scholarly journals Phase 1 Studies of Poziotinib, an Irreversible Pan-HER Tyrosine Kinase Inhibitor in Patients with Advanced Solid Tumors

2018 ◽  
Vol 50 (3) ◽  
pp. 835-842 ◽  
Author(s):  
Tae Min Kim ◽  
Keun-Wook Lee ◽  
Do-Youn Oh ◽  
Jong-Seok Lee ◽  
Seock-Ah Im ◽  
...  
Keyword(s):  
Tyrosine Kinase ◽  
Tyrosine Kinase Inhibitor ◽  
Solid Tumors ◽  
Kinase Inhibitor ◽  
Phase 1 ◽  
Advanced Solid Tumors

scholarly journals Phase I Study of Bosutinib, a Src/Abl Tyrosine Kinase Inhibitor, Administered to Patients with Advanced Solid Tumors

2011 ◽  
Vol 18 (4) ◽  
pp. 1092-1100 ◽  
Author(s):  
Adil I. Daud ◽  
Smitha S. Krishnamurthi ◽  
Mansoor N. Saleh ◽  
Barbara J. Gitlitz ◽  
Mitesh J. Borad ◽  
...  
Keyword(s):  
Tyrosine Kinase ◽  
Phase I ◽  
Tyrosine Kinase Inhibitor ◽  
Solid Tumors ◽  
Phase I Study ◽  
Kinase Inhibitor ◽  
Advanced Solid Tumors ◽  
Abl Tyrosine Kinase ◽  
Abl Tyrosine Kinase Inhibitor

Entrectinib: A new Selective Tyrosine Kinase Inhibitor Approved for the Treatment of Pediatric and Adult Patients with NTRK Fusion-positive, Recurrent or Advanced Solid Tumors

2021 ◽  
Vol 28 ◽  
Author(s):  
Hind M. Osman ◽  
Meral Tuncbilek
Keyword(s):  
Tyrosine Kinase ◽  
Tyrosine Kinase Inhibitor ◽  
Solid Tumors ◽  
Tyrosine Kinases ◽  
Kinase Inhibitor ◽  
Adult Patients ◽  
Advanced Solid Tumors ◽  
Synthesis Mechanism ◽  
Accelerated Approval ◽  
Positive Recurrent

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 for the treatment of 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. Method: 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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