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

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 (EGFR^T790M) 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 EGFR^T790M currently in advanced clinical development in NSCLC. Early clinical data suggested significant activity in

SUBMITTER: Tran PN 

PROVIDER: S-EPMC5310702 | biostudies-literature | 2016

REPOSITORIES: biostudies-literature