act mut gain of function FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 C228R gain of function - predicted FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 Y647C gain of function - predicted FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 R669Q gain of function - predicted FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 amp no effect FGFR Inhibitor (Pan) FGFR3 Antibody FGFR3 Inhibitor
FGFR3 G370C gain of function FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 S371C gain of function FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 R669G gain of function FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 K650E gain of function - predicted FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 G382R gain of function FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 R200C gain of function FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 D641G gain of function FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 N540S gain of function - predicted FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 V555M gain of function FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 D641N gain of function FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 V788M gain of function - predicted FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3-BAIAP2L1 gain of function FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 R124W gain of function - predicted FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 I538V gain of function - predicted FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 Y375C gain of function FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 K650Q gain of function - predicted FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 R248C gain of function FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 G380R gain of function FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 K650T gain of function - predicted FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3-TACC3 gain of function FGFR Inhibitor (Pan) FGFR3 Inhibitor U0126
FGFR3 A391E gain of function FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 over exp no effect FGFR Inhibitor (Pan) FGFR3 Antibody FGFR3 Inhibitor
FGFR3 D786N gain of function - predicted FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 V50I gain of function - predicted FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 G372C gain of function FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 N540K gain of function FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 K652E gain of function - predicted FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 S249C gain of function FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 Y373C gain of function FGFR Inhibitor (Pan) FGFR3 Inhibitor
FGFR3 K650M gain of function FGFR Inhibitor (Pan) FGFR3 Inhibitor