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

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 EGF...

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Autores principales:	Tran PN, Klempner SJ
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2016
Materias:	Lung cancer rociletinib EGFR T790M CO-1686 resistance tyrosine kinase inhibitor Neoplasms. Tumors. Oncology. Including cancer and carcinogens RC254-282
Acceso en línea:	https://doaj.org/article/257d16dc79d6480186401d46e39d1bd1
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spelling	oai:doaj.org-article:257d16dc79d6480186401d46e39d1bd12021-12-02T01:09:33ZProfile of rociletinib and its potential in the treatment of non-small-cell lung cancer1179-2728https://doaj.org/article/257d16dc79d6480186401d46e39d1bd12016-07-01T00:00:00Zhttps://www.dovepress.com/profile-of-rociletinib-and-its-potential-in-the-treatment-of-non-small-peer-reviewed-article-LCTThttps://doaj.org/toc/1179-2728Phu 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 inhibitorTran PNKlempner SJDove Medical PressarticleLung cancerrociletinibEGFRT790MCO-1686resistancetyrosine kinase inhibitorNeoplasms. Tumors. Oncology. Including cancer and carcinogensRC254-282ENLung Cancer: Targets and Therapy, Vol 2016, Iss Issue 1, Pp 91-97 (2016)
institution	DOAJ
collection	DOAJ
language	EN
topic	Lung cancer rociletinib EGFR T790M CO-1686 resistance tyrosine kinase inhibitor Neoplasms. Tumors. Oncology. Including cancer and carcinogens RC254-282
spellingShingle	Lung cancer rociletinib EGFR T790M CO-1686 resistance tyrosine kinase inhibitor Neoplasms. Tumors. Oncology. Including cancer and carcinogens RC254-282 Tran PN Klempner SJ Profile of rociletinib and its potential in the treatment of non-small-cell lung cancer
description	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
format	article
author	Tran PN Klempner SJ
author_facet	Tran PN Klempner SJ
author_sort	Tran PN
title	Profile of rociletinib and its potential in the treatment of non-small-cell lung cancer
title_short	Profile of rociletinib and its potential in the treatment of non-small-cell lung cancer
title_full	Profile of rociletinib and its potential in the treatment of non-small-cell lung cancer
title_fullStr	Profile of rociletinib and its potential in the treatment of non-small-cell lung cancer
title_full_unstemmed	Profile of rociletinib and its potential in the treatment of non-small-cell lung cancer
title_sort	profile of rociletinib and its potential in the treatment of non-small-cell lung cancer
publisher	Dove Medical Press
publishDate	2016
url	https://doaj.org/article/257d16dc79d6480186401d46e39d1bd1
work_keys_str_mv	AT tranpn profileofrociletinibanditspotentialinthetreatmentofnonsmallcelllungcancer AT klempnersj profileofrociletinibanditspotentialinthetreatmentofnonsmallcelllungcancer
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Profile of rociletinib and its potential in the treatment of non-small-cell lung cancer

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