Pharmacokinetics of crizotinib in NSCLC patients

作者: Gerhard Hamilton , Barbara Rath , Otto Burghuber

DOI: 10.1517/17425255.2015.1021685

关键词: Tyrosine-kinase inhibitorCancerMetaboliteDrugCancer researchPharmacologyBioavailabilityAnaplastic lymphoma kinaseCrizotinibMedicinePharmacokinetics

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...

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