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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。

Etravirine and rilpivirine: nonnucleoside reverse transcriptase inhibitors with activity against human immunodeficiency virus type 1 strains resistant to previous nonnucleoside agents.

作者信息

Fulco Patricia Pecora, McNicholl Ian R

机构信息

Department of Pharmacy, Virginia Commonwealth University Medical Center, Virginia Commonwealth University, Richmond, Virginia, USA.

出版信息

Pharmacotherapy. 2009 Mar;29(3):281-94. doi: 10.1592/phco.29.3.281.

Abstract

Etravirine and rilpivirine are two new nonnucleoside reverse transcriptase inhibitors (NNRTIs) that have the distinct advantage of being able to be used in patients with exposure to previous NNRTIs (e.g., nevirapine or efavirenz). Etravirine was approved by the United States Food and Drug Administration to be used twice/day in treatment-experienced patients infected with the human immunodeficiency virus. The approval was based on phase III clinical studies in which 61% of etravirine-treated patients reached an undetectable viral load of less than 50 copies/ml compared with 40% of patients who received the optimized background regimen. Etravirine was well tolerated with a self-limiting skin rash being the most common toxicity, reported in 19% of patients. Rilpivirine, a once-daily NNRTI, is entering phase III studies; the drug appears to be effective against a broad range of NNRTI-resistant viruses including etravirine-resistant strains.

摘要

依曲韦林和利匹韦林是两种新型非核苷类逆转录酶抑制剂(NNRTIs),它们具有明显优势,可用于曾接触过其他NNRTIs(如奈韦拉平或依非韦伦)的患者。依曲韦林已获美国食品药品监督管理局批准,用于接受过治疗的人类免疫缺陷病毒感染患者,每日服用两次。该批准基于III期临床研究,研究中61%接受依曲韦林治疗的患者病毒载量降至不可检测水平(低于50拷贝/毫升),而接受优化背景治疗方案的患者这一比例为40%。依曲韦林耐受性良好,最常见的毒性反应是自限性皮疹,19%的患者出现该反应。利匹韦林是一种每日服用一次的NNRTI,正在进行III期研究;该药物似乎对多种耐NNRTI病毒有效,包括耐依曲韦林毒株。

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