Maraviroc: Pharmacokinetics and drug Interactions
Maraviroc: Pharmacokinetics and drug Interactions
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Maraviroc：药代动力学和药物相互作用
作者：
S. Abel;D. Back;M. Vourvahis
Maraviroc 是一种有效的选择性 CCR5 拮抗剂，是此类新型口服药物中第一个被批准用于治疗 CCR5-tropic HIV 1 型的药物。 Maraviroc 广泛由 CYP3A4 代谢，肾清除率约占总清除率的 23%。马拉韦罗的半衰期约为 16 小时。 Maraviroc 在临床相关剂量下不会抑制任何主要 CYP450 酶，并且未显示出对其他药物血浆浓度的任何临床相关影响；因此，不需要调整共同给药的药物的剂量。调节 CYP3A4 活性的药物会改变马拉韦罗的暴露量，在某些情况下，需要调整马拉韦罗的剂量。本文旨在回顾马拉韦罗的所有药代动力学和药物相互作用数据，并全面总结马拉韦罗与所有类别的抗逆转录病毒治疗药物以及其他常用药物联合用药时的剂量调整建议。
Maraviroc is a potent selective CCR5 antagonist and is the first of this new class of oral agents to be approved for the treatment of CCR5-tropic HIV type-1. Maraviroc is extensively metabolized by CYP3A4, with renal clearance accounting for approximately 23% of total clearance. The half-life of maraviroc is approximately 16 h. Maraviroc does not inhibit any of the major CYP450 enzymes at clinically relevant doses and it has not shown any clinically relevant effects on plasma concentrations of other agents; hence, no dose adjustments of coadministered agents are required. Maraviroc exposure is altered by agents that modulate the activity of CYP3A4 and, in some circumstances, maraviroc dose adjustment is necessary. This article aims to review all pharmacokinetic and drug interaction data available for maraviroc, and to provide a comprehensive summary of the dose adjustment recommendations for maraviroc when coadministered with agents from all classes of antiretroviral therapy as well as other commonly coadministered agents.
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