Drug Class Detail

Drug Class AXL Inhibitor

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Drug Name Trade Name Synonyms Drug Classes Drug Description
Glesatinib MGCD265 AXL Inhibitor 24 MET Inhibitor 50 RON Inhibitor 10 VEGFR Inhibitor (Pan) 30 Glesatinib (MGCD265) inhibits several tyrosine kinases including MET, MST1R (RON), and AXL, as well as VEGFR1-3, and TIE2, which may result in decreased tumor growth (PMID: 25806189, PMID: 26555154).
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).
Merestinib LY2801653 AXL Inhibitor 24 DDR1 Inhibitor 8 DDR2 inhibitor 7 FLT3 Inhibitor 48 MET Inhibitor 50 RON Inhibitor 10 ROS1 Inhibitor 14 Trk Receptor Inhibitor (Pan) 23 Merestinib (LY2801653) inhibits several receptor tyrosine kinases including MET, MST1R (RON), AXL, MERTK, TYRO3, ROS1 fusions, PDGFRA, FLT3, TEK, DDR1/2, MKNK1/2, and NTRK1/2/3 with greatest activity against NTRK1, and may result in decreased tumor growth (PMID: 23275061, PMID: 24305878, PMID: 29568395).
LDC1267 AXL Inhibitor 24 LDC1267 is a specific TAM kinase inhibitor, with activity against Tyro3, AXL, and MERTK, which potentially enhances anti-tumor immune response and decreases tumor metastasis (PMID: 24553136).
Ningetinib CT053PTSA AXL Inhibitor 24 MET Inhibitor 50 VEGFR2 Inhibitor 34 Ningetinib inhibits cMet, Vegfr2, and Axl, which may synergistically inhibits tumor cell growth (Cancer Res 2014;74(19 Suppl):Abstract nr 1755).
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).
Gilteritinib Xospata ASP2215 AXL Inhibitor 24 FLT3 Inhibitor 48 Xospata (gilteritinib) is a small molecule inhibitor of FLT3 and AXL that has activity against FLT3-ITD, FLT3 F691L, and FLT3 D835 mutations, potentially resulting in decreased tumor growth (J Clin Oncol 32:5s, 2014 (suppl; abstr 7070), PMID: 25891481). Xospata (gilteritinib) is FDA approved for use in patients with relapsed or refractory acute myeloid leukemia (AML) with a FLT3 mutation (FDA.gov).
R916562 AXL Inhibitor 24 VEGFR2 Inhibitor 34 R916562 is a small molecule that inhibits both Axl and Vegfr2, therefore results in synergistic inhibition of tumor angiogenesis and metastasis (PMID: 28711351).
Bosutinib Bosulif SKI-606 ABL Inhibitor (pan) 8 AXL Inhibitor 24 BTK inhibitor 20 SRC Inhibitor 26 TNK2 Inhibitor 6 Bosulif (bosutinib) inhibits SRC and ABL kinases, and has additional activity against other kinases including AXL, TNK2, BTK, resulting in decreased pathway activation and inhibition of tumor cell proliferation (PMID: 12543790, PMID: 19039322, PMID: 26555154). Bosulif (bosutinib) is FDA approved for use in patients with Ph+ (BCR-ABL) chronic myelogenous leukemia (FDA.gov).
DS-1205c AXL Inhibitor 24 DS-1205c is a small molecule inhibitor of Axl, which may have anti-tumor activity (J Thorac Oncol. 2017 Nov, 12(11): S2289-S2290, abstract P3.04-012).
BMS-777607 ASLAN002 AXL Inhibitor 24 MET Inhibitor 50 RON Inhibitor 10 BMS-777607 (ASLAN002) is a small molecule that inhibits c-MET, MST1R (RON), and AXL, resulting in decreased downstream pathway activation, potentially resulting in decreased tumor cell growth and metastasis (PMID: 20515943, PMID: 24233399, PMID: 26555154).
MGCD516 Sitravatinib AXL Inhibitor 24 DDR1 Inhibitor 8 DDR2 inhibitor 7 KIT Inhibitor 48 MET Inhibitor 50 RET Inhibitor 36 Trk Receptor Inhibitor (Pan) 23 VEGFR Inhibitor (Pan) 30 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).
INCB081776 AXL Inhibitor 24 INCB081776 is a dual inhibitor of Axl and Mer that blocks TAM family kinase signaling, which may results in enhanced anti-tumor immunity (Cancer Res 2018;78(13 Suppl):Abstract nr 3759).
ADCT-601 AXL Inhibitor 24 ADCT-601 is an antibody-drug conjugate comprising an antibody targeting AXL linked to PL1601, which delivers the cytotoxic agent SG3199 to AXL-expressing tumor cells, potentially leading to decreased tumor growth (Cancer Res July 1 2018 (78) (13 Supplement) 2792A).
TP-0903 AXL Inhibitor 24 TP-0903 is a selective Axl inhibitor that inhibits tumor cell survival (PMID: 22247788).
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).
NPS-1034 AXL Inhibitor 24 MET Inhibitor 50 NPS-1034 inhibits AXL and MET, including mutant forms of MET, as well as other kinases, which potentially results in decreased tumor cell growth and may overcome MET or AXL mediated drug resistance (PMID: 24173966, PMID: 24165158).
BGB-324 Bemcentinib BGB324 AXL Inhibitor 24 BGB-324 (Bemcentinib) is a small molecule inhibitor of Axl, which inhibits tumor growth and may overcome EMT-mediated acquired drug resistance (PMID: 20145120).
ONO-7475 AXL Inhibitor 24 ONO-7475 inhibits AXL and MER, potentially leading to reduced growth and increased apoptosis of tumor cells (PMID: 28912176).
DS-1205b AXL Inhibitor 24 DS-1205b inhibits AXL, which potentially results in decreased cell migration, and reduced tumor growth (Ann Oncol 2017, Vol 28, Suppl 5, Abstract #395P).
BPI-9016M AXL Inhibitor 24 MET Inhibitor 50 BPI-9016M is a small molecule that inhibits MET and AXL and has potential anti-tumor activity (PMID: 29028616, J Clin Oncol 2018 36:15_suppl, e21108-e21108).
RXDX-106 AXL Inhibitor 24 MET Inhibitor 50 RXDX-106 is a small molecule inhibitor of TAM family kinases (Axl, Mer, and Tyro3) and cMet that promotes anti-tumor immune response, resulting in tumor growth inhibition (Eur J Cancer, Vol 69, Supplement 1, December 2016, Page S31).
SGI-7079 AXL Inhibitor 24 SGI-7079 inhibits AXL, which potentially results in decreased tumor cell growth and migration (PMID: 23091115, PMID: 24014597).
HuMax-Axl-ADC AXL Inhibitor 24 HuMax-Axl-ADC is an antibody-drug conjugate comprising an AXL targeted antibody linked to the anti-microtubule compound MMAE, which potentially decreases tumor growth (J Clin Oncol 35, 2017 (suppl; abstr TPS2605)).
Molecular Profile Protein Effect Treatment Approaches