作者: Gerhard Hamilton , Barbara Rath , Otto Burghuber
DOI: 10.1517/17425255.2015.1021685
关键词: Tyrosine-kinase inhibitor 、 Cancer 、 Metabolite 、 Drug 、 Cancer research 、 Pharmacology 、 Bioavailability 、 Anaplastic lymphoma kinase 、 Crizotinib 、 Medicine 、 Pharmacokinetics
摘要: Introduction: For a subpopulation of NSCLC patients genetic rearrangement the anaplastic lymphoma kinase (ALK) was found as driver mutation, which can be targeted by selective inhibitor crizotinib.Areas covered: This article presents an overview clinical studies that provided characterization pharmacokinetic parameters for administration crizotinib to cancer and factors influencing profiles this drug.Expert opinion: Crizotinib is administered orally capsule indicated 250 mg BID continuously maximal tolerated dose in patients. Bioavailability ∼ 40% are influenced food only minor degree. drug corresponds significant inhibition mutated ALK, retards tumor growth achieves responses majority lactam single metabolite with inhibitory activity ALK fusion protein. Metabol...