Novel ALK inhibitors in clinical use and development.

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Iragavarapu C, Mustafa M, Akinleye A, Furqan M, Mittal V, Cang S, Liu D

Novel ALK inhibitors in clinical use and development.

J Hematol Oncol. 2015 Feb 27;8:17. doi: 10.1186/s13045-015-0122-8.

PubMed ID

25888090 [ View in PubMed

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Abstract

Anaplastic lymphoma kinase 1 (ALK-1) is a member of the insulin receptor tyrosine kinase family. ALK-1 was initially found in anaplastic large cell lymphoma (ALCL). ALK mutations have also been implicated in the pathogenesis of non-small cell lung cancer (NSCLC) and other solid tumors. Multiple small molecule inhibitors with activity against ALK and related oncoproteins are under clinical development. Two of them, crizotinib and ceritinib, have been approved by FDA for treatment of locally advanced and metastatic NSCLC. More agents (alectinib, ASP3026, X396) with improved safety, selectivity, and potency are in the pipeline. Dual inhibitors targeting ALK and EGFRm (AP26113), TRK (TSR011), FAK (CEP-37440), or ROS1 (RXDX-101, PF-06463922) are under active clinical development.

DrugBank Data that Cites this Article

Drugs

Brigatinib

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Brigatinib	ALK tyrosine kinase receptor	Protein	Humans	Yes	Inhibitor	Details
Brigatinib	Epidermal growth factor receptor	Protein	Humans	Yes	Inhibitor	Details