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Ref Type Journal Article
PMID (24410791)
Authors Niu FY, Wu YL
Title Novel agents and strategies for overcoming EGFR TKIs resistance.
Journal Vol Issue Date Pages Journal Short Title
Experimental hematology & oncology 3 1 2014 2 Exp Hematol Oncol
URL
Abstract Text Since the recognition of epidermal growth factor receptor (EGFR) as a therapeutic target, EGFR tyrosine kinase inhibitors (TKIs) have been used in lung cancer patients with EGFR mutations, which has been a major breakthrough for lung cancer treatment.. The progression-free survival (PFS) of patients with EGFR mutations treated with EGFR TKIs is significantly prolonged compared with that of patients who underwent standard chemotherapy. However, all patients who initially respond to EGFR TKIs eventually develop acquired resistance (AR). Many small molecule agents and monoclonal antibodies (McAb) targeting signaling pathways are potential therapeutic regimens for overcoming resistance, and various therapeutic strategies are used in clinical practice. Here we review the novel agents and therapeutic strategies for overcoming AR to EGFR TKIs.

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Molecular Profile Treatment Approach
Gene Name Source Synonyms Protein Domains Gene Description Gene Role
Therapy Name Drugs Efficacy Evidence Clinical Trials
Rociletinib Rociletinib 0 7
Drug Name Trade Name Synonyms Drug Classes Drug Description
Rociletinib CO1686|AVL-301|CNX-419|CS-1631|CO-1686 EGFR Inhibitor 3rd gen 26 Rociletinib (CO-1686) is a third-generation EGFR TKI inhibitor and inhibits mutant forms of EGFR including T790M (PMID: 24410791, PMID: 32528828).
Gene Variant Impact Protein Effect Variant Description Associated with drug Resistance
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References