Christine M Azelby1, Mandy R Sakamoto1, Daniel W Bowles2,3. 1. Department of Medicine, University of Colorado Anschutz Medical Campus, Colorado, AU, USA. 2. Division of Medical Oncology, Department of Medicine, University of Colorado Anschutz Medical Campus, 12801 E 17th Ave, 1665 Aurora Court, Colorado, AU, USA. daniel.bowles@cuanschutz.edu. 3. Rocky Mountain Regional VA Medical Center, Aurora, CO, USA. daniel.bowles@cuanschutz.edu.
Abstract
PURPOSE OF REVIEW: Molecular drivers are increasingly identified as therapeutic targets for non-small cell lung cancer (NSCLC). This review focuses on the role of ROS1 inhibitors in treating relapsed/metastatic ROS-1 altered (ROS1+) NSCLC. RECENT FINDINGS: Four FDA-approved drugs have significant activity against ROS1+ NSCLC: crizotinib, ciritinib, lorlatinib, and entrectinib. Each drug yields an overall response rates exceeding 60% with ciritinib, lorlatinib, and entrectinib possessing intracranial activity. The drugs have manageable toxicity profiles. ROS1 alterations are rare molecular drivers of NSCLC that can be effectively treated with a variety of ROS1-targetd drugs. New agents are being identified that may treat resistance mutations.
PURPOSE OF REVIEW: Molecular drivers are increasingly identified as therapeutic targets for non-small cell lung cancer (NSCLC). This review focuses on the role of ROS1 inhibitors in treating relapsed/metastatic ROS-1 altered (ROS1+) NSCLC. RECENT FINDINGS: Four FDA-approved drugs have significant activity against ROS1+ NSCLC: crizotinib, ciritinib, lorlatinib, and entrectinib. Each drug yields an overall response rates exceeding 60% with ciritinib, lorlatinib, and entrectinib possessing intracranial activity. The drugs have manageable toxicity profiles. ROS1 alterations are rare molecular drivers of NSCLC that can be effectively treated with a variety of ROS1-targetd drugs. New agents are being identified that may treat resistance mutations.
Authors: Alain Charest; Keara Lane; Kevin McMahon; Julie Park; Elizabeth Preisinger; Helen Conroy; David Housman Journal: Genes Chromosomes Cancer Date: 2003-05 Impact factor: 5.006
Authors: Klarisa Rikova; Ailan Guo; Qingfu Zeng; Anthony Possemato; Jian Yu; Herbert Haack; Julie Nardone; Kimberly Lee; Cynthia Reeves; Yu Li; Yerong Hu; Zhiping Tan; Matthew Stokes; Laura Sullivan; Jeffrey Mitchell; Randy Wetzel; Joan Macneill; Jian Min Ren; Jin Yuan; Corey E Bakalarski; Judit Villen; Jon M Kornhauser; Bradley Smith; Daiqiang Li; Xinmin Zhou; Steven P Gygi; Ting-Lei Gu; Roberto D Polakiewicz; John Rush; Michael J Comb Journal: Cell Date: 2007-12-14 Impact factor: 41.582
Authors: Alexander Drilon; Romel Somwar; Jacob P Wagner; Nadeem A Vellore; Christopher A Eide; Matthew S Zabriskie; Maria E Arcila; Jaclyn F Hechtman; Lu Wang; Roger S Smith; Mark G Kris; Gregory J Riely; Brian J Druker; Thomas O'Hare; Marc Ladanyi; Monika A Davare Journal: Clin Cancer Res Date: 2015-12-16 Impact factor: 12.531