Drug Class Detail

Drug Class RET Inhibitor

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Drug Name Trade Name Synonyms Drug Classes Drug Description
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).
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).
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).
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).
SAR302503 Fedratinib TG101348 FLT3 Inhibitor 48 JAK2 Inhibitor - ATP competitive 14 RET Inhibitor 36 Fedratinib (SAR302503) binds and inhibits JAK2, FLT3, and RET kinases, which may inhibit cell proliferation and tumor growth (PMID: 17541402).
LOXO-292 RET Inhibitor 36 LOXO-292 is an inhibitor of RET, specifically targeting RET mutations and fusions, and may block the growth of cells with Ret activity (NCI Drug Dictionary).
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).
Ponatinib Iclusig AP24534 BCR-ABL Inhibitor 23 DDR1 Inhibitor 8 DDR2 inhibitor 7 FGFR Inhibitor (Pan) 17 FLT3 Inhibitor 48 KIT Inhibitor 48 PDGFR-alpha Inhibitor 7 RET Inhibitor 36 SRC Inhibitor 26 VEGFR Inhibitor (Pan) 29 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).
Y078-DM4 RET Inhibitor 36 Y078-DM4 is an antibody-drug conjugate composed of a RET antibody (Y078) linked to a derivative of the cytotoxic agent maytansine, which may lead to increased cytotoxicity in RET-expressing tumors (PMID: 26240273).
RXDX-105 AC013773|CEP-32496 ABL Inhibitor (pan) 8 ABL1 Inhibitor 4 BCR-ABL Inhibitor 23 BRAF Inhibitor 18 CRAF Inhibitor 10 KIT Inhibitor 48 PDGFR-beta Inhibitor 13 RET Inhibitor 36 VEGFR2 Inhibitor 34 RXDX-105 (CEP-32496) inhibits wild-type BRAF, BRAF V600E, c-RAF, ABL1 (and BCR-ABL), c-KIT, RET, PDGFR beta, and VEGFR2, potentially resulting in decreased tumor growth (PMID: 22319199).
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).
CLM3 EGFR Inhibitor (Pan) 38 RET Inhibitor 36 VEGFR2 Inhibitor 34 CLM3 is an small molecule multi-kinase inhibitor with activity against several kinases including Ret, Vegfr2, and Egfr, which potentially leads to decreased tumor cell growth (PMID: 21459081, PMID: 24423321).
Vandetanib Caprelsa ZD6474 ABL1 Inhibitor 4 EGFR Inhibitor (Pan) 38 RET Inhibitor 36 SRC Inhibitor 26 VEGFR Inhibitor (Pan) 29 Caprelsa (vandetanib) is a multi-tyrosine kinase inhibitor with activity against VEGFR, EGFR, RET, SRC, and ABL1 kinases, potentially resulting in decreased tumor growth (PMID: 25031937, PMID: 25490448). Caprelsa (vandetanib) is FDA approved for use in medullary thyroid cancer (FDA.gov).
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).
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).
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).
TG101209 FLT3 Inhibitor 48 JAK2 Inhibitor - ATP competitive 14 RET Inhibitor 36 TG101209 is an ATP-competitive inhibitor of JAK2, RET, and FLT3 kinases, which may inhibit proliferation and induce apoptosis in cancer cells (PMID: 17541402).
Pz-1 RET Inhibitor 36 VEGFR2 Inhibitor 34 Pz-1 is an inhibitor with activity against Ret and Kdr, which may result in tumor growth inhibition (PMID: 26126987).
Apatinib Rivoceranib YN968D1 KIT Inhibitor 48 RET Inhibitor 36 SRC Inhibitor 26 VEGFR2 Inhibitor 34 Apatinib (YN968D1) is an inhibitor of receptor tyrosine kinases, including KDR (VEGFR2), RET, c-KIT, Src, and PDGFRa, which may result in reduced cell proliferation and inhibition of tumor growth (PMID: 21443688).
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).
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).
Famitinib SHR1020 FLT3 Inhibitor 48 KIT Inhibitor 48 PDGFR-beta Inhibitor 13 RET Inhibitor 36 VEGFR2 Inhibitor 34 VEGFR3 Inhibitor 5 Famitinib is an analog of Sutent (sunitinib), a receptor tyrosine kinase (RTK) inhibitor, which inhibits receptor tyrosine kinases including c-Kit, VEGFR2/3, PDGFR-beta, RET, and FLT3 to reduce cell proliferation and tumor growth (PMID: 23126373).
Y078-DM1 RET Inhibitor 36 Y078-DM1 is an antibody drug conjugate composed of a RET antibody (Y078) linked to a derivative of the cytotoxic agent maytansine, which may lead to increased cytotoxicity in RET-expressing tumors (PMID: 26240273).
HG-6-63-01 RET Inhibitor 36 HG-6-63-01 inhibits RET, resulting in decreased downstream signaling and reduced tumor cell proliferation (PMID: 26046350).
BLU-667 BLU667 RET Inhibitor 36 BLU-667 selectively inhibits activated Ret, which may result in decreased tumor growth (Mol Cancer Ther 2018;17(1 Suppl):Abstract nr B151).
Alectinib Alecensa CH5424802|RO5424802 ALK Inhibitor 19 RET Inhibitor 36 Alecensa (alectinib) is an inhibitor of RET and ALK, including ALK fusions and the gatekeeper mutation, L1196M (PMID: 21575866, PMID: 25349307). Alecensa (alectinib) is FDA-approved for use in patients with ALK-positive non-small cell lung cancer (FDA.gov).
Cabozantinib Cometriq Cabometyx|Cabozantinib-s-malate|XL184 AXL Inhibitor 24 FLT3 Inhibitor 48 KIT Inhibitor 48 MET Inhibitor 50 RET Inhibitor 36 ROS1 Inhibitor 14 VEGFR2 Inhibitor 34 Cometriq (Cabometyx, cabozantinib) inhibits several receptor tyrosine kinases, including VEGFR2, FLT3, AXL, MET, RET, ROS1 fusions, and c-KIT (PMID: 27370605, PMID: 21926191). Cometriq (cabozantinib) is FDA approved for medullary thyroid cancer and Cabometyx (cabozantinib) is FDA approved for advanced renal cell carcinoma and in sorafenib previously treated hepatocellular carcinoma (FDA.gov).
ALW-II-41-27 RET Inhibitor 36 ALW-II-41-27 is a small molecule that inhibits EPHA2 and RET, leading to decreased tumor cell proliferation and viability (PMID: 24713656, PMID: 26046350).
JNJ-26483327 EGFR Inhibitor (Pan) 38 HER2 Inhibitor 20 RET Inhibitor 36 JNJ-26483327 is a multi-kinase inhbitor, which inhibits wild-type and mutant EGFR, RET, and has activity against VEGFR3, ERBB2 (HER2), ERBB4, and SRC family members (PMID: 20823884).
Sorafenib Nexavar BAY 43-9006 CSF1R Inhibitor 22 FLT3 Inhibitor 48 KIT Inhibitor 48 PDGFR-beta Inhibitor 13 RAF Inhibitor (Pan) 17 RET Inhibitor 36 VEGFR2 Inhibitor 34 Nexavar (sorafenib) is a multikinase inhibitor with activity against several kinases, including RAF kinases, VEGFR2, VEGFR3, PDGFR-beta, KIT, FLT3, RET, and CSF1R, potentially resulting in decreased tumor growth (PMID: 18445656, PMID: 15466206, PMID: 21517818). Nexavar (sorafenib) is approved for metastatic differentiated thyroid carcinoma, hepatocellular carcinoma, and renal cell carcinoma (FDA.gov).
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).
MGCD516 Sitravatinib AXL Inhibitor 24 DDR1 Inhibitor 8 DDR2 inhibitor 7 KIT Inhibitor 48 MET Inhibitor 50 RET Inhibitor 36 Trk Receptor Inhibitor (Pan) 21 VEGFR Inhibitor (Pan) 29 MGCD516 (Sitravatinib) inhibits several receptor tyrosine kinases including AXL, MET, KIT, VEGFR1-3, RET family members, TRK family members, DDR, and Eph family members, resulting in abrogation of downstream signaling and decreased cell proliferation in tumors overexpressing the target proteins (PMID: 26675259).
AD80 RET Inhibitor 36 S6 Kinase Inhibitor 5 AD80 inhibits several kinases including RET and S6K, which may result in decreased tumor growth (PMID: 22678283, PMID: 28249155).
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).
XMD15-44 RET Inhibitor 36 XMD15-44 inhibits RET, resulting in decreased downstream signaling and reduced tumor cell proliferation (PMID: 26046350).
GTx-186 ALK Inhibitor 19 RET Inhibitor 36 ROS1 Inhibitor 14 Trk Receptor Inhibitor (Pan) 21 GTx-186 is a multi-kinase inhibitor targeting TRKA/B/C, ROS1 fusions, ALK, and RET, potentially resulting in decreased growth of ROS1 and TRKA over expressing tumors (PMID: 24386191).
Molecular Profile Protein Effect Treatment Approaches
RET amp unknown RET Inhibitor
RET C630Y gain of function - predicted RET Inhibitor
RET S891A gain of function RET Inhibitor
RET L633_C634dup gain of function RET Inhibitor
RET C515S gain of function RET Inhibitor
RET C634_R635insHELC gain of function RET Inhibitor
RET C630F gain of function RET Inhibitor
RET Y791F gain of function RET Inhibitor
RET C634W gain of function RET Inhibitor
RET S904F unknown RET Inhibitor
RET G533C gain of function RET Inhibitor
RET C630G unknown RET Inhibitor
RET C634Y gain of function RET Inhibitor
RET V292M gain of function RET Inhibitor
RET S649L gain of function RET Inhibitor
RET act mut gain of function RET Inhibitor
RET C630S unknown RET Inhibitor
RET M848T gain of function - predicted RET Inhibitor
RET D631Y gain of function RET Inhibitor
RET C634L gain of function RET Inhibitor
RET C634F gain of function - predicted RET Inhibitor
RET R833C gain of function RET Inhibitor
RET I852M gain of function RET Inhibitor
RET V804M gain of function RET Inhibitor
RET K666E gain of function RET Inhibitor
RET C515W gain of function RET Inhibitor
RET V804L gain of function RET Inhibitor
RET A883T gain of function - predicted RET Inhibitor
RET E505_G506del gain of function RET Inhibitor
RET E632_L633del gain of function - predicted RET Inhibitor
RET E805K gain of function - predicted RET Inhibitor
RET C634S gain of function RET Inhibitor
RET A883F gain of function RET Inhibitor
RET C630R gain of function RET Inhibitor
RET M918T gain of function RET Inhibitor
RET C618R gain of function RET Inhibitor
RET C620Y gain of function RET Inhibitor
RET Y606C gain of function RET Inhibitor
RET M918V no effect - predicted RET Inhibitor
RET C609S gain of function - predicted RET Inhibitor
RET C609Y gain of function RET Inhibitor
RET C611Y gain of function RET Inhibitor
RET C634G gain of function - predicted RET Inhibitor
RET C634R gain of function RET Inhibitor
RET E768D gain of function RET Inhibitor