title: Dacomitinib for the treatment of advanced or metastatic non-small-cell lung cancer.
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.
authors.affiliation: The Chinese University of Hong Kong, Sir YK Pau Cancer Center, State Key Laboratory of Southern China, Prince of Wales Hospital, Hong Kong, China.
authors.forename: Tony
authors.initials: T
authors.lastname: Mok
authors.forename: Kirsty
authors.initials: K
authors.lastname: Lee
authors.forename: Michael
authors.initials: M
authors.lastname: Tang
authors.forename: Linda
authors.initials: L
authors.lastname: Leung
mesh_terms: D002289:Carcinoma, Non-Small-Cell Lung / Q000188:drug therapy* / Q000235:genetics / Q000473:pathology; D002986:Clinical Trials as Topic; D004341:Drug Evaluation; D064420:Drug-Related Side Effects and Adverse Reactions / Q000473:pathology; D066246:ErbB Receptors / Q000037:antagonists & inhibitors / Q000235:genetics*; D006801:Humans; D020714:Maximum Tolerated Dose; D009154:Mutation; D009362:Neoplasm Metastasis; D009367:Neoplasm Staging; D047428:Protein Kinase Inhibitors / Q000009:adverse effects / Q000145:classification / Q000627:therapeutic use*; D011505:Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors; D052999:Quinazolinones / Q000009:adverse effects / Q000627:therapeutic use*
chemical_list: D047428:Protein Kinase Inhibitors; D052999:Quinazolinones; C525726:dacomitinib; D066246:ErbB Receptors; D011505:Protein-Tyrosine Kinases