Novel ALK inhibitors in clinical use and development

被引：79

作者：

Iragavarapu, Chaitanya ^{[1
,2
]}

Mustafa, Milaim ^{[1
,2
]}

Akinleye, Akintunde ^{[1
,2
]}

Furqan, Muhammad ^{[3
]}

Mittal, Varun ^{[4
]}

Cang, Shundong ^{[5
]}

Liu, Delong ^{[6
]}

机构：

[1] Westchester Med Ctr, Dept Med, Valhalla, NY 10595 USA

[2] New York Med Coll, Valhalla, NY 10595 USA

[3] Univ Iowa, Carver Coll Med, Div Hematol & Oncol, Dept Med, Iowa City, IA 52242 USA

[4] Albert Einstein Med Ctr, Div Hematol Oncol, Dept Med, Philadelphia, PA 19141 USA

[5] Zhengzhou Univ, Henan Prov Peoples Hosp, Dept Oncol, Zhengzhou 450052, Peoples R China

[6] Zhengzhou Univ, Henan Canc Hosp, Zhengzhou 450052, Peoples R China

来源：

JOURNAL OF HEMATOLOGY & ONCOLOGY | 2015年 / 8卷

关键词：

Anaplastic lymphoma kinase; ALK-1; Crizotinib; Ceritinib; ANAPLASTIC LYMPHOMA KINASE; LARGE-CELL LYMPHOMA; LUNG-CANCER; EML4-ALK FUSION; NPM-ALK; TYROSINE KINASE; CRIZOTINIB RESISTANCE; GENOMIC BREAKPOINTS; NUCLEAR EXPORT; GENE FUSION;

D O I：

10.1186/s13045-015-0122-8

中图分类号：

R73 [肿瘤学];

学科分类号：

100214 ;

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.

引用

页数：9

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