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Review
. 2015 Feb 27:8:17.
doi: 10.1186/s13045-015-0122-8.

Novel ALK inhibitors in clinical use and development

Chaitanya Iragavarapu  1 , Milaim Mustafa  2 , Akintunde Akinleye  3 , Muhammad Furqan  4 , Varun Mittal  5 , Shundong Cang  6 , Delong Liu  7
Affiliations
Review

Novel ALK inhibitors in clinical use and development

Chaitanya Iragavarapu et al. J Hematol Oncol. .

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.

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