Dacomitinib for the treatment of advanced or metastatic non-small-cell lung cancer. (April 2014)

• Record Type: Journal Article
• Authors: Mok, Tony; Lee, Kirsty; Tang, Michael; Leung, Linda
• Is Part Of: Future oncology. Volume 10:Number 5(2014)
• Page Start: 813
• Page End: 822
• Publication Date: 2014-04
• Subjects: afatinib -- carcinoma -- EGF -- erlotinib -- gefitinib -- non-small-cell lung -- protein kinase inhibitors -- receptor; Oncology -- Periodicals; 616.99405
• DOI: 10.2217/fon.14.22
• Languages: English
• ISSNs: 1479-6694

Abstract

ABSTRACT: : Dacomitinib (PF-00299804) is a second-generation irreversible HER tyrosine kinase inhibitor (TKI). In preclinical studies, dacomitinib has demonstrated anti-tumor activity in lung cancer cell lines with sensitive and resistant EGFR mutations (including the T790 mutation). Safety and well tolerability of dacomitinib were demonstrated in Phase I studies with stomatitis, diarrhea and skin toxicities being the dose-limiting toxicities. The maximum tolerated dose was established to be 45 mg/day. In Phase II and III studies, dacomitinib has shown clinical activity in both HER tyrosine kinase-naive and HER tyrosine kinase failure settings. Further clinical trials are underway to evaluate the efficacy of dacomitinib in non-small-cell lung cancer.