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新型 NNRTIs 治疗 HIV 的治疗新前景:浅析最新数据。

New therapeutic landscape of NNRTIs for treatment of HIV: a look at recent data.

机构信息

University of Miami Miller School of Medicine, Division of Infectious Diseases, Department of Medicine, Room 857 Clinical Research Bldg, 1120 NW 14th Street, Miami, FL 33136, USA.

出版信息

Expert Opin Pharmacother. 2012 Dec;13(18):2601-12. doi: 10.1517/14656566.2012.742506.

Abstract

INTRODUCTION

A key objective with highly active antiretroviral therapy for the treatment of HIV infection has been the optimization of antiretroviral drug combinations for individual patients.

AREAS COVERED

Overall, non-nucleoside reverse transcriptase inhibitor (NNRTI)-based regimens (in combination with two nucleoside reverse transcriptase inhibitors (NRTIs)) have become mainstays for initial ARV regimens. Early NNRTIs, efavirenz and nevirapine, are similarly efficacious, but differ according to their toxicity profiles. Newer NNRTIs, rilpivirine and etravirine are also efficacious. Etravirine was designed to overcome common first-line NNRTI resistance mutations, and serves as a second line agent.

EXPERT OPINION

As a class, NNRTIs are key components of ARV regimens. Currently, there are 3 NNRTIs that may be used in first-line regimens, and one in second-line regimens. ARV regimen optimization depends on matching individual drug efficacy, safety, resistance, and toxicity profiles to particular patients. Once-daily dosing options are essential to treatment simplification strategies, which have been shown to enhance regimen compliance and durabiltiy. These are especially important due to the low genetic barrier to resistance generally associated with NNRTIs. As newer drugs are introduced, especially as part of once-daily, single-tablet regimens, this will expand the number of convenient and efficacious treatment options available.

摘要

简介

高效抗逆转录病毒疗法治疗 HIV 感染的一个关键目标是优化针对个体患者的抗逆转录病毒药物组合。

涵盖领域

总的来说,基于非核苷类逆转录酶抑制剂(NNRTI)的方案(与两种核苷类逆转录酶抑制剂(NRTIs)联合使用)已成为初始 ARV 方案的主要方案。早期的 NNRTI,依非韦伦和奈韦拉平,同样有效,但根据其毒性特征有所不同。新的 NNRTI,利匹韦林和依曲韦林也同样有效。依曲韦林旨在克服常见的一线 NNRTI 耐药突变,作为二线药物。

专家意见

作为一类药物,NNRTIs 是 ARV 方案的关键组成部分。目前,有 3 种 NNRTIs 可用于一线方案,1 种可用于二线方案。ARV 方案的优化取决于将个体药物的疗效、安全性、耐药性和毒性特征与特定患者相匹配。每日一次的给药方案对于简化治疗策略至关重要,因为它已被证明可以提高方案的依从性和耐久性。这一点非常重要,因为 NNRTIs 通常与较低的遗传耐药性相关。随着新药物的引入,尤其是作为每日一次、单片制剂的一部分,这将扩大有效且方便的治疗选择的数量。

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