Back to Journals » Lung Cancer: Targets and Therapy » Volume 7

Profile of rociletinib and its potential in the treatment of non-small-cell lung cancer

Authors Tran P, Klempner S

Received 25 March 2016

Accepted for publication 2 May 2016

Published 18 July 2016 Volume 2016:7 Pages 91—97

DOI https://doi.org/10.2147/LCTT.S94337

Checked for plagiarism Yes

Review by Single anonymous peer review

Peer reviewer comments 2

Editor who approved publication: Prof. Dr. Pan-Chyr Yang


Phu N Tran,1 Samuel J Klempner2,3

1Division of Hematology/Oncology, University of California Irvine, Irvine, CA, 2Angeles Clinic and Research Institute, 3Cedars-Sinai Medical Center, Los Angeles, CA, USA

Abstract: Patients with non-small-cell lung cancer (NSCLC) harboring activating mutations in EGFR benefit from treatment with EGFR small-molecule tyrosine-kinase inhibitors. However, the development of acquired resistance to EGFR inhibitors is universal and limits treatment efficacy. Over half of patients receiving first-generation EGFR inhibitors (erlotinib and gefitinib) develop resistance via the gatekeeper EGFR T790M (EGFRT790M) mutation, and therapies able to overcome T790M-mediated resistance have been an unmet need in NSCLC. Rociletinib (CO-1686) is a third-generation small-molecule EGFR inhibitor with potent activity against EGFRT790M currently in advanced clinical development in NSCLC. Early clinical data suggested significant activity in EGFR-mutant NSCLC harboring T790M alterations. However, important questions regarding side-effect profile, comparability to competitor compounds, acquired resistance, EGFR-therapy sequencing, and combination therapies remain. Here, we review the available preclinical and clinical data for rociletinib, highlight the comparison to other third-generation EGFR inhibitors, and discuss resistance implications and future directions in NSCLC.

Keywords: lung cancer, rociletinib, EGFR, T790M, CO-1686, resistance, tyrosine-kinase inhibitor

Creative Commons License This work is published and licensed by Dove Medical Press Limited. The full terms of this license are available at https://www.dovepress.com/terms.php and incorporate the Creative Commons Attribution - Non Commercial (unported, v3.0) License. By accessing the work you hereby accept the Terms. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed. For permission for commercial use of this work, please see paragraphs 4.2 and 5 of our Terms.

Download Article [PDF]  View Full Text [HTML][Machine readable]