title: Novel ALK inhibitors in clinical use and development.
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.
authors.affiliation: Department of Medicine, Westchester Medical Center and New York Medical College, Valhalla, NY, 10595, USA. Iragavarapuc@wcmc.com.
authors.forename: Chaitanya
authors.initials: C
authors.lastname: Iragavarapu
authors.affiliation: Department of Medicine, Westchester Medical Center and New York Medical College, Valhalla, NY, 10595, USA. mmustafa@une.edu.
authors.forename: Milaim
authors.initials: M
authors.lastname: Mustafa
authors.affiliation: Department of Medicine, Westchester Medical Center and New York Medical College, Valhalla, NY, 10595, USA. docakin@gmail.com.
authors.forename: Akintunde
authors.initials: A
authors.lastname: Akinleye
authors.affiliation: Department of Medicine, Division of Hematology and Oncology, University of Iowa Carver College of Medicine, Iowa City, IA, 52242, USA. dr_furqandow@yahoo.com.
authors.forename: Muhammad
authors.initials: M
authors.lastname: Furqan
authors.affiliation: Department of Medicine, Division of Hematology/Oncology, Albert Einstein Medical Center, Philadelphia, PA, 19141, USA. varun.doc7@gmail.com.
authors.forename: Varun
authors.initials: V
authors.lastname: Mittal
authors.affiliation: Department of Oncology, Henan Province People's Hospital|, Zhengzhou University, Zhengzhou, China. cangshundong@163.com.
authors.forename: Shundong
authors.initials: S
authors.lastname: Cang
authors.affiliation: Henan Cancer Hospital, Zhengzhou University, Zhengzhou, China. delong_liu@nymc.edu.
authors.forename: Delong
authors.initials: D
authors.lastname: Liu
mesh_terms: D000077548:Anaplastic Lymphoma Kinase; D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy*; D047428:Protein Kinase Inhibitors / Q000494:pharmacology*; D020794:Receptor Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors*
chemical_list: D000970:Antineoplastic Agents; D047428:Protein Kinase Inhibitors; C000626173:ALK protein, human; D000077548:Anaplastic Lymphoma Kinase; D020794:Receptor Protein-Tyrosine Kinases