Drug Class Detail

Drug Class ROS1 Inhibitor

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Drug Name Trade Name Synonyms Drug Classes Drug Description
AZD3463 ALK Inhibitor 19 IGF-1R Inhibitor 17 ROS1 Inhibitor 14 AZD3463 inhibits IGF1R and ALK, including wild-type and mutant ALK, and has additional activity against ROS1 fusions, which decreases downstream signaling resulting in reduced tumor cell growth (PMID: 26786851, PMID: 26372962).
Lorlatinib Lorbrena PF-06463922 ALK Inhibitor 19 ROS1 Inhibitor 14 Lorbrena (lorlatinib) is a small molecule inhibitor of Alk and Ros1 fusion proteins, which may result in suppression of Alk and Ros1-mediated signaling thereby inhibiting cell growth and causing tumor regression (PMID: 26144315). Lorbrena (lorlatinib) is FDA approved for use in patients with ALK-positive non-small cell lung cancer (FDA.gov).
DS-6051a ROS1 Inhibitor 14 Trk Receptor Inhibitor (Pan) 23 DS-6051a is the free base form of DS-6051b that inhibits ROS1 and NTRK1/2/3, which may lead to growth inhibition in tumor cells (PMID: 27477320).
ASP3026 ALK Inhibitor 19 ROS1 Inhibitor 14 ASP3026 selectively inhibits Alk, Ros1 fusions, and Ack, resulting in growth inhibition in tumor cells (PMID: 24419060).
Ceritinib Zykadia LDK378 ALK Inhibitor 19 ROS1 Inhibitor 14 Zykadia (ceritinib) inhibits ALK, including ALK mutations and fusions, and has additional activity against ROS1 fusions, potentially resulting in decreased tumor cell growth (PMID: 25322323, PMID: 26372962). Zykadia (ceritinib) is FDA approved for ALK-positive metastatic non-small cell lung cancer (FDA.gov).
Foretinib GSK1363089G|XL880|EXEL-2880 MET Inhibitor 50 ROS1 Inhibitor 14 TrkA Receptor Inhibitor 7 VEGFR2 Inhibitor 34 Foretinib (GSK1363089) is a multi-kinase inhibitor with activity against several receptor tyrosine kinases, including MET, KDR (VEGFR2), as well as ROS1 and NTRK fusions, which may result in decreased tumor angiogenesis and growth (PMID: 19808973, PMID: 26372962, PMID: 29463555).
GTx-186 ALK Inhibitor 19 RET Inhibitor 36 ROS1 Inhibitor 14 Trk Receptor Inhibitor (Pan) 23 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).
Repotrectinib TPX-0005 ALK Inhibitor 19 JAK2 Inhibitor 17 ROS1 Inhibitor 14 SRC Inhibitor 26 Trk Receptor Inhibitor (Pan) 23 Repotrectinib (TPX-0005) is a multi-kinase inhibitor that demonstrates strong activity against Ros1, Ntrk1/2/3, and Alk, and also inhibits Jak2 and Src family kinases, resulting in tumor cell death (PMID: 30093503).
Entrectinib RXDX-101 ALK Inhibitor 19 ROS1 Inhibitor 14 Trk Receptor Inhibitor (Pan) 23 Entrectinib (RXDX-101) inhibits the activity of TrkA/B/C, Ros1 fusion proteins, and Alk, which leads to induction of apoptosis and inhibition of proliferation in cells expressing these kinases (PMID: 27003761).
DS6051b DS-6051B|DS-6051 ROS1 Inhibitor 14 Trk Receptor Inhibitor (Pan) 23 DS6051b is an inhibitor of NTRK1/2/3 and ROS1 fusion proteins, which inhibits downstream signaling and may lead to decreased tumor cell growth (Cancer Res 2016;76(14 Suppl):Abstract nr CT024).
Crizotinib Xalkori PF-02341066 ALK Inhibitor 19 MET Inhibitor 50 RON Inhibitor 10 ROS1 Inhibitor 14 Xalkori (crizotinib), inhibits ALK kinase, ALK fusion proteins, c-Met, ROS1 fusion proteins, and MST1R (RON), resulting in growth inhibition of tumor cells (PMID: 26951079, PMID: 22617245). Xalkori (crizotinib) is FDA approved for use in patients with ALK or ROS1 positive non-small cell lung cancer (FDA.gov).
Brigatinib Alunbrig AP26113 ALK Inhibitor 19 EGFR Inhibitor (Pan) 38 FLT3 Inhibitor 48 IGF-1R Inhibitor 17 ROS1 Inhibitor 14 Alunbrig (brigatinib) is a multi-kinase inhibitor with selected activity against ALK, ROS1 fusions, FLT3, IGF1R and mutant EGFR, potentially resulting in decreased tumor growth (PMID: 27780853). Alunbrig (brigatinib) is FDA approved for use in patients with ALK-positive non-small cell lung cancer who have progressed on or are intolerant to crizotinib (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).
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).
Molecular Profile Protein Effect Treatment Approaches
ROS1 rearrange unknown ROS1 Inhibitor
ROS1 fusion unknown ROS1 Inhibitor
ETV6-ROS1 gain of function - predicted ROS1 Inhibitor