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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


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

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