Drug Class Detail

Drug Class PDGFR-alpha Inhibitor

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Drug Name Trade Name Synonyms Drug Classes Drug Description
Avapritinib BLU-285 KIT Inhibitor 48 PDGFR-alpha Inhibitor 7 Avapritinib (BLU-285) is a selective inhibitor of PDGFRA D842V and KIT exon 17 mutants, including KIT D816V, potentially resulting in decreased tumor growth (AACR; 2015. Abstract nr 791).
Ponatinib Iclusig AP24534 BCR-ABL Inhibitor 23 DDR1 Inhibitor 8 DDR2 inhibitor 7 FGFR Inhibitor (Pan) 18 FLT3 Inhibitor 48 KIT Inhibitor 48 PDGFR-alpha Inhibitor 7 RET Inhibitor 36 SRC Inhibitor 26 VEGFR Inhibitor (Pan) 30 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).
Quizartinib AC220 FLT3 Inhibitor 48 KIT Inhibitor 48 PDGFR-alpha Inhibitor 7 RET Inhibitor 36 Quizartinib (AC220) targets both wild-type and mutant FLT3 containing activating internal tandem duplications, as well as PDGFRA, RET, and KIT, which may induce apoptosis and inhibit tumor growth (PMID: 19654408, PMID: 23497317).
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).
Chiauranib CS2164 Aurkb Inhibitors 17 CSF1R Inhibitor 22 KIT Inhibitor 48 PDGFR-alpha Inhibitor 7 VEGFR Inhibitor (Pan) 30 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).
Amuvatinib MP470|HPK56 AXL Inhibitor 24 FLT3 Inhibitor 48 KIT Inhibitor 48 MET Inhibitor 50 PDGFR-alpha Inhibitor 7 RET Inhibitor 36 Amuvatinib (MP470) is a multi-kinase inhibitor, with activity against KIT, MET, AXL, RET, FLT3, and PDGFR-alpha, that also inhibits Rad51 induction, which may enhance the efficacy of chemotherapeutic agents (PMID: 17325667, PMID: 21903282, PMID: 20563581).
DCC-2618 KIT Inhibitor 48 PDGFR-alpha Inhibitor 7 DCC-2618 is a dual inhibitor of KIT and PDGFRa, resulting in growth inhibition and anti-tumor effects (PMID: 29439183).
Molecular Profile Protein Effect Treatment Approaches
PDGFRA N848K gain of function - predicted PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA N659K gain of function - predicted PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA R748G gain of function PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA R841_D842delinsKI gain of function - predicted PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA M844_S847del gain of function - predicted PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA D846Y gain of function - predicted PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA H845Y gain of function PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA V561A gain of function - predicted PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA Y849S gain of function PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA amp no effect PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA P577T gain of function - predicted PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA Y555C gain of function - predicted PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA D842I gain of function - predicted PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA S566_E571delinsR gain of function - predicted PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA D842V gain of function PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor Avapritinib
PDGFRA P345S gain of function - predicted PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA V536E gain of function PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA C456_R481del gain of function PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA E311_K312del gain of function PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA G853D gain of function - predicted PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA D842Y gain of function - predicted PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA H650Q gain of function PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA P577S gain of function - predicted PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA C450_K451insMIEWMI gain of function PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA H845_N848delinsP gain of function - predicted PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA V561_I562insER gain of function - predicted PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA V544_L545insAVLVLLVIVIISLI gain of function PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA I843_D846del gain of function - predicted PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA Y375_K455del gain of function PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA V658A gain of function - predicted PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA D842_D846del gain of function - predicted PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA V561D gain of function PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA R841K gain of function - predicted PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA I843_M844del gain of function - predicted PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA I843del gain of function - predicted PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA Y288C gain of function - predicted PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA D842_M844del gain of function - predicted PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA D842_I843delinsIM gain of function - predicted PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA N659S gain of function PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA act mut gain of function PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA D842_H845del gain of function - predicted PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA C456_N468del gain of function PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA Y849C gain of function - predicted PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor