Drug Class Detail

Drug Class PDGFR Inhibitor (Pan)

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Drug Name Trade Name Synonyms Drug Classes Drug Description
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).
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).
CP-673451 PDGFR Inhibitor (Pan) 27 CP-673451 is an inhibitor of PDGFR kinase, which may inhibit tumor angiogenesis and tumor growth (PMID: 15705896).
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).
Crenolanib CP-868596 FLT3 Inhibitor 48 PDGFR Inhibitor (Pan) 27 Crenolanib is a type III receptor tyrosine kinase inhibitor of PDGFR-alpha/beta and FLT3, which results in inhibition of downstream signaling and prevents growth in tumor cells (PMID: 22745105).
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).
GZD856 PDGFR Inhibitor (Pan) 27 GZD856 inhibits PDGFRA and PDGFRB, potentially resulting in decreased tumor growth (PMID: 26940138).
Dasatinib Sprycel BMS-354825 ABL Inhibitor (pan) 8 BCR-ABL Inhibitor 23 BTK inhibitor 20 CSF1R Inhibitor 22 DDR1 Inhibitor 8 DDR2 inhibitor 7 KIT Inhibitor 48 PDGFR Inhibitor (Pan) 27 SRC Inhibitor 26 TNK2 Inhibitor 6 Sprycel (dasatinib) is an inhibitor of the SRC-family of protein kinases, BCR-ABL, and ABL, and has additional activity against other kinases including KIT, DDR1/2, PDGFRA/B, and EPHA2, which prevents cell growth (PMID: 25709401, PMID: 25284748, PMID: 18797457). Sprycel (dasatinib) is FDA approved for both Philadelphia chromosome positive adult and pediatric chronic myelogenous leukemia and adult acute lymphoblastic leukemia (FDA.gov).
Sunitinib Sutent SU011248 CSF1R Inhibitor 22 FLT3 Inhibitor 48 KIT Inhibitor 48 PDGFR Inhibitor (Pan) 27 RET Inhibitor 36 VEGFR2 Inhibitor 34 Sutent (sunitinib) inhibits KDR (VEGFR2), PDGFR, c-KIT, FLT3, RET, and CSF1R, thereby inhibiting angiogenesis and cell proliferation (NCI Drug Dictionary; PMID: 25085632). Sutent (sunitinib) is approved for neuroendocrine tumors of the pancreas, advanced renal cell carcinoma, and GIST (FDA.gov).
Masitinib AB1010 KIT Inhibitor 48 PDGFR Inhibitor (Pan) 27 Masitinib (AB1010) inhibits several receptor tyrosine kinases including c-KIT, PDGFR, and LYN, which may result in inhibition of cell proliferation (PMID: 19789626).
AG1295 AG-1295 FLT3 Inhibitor 48 KIT Inhibitor 48 PDGFR Inhibitor (Pan) 27 AG1295 inhibits the tyrosine kinase activity of PDGFRA, PDGFRB, KIT, and FLT3, which may inhibit growth and promote apoptosis in cancer cells (PMID: 11468194, PMID: 7954456).
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).
MK2461 MET Inhibitor 50 PDGFR Inhibitor (Pan) 27 RON Inhibitor 10 VEGFR1 Inhibitor 4 MK2461 inhibits wild-type and activated forms of MET, and also has activity against VEGFR1 (FLT1), MST1R (RON), and PDGFR resulting in inhibition of downstream signaling and decreased tumor growth (PMID: 20145145).
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).
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).
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).
Flumatinib HH-GV678 BCR-ABL Inhibitor 23 KIT Inhibitor 48 PDGFR Inhibitor (Pan) 27 Flumatinib inhibits KIT, PDGFR, and BCR-ABL, potentially resulting in decreased tumor cell proliferation (NCI Drug Dictionary).
Nilotinib Tasigna AMN-107 ABL Inhibitor (pan) 8 BCR-ABL Inhibitor 23 CSF1R Inhibitor 22 DDR1 Inhibitor 8 DDR2 inhibitor 7 KIT Inhibitor 48 PDGFR Inhibitor (Pan) 27 Tasigna (nilotinib) inhibits several tyrosine kinases including BCR-ABL, PDGFR, KIT, DDR and CSF-1R, potentially resulting in reduced tumor cell proliferation (PMID: 21419934, PMID: 25284748). Tasigna (nilotinib) is FDA approved for use in patients with Ph+ chronic myeloid leukemia (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).
PP-121 ABL Inhibitor (pan) 8 mTOR Inhibitor 48 PDGFR Inhibitor (Pan) 27 SRC Inhibitor 26 VEGFR2 Inhibitor 34 PP-121 inhibits several types of kinases including, PDGFR, Hck, mTOR, KDR (VEGFR2), Src and Abl to prevent cell proliferation (PMID: 24867098).
AGL2043 AGL-2043 FLT3 Inhibitor 48 KIT Inhibitor 48 PDGFR Inhibitor (Pan) 27 AGL2043 inhibits the tyrosine kinase activity of PDGFRA, PDGFRB, KIT, and FLT3, which may inhibit growth and promote apoptosis in cancer (PMID: 12670652).
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).
AG1296 AG-1296 KIT Inhibitor 48 PDGFR Inhibitor (Pan) 27 AG1296 is a tyrphostin which binds and inhibits PDGFR and c-KIT which may reduce proliferation and tumor growth (PMID: 7954456, PMID: 15150607).
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).
Imatinib mesylate Gleevec CGP-57148B|STI571 ABL Inhibitor (pan) 8 BCR-ABL Inhibitor 23 CSF1R Inhibitor 22 KIT Inhibitor 48 PDGFR Inhibitor (Pan) 27 Gleevec (imatinib mesylate) is a multi-target inhibitor of c-Kit, Pdgfr, and Bcr-Abl (NCI Drug Dictionary). Gleevec (imatinib mesylate) is FDA approved for c-KIT positive GIST and dermatofibrosarcoma protuberans, Philadelphia chromosome positive chronic myeloid leukemia, and FIP1L1-PDGFRA positive chronic eosinophilic leukemia (FDA.gov).
Molecular Profile Protein Effect Treatment Approaches
PDGFRA R841K gain of function - predicted PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA Y555C gain of function - predicted PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA V658A gain of function - predicted PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA N659S gain of function PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA C450_K451insMIEWMI gain of function PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA H650Q gain of function PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA V536E gain of function PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA amp no effect PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA R841_D842delinsKI gain of function - predicted PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA D846Y gain of function - predicted PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA S566_E571delinsR gain of function - predicted PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA N659K gain of function - predicted PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA G853D 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
PDGFRA D842_M844del gain of function - predicted PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA V561A gain of function - predicted PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA Y375_K455del gain of function PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA R748G gain of function PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA Y849S gain of function PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA V544_L545insAVLVLLVIVIISLI gain of function PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA N848K gain of function - predicted PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA P345S gain of function - predicted PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA E311_K312del gain of function PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA I843_D846del gain of function - predicted PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA M844_S847del gain of function - predicted PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA H845Y gain of function PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA V561D gain of function PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA P577T gain of function - predicted PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA I843_M844del gain of function - predicted PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA D842_D846del gain of function - predicted PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA D842I gain of function - predicted PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA D842Y gain of function - predicted PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA P577S gain of function - predicted PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA H845_N848delinsP gain of function - predicted PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA Y288C gain of function - predicted PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA I843del gain of function - predicted PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA act mut gain of function PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA C456_R481del gain of function PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA D842V gain of function PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor Avapritinib
PDGFRA V561_I562insER gain of function - predicted PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA D842_H845del gain of function - predicted PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor
PDGFRA D842_I843delinsIM gain of function - predicted PDGFR Inhibitor (Pan) PDGFR-alpha Inhibitor