Novel ALK inhibitors in clinical use and development

Journal of Hematology & Oncology

Delong Liu²  Shundong Cang⁵  Varun Mittal¹  Muhammad Furqan⁴  Akintunde Akinleye³  Milaim Mustafa³  Chaitanya Iragavarapu³ 

[1] Department of Medicine, Division of Hematology/Oncology, Albert Einstein Medical Center, Philadelphia 19141, PA, USA;Henan Cancer Hospital, Zhengzhou University, Zhengzhou, China;Department of Medicine, Westchester Medical Center and New York Medical College, Valhalla 10595, NY, USA;Department of Medicine, Division of Hematology and Oncology, University of Iowa Carver College of Medicine, Iowa City 52242, IA, USA;Department of Oncology, Henan Province People’s Hospital

[2] , Zhengzhou University, Zhengzhou, China

关键词: Ceritinib;    Crizotinib;    ALK-1;    Anaplastic lymphoma kinase;   

Others  :  1133307
DOI  :  10.1186/s13045-015-0122-8

 received in 2014-12-29, accepted in 2015-02-13,  发布年份 2015

【 摘 要 】

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.

【 授权许可】

   
2015 Iragavarapu et al.; licensee BioMed Central.

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