Drug Class Detail

Drug Class ALK Inhibitor

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Drug Name Trade Name Synonyms Drug Classes Drug Description
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).
Ensartinib X-396 ALK Inhibitor 19 Ensartinib (X-396) is a small molecule inhibitor of ALK, which inhibits downstream signaling and potentially leads to decreased growth of ALK-expressing tumors (PMID: 21613408).
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).
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).
Panulisib P7170 ALK Inhibitor 19 DNA_PK Inhibitor 5 mTOR Inhibitor 48 PI3K Inhibitor (Pan) 34 Panulisib (P7170) inhibits Pi3k, mTOR, Alk, and DNA-PK, resulting in inhibition of cancer cell growth (PMID: 25466244).
Belizatinib TSR-011 ALK Inhibitor 19 Trk Receptor Inhibitor (Pan) 23 Belizatinib (TSR-011) binds to ALK and TRK kinases and inhibits downstream signaling, which may result in decreased proliferation of ALK/TRK expressing tumor cells (PMID: 26753004).
CEP-37440 ALK Inhibitor 19 FAK inhibitor 14 CEP-37440 is a dual kinase inhibitor, which binds to and inhibits ALK and FAK, resulting in decreased downstream signaling and reduced tumor growth (PMID: 25322323).
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).
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).
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).
CEP-28122 ALK Inhibitor 19 CEP-28122 is a small molecule inhibitor of ALK that inhibits growth of ALK-positive tumors (PMID: 22203728).
BMS-754807 ALK Inhibitor 19 Aurka Inhibitors 23 Aurkb Inhibitors 17 IGF-1R Inhibitor 17 MET Inhibitor 50 TrkA Receptor Inhibitor 7 BMS-754807 is a multi-kinase inhibitor with activity against IGF-1R, insulin receptor, MET, ALK, TRKA, TRKB, AURKA, and AURKB, potentially resulting in decreased tumor cell proliferation (PMID: 25748921).
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).
Dalantercept ACE-041|ALK1-Fc ALK Inhibitor 19 Dalantercept (ACE-041) is an ALK1 ligand trap composed of the ALK1 extracellular domain linked to the IgG Fc region, which binds to ALK1 ligands and prevents binding to the receptor, potentially leading to decreased tumor angiogenesis and growth and increased sensitivity to chemotherapeutic agents (PMID: 25708802, PMID: 26373572).
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).
ASP3026 ALK Inhibitor 19 ROS1 Inhibitor 14 ASP3026 selectively inhibits Alk, Ros1 fusions, and Ack, resulting in growth inhibition in tumor cells (PMID: 24419060).
TAE684 NVP-TAE684 ALK Inhibitor 19 TNK2 Inhibitor 6 TAE684 inhibits Fes, Alk, and Tnk2 (Ack1) kinase activity, which may result in decreased proliferation of tumor cells (PMID: 17185414, PMID: 25699576, PMID: 22520759).
X-376 ALK Inhibitor 19 X-376 is a small molecule inhibitor of Alk, which may reduce growth of ALK-driven tumor cells (PMID: 21613408).
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).
Molecular Profile Protein Effect Treatment Approaches
ALK L1196M gain of function - predicted ALK Inhibitor
NPM1-ALK gain of function ALK Inhibitor
ALK rearrange unknown ALK Inhibitor
ALK K1062M gain of function ALK Inhibitor
ALK L1196Q gain of function - predicted ALK Inhibitor
ALK F1174S gain of function ALK Inhibitor
ALK F1245C gain of function ALK Inhibitor
ALK L1198P gain of function - predicted ALK Inhibitor
ETV6-ALK gain of function - predicted ALK Inhibitor
ALK F1174C gain of function ALK Inhibitor
ALK F1174V gain of function - predicted ALK Inhibitor
ALK L1198F gain of function ALK Inhibitor
ALK F1174I gain of function ALK Inhibitor
ALK Y1278S gain of function ALK Inhibitor
ALK G1269S gain of function - predicted ALK Inhibitor
ALK I1171N gain of function ALK Inhibitor
ALK act mut gain of function ALK Inhibitor
ALK R1192P gain of function ALK Inhibitor
EML4-ALK gain of function ALK Inhibitor
ALK G1201E gain of function ALK Inhibitor
ALK G1128A gain of function ALK Inhibitor
ALK F1174L gain of function ALK Inhibitor
ALK fusion unknown ALK Inhibitor
ALK R1275Q gain of function ALK Inhibitor
ALK M1166R gain of function ALK Inhibitor