Kiser Jennifer J
Department of Pharmaceutical Sciences, University of Colorado Denver, School of Pharmacy, Denver, Colorado 80262, USA.
Curr Opin HIV AIDS. 2008 May;3(3):330-41. doi: 10.1097/COH.0b013e3282fbaa6b.
Two agents from antiretroviral classes with novel mechanisms of action against HIV received regulatory approval in 2007. Maraviroc is the first in the class of chemokine coreceptor 5 antagonists and raltegravir is the first in the class of integrase inhibitors. There are other compounds in these two new classes in later stages of clinical development, as well as several protease inhibitors and nonnucleoside reverse transcriptase inhibitors that have been recently approved or are under investigation for use in treatment-experienced patients. The purpose of this article is to review the pharmacologic characteristics of these newly approved and investigational antiretroviral drugs, with particular emphasis on data presented or published within the past year.
Several pivotal studies describing the efficacy, safety, and pharmacologic properties of maraviroc, vicriviroc, etravirine, rilpivirine, raltegravir, elvitegravir, darunavir/ritonavir, and tipranavir/ritonavir have begun to emerge.
To date, these agents have demonstrated promising virologic activity with primarily excellent tolerability, but there is still much to learn about their pharmacology. Future studies should evaluate their potential for drug-drug interactions and elucidate their concentration-effect relationships. An appreciation for the pharmacology of these drugs is critical to their optimal use.
2007年，两种具有全新抗HIV作用机制的抗逆转录病毒药物获得了监管部门的批准。马拉维若为趋化因子共受体5拮抗剂类中的首个药物，雷特格韦是整合酶抑制剂类中的首个药物。这两个新类别中还有其他化合物正处于临床开发后期阶段，此外，还有几种蛋白酶抑制剂和非核苷类逆转录酶抑制剂最近已获批准或正在接受用于经治患者的研究。本文旨在综述这些新批准和正在研究的抗逆转录病毒药物的药理学特性，特别强调过去一年中公布或发表的数据。
几项描述马拉维若、维立拉若、依曲韦林、利匹韦林、雷特格韦、埃替格韦、达芦那韦/利托那韦和替拉那韦/利托那韦的疗效、安全性及药理学特性的关键研究已陆续出现。
迄今为止，这些药物已显示出有前景的病毒学活性，且耐受性总体良好，但关于它们的药理学仍有许多有待了解之处。未来的研究应评估它们发生药物相互作用的可能性，并阐明其浓度-效应关系。了解这些药物的药理学对于其最佳应用至关重要。
