期刊
CURRENT MEDICINAL CHEMISTRY
卷 29, 期 15, 页码 2602-2616出版社
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/0929867328666210914121324
关键词
Entrectinib; indazol benzamide; Trk ABC; ALK; ROS1 inhibitor; NTRK fusion-positive tumors
This study summarizes recent research on the newly approved selective tyrosine kinase inhibitor entrectinib, including its synthesis, mechanism of action, and clinical trials. Based on three clinical studies, entrectinib was found to have good tolerance and manageable safety profile, and it induced clinically meaningful responses in recurrent or advanced solid tumors associated with NTRK fusion-positive or ROS1+ NSCLC. It also demonstrated substantial efficacy in patients with CNS metastases.
Background: Entrectinib is a highly potent ATP-competitive and selective inhibitor of tyrosine kinases - Trk A B C, ALK, and ROS1. It was developed by Roche and initially approved in Japan in 2019 to treat pediatric and adult patients with NTRK fusion-positive, recurrent, or advanced solid tumors. In August 2019, entrectinib received accelerated approval by the U.S FDA for this indication. It is also the first FDA-approved drug designed to target both NTRK and ROS1. Objective: We aim to summarize recent studies related to the synthesis, mechanism of action, and clinical trials of the newly approved selective tyrosine kinase inhibitor entrectinib. Methods: We conduct a literature review of the research studies on the new highly-potent small-molecule entrectinib. Conclusion: Entrectinib, based on three clinical studies (ALKA, STARTRK-1, and STARTRK-2), was well tolerated, with a manageable safety profile. It induced clinically meaningful responses in recurrent or advanced solid tumors associated with NTRK fusion-positive or ROS1+ NSCLC. It demonstrated substantial efficacy in patients with CNS metastases.
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