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依曲韦林用于治疗HIV-1:应对非核苷类逆转录酶抑制剂类药物的局限性

Etravirine for HIV-I: addressing the limitations of the nonnucleoside reverse transcriptase inhibitor class.

作者信息

Grennan Troy, Walmsley Sharon

机构信息

Department of Infectious Diseases, McMaster University, St Joseph's Healthcare F506-1, Hamilton, Ontario, Canada.

出版信息

J Int Assoc Physicians AIDS Care (Chic). 2009 Nov-Dec;8(6):354-63. doi: 10.1177/1545109709347373. Epub 2009 Oct 23.

DOI:10.1177/1545109709347373
PMID:19855100
Abstract

Etravirine (ETR) is a second-generation nonnucleoside reverse transcriptase inhibitor (NNRTI) specifically designed for treatment-experienced patients infected with HIV-1. Its unique strength over other, older agents in the NNRTI class is its higher genetic barrier to resistance, allowing it to be used effectively in patients with limited treatment options. The arrival of ETR in the market has made sequential NNRTI therapy possible for the first time in the history of HIV treatment, as it can maintain virologic activity in the presence of certain (and sometimes multiple) NNRTI mutations. Although ETR has demonstrated efficacy in treatment-experienced and NNRTI-resistant patients in large trials, further analyses on its resistance profile are ongoing. As new data emerge on the weighting of ETR's resistance-associated mutations (RAMs), investigators and clinicians will no doubt be able to further characterize its specific place in the HIV treatment armamentarium.

摘要

依曲韦林(ETR)是一种第二代非核苷类逆转录酶抑制剂(NNRTI),专为治疗经验丰富的HIV-1感染患者设计。与NNRTI类别中的其他较老药物相比,其独特优势在于对耐药性具有更高的基因屏障,从而能够在治疗选择有限的患者中有效使用。ETR进入市场后,HIV治疗史上首次使序贯NNRTI治疗成为可能,因为它在存在某些(有时是多个)NNRTI突变的情况下仍能维持病毒学活性。尽管ETR在大型试验中已证明对治疗经验丰富和对NNRTI耐药的患者有效,但对其耐药谱的进一步分析仍在进行中。随着关于ETR耐药相关突变(RAM)权重的新数据不断出现,研究人员和临床医生无疑将能够进一步明确其在HIV治疗药物库中的具体地位。

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Etravirine for HIV-I: addressing the limitations of the nonnucleoside reverse transcriptase inhibitor class.依曲韦林用于治疗HIV-1:应对非核苷类逆转录酶抑制剂类药物的局限性
J Int Assoc Physicians AIDS Care (Chic). 2009 Nov-Dec;8(6):354-63. doi: 10.1177/1545109709347373. Epub 2009 Oct 23.
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Etravirine and rilpivirine: nonnucleoside reverse transcriptase inhibitors with activity against human immunodeficiency virus type 1 strains resistant to previous nonnucleoside agents.依曲韦林和利匹韦林:对先前非核苷类药物耐药的1型人类免疫缺陷病毒株具有活性的非核苷类逆转录酶抑制剂。
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Shifting paradigms: the resistance profile of etravirine.转变范式:依曲韦林的耐药谱
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