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Novel ALK inhibitors in clinical use and development
Journal article   Open access   Peer reviewed

Novel ALK inhibitors in clinical use and development

Chaitanya Iragavarapu, Milaim Mustafa, Akintunde Akinleye, Muhammad Furqan, Varun Mittal, Shundong Cang and Delong Liu
Journal of hematology and oncology, Vol.8(1), pp.17-17
02/27/2015
DOI: 10.1186/s13045-015-0122-8
PMCID: PMC4349797
PMID: 25888090
url
https://doi.org/10.1186/s13045-015-0122-8View
Published (Version of record) Open Access

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.
Receptor Protein-Tyrosine Kinases - antagonists & inhibitors Antineoplastic Agents - pharmacology Protein Kinase Inhibitors - pharmacology Animals Humans Neoplasms - drug therapy

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