Etravirine and Rilpivirine: Nonnucleoside Reverse Transcriptase Inhibitors with Activity Against Human Immunodeficiency Virus Type 1 Strains Resistant to Previous Nonnucleoside Agents

被引:35
作者
Fulco, Patricia Pecora [3 ,4 ]
McNicholl, Ian R. [1 ,2 ]
机构
[1] San Francisco Gen Hosp, Med Ctr, UCSF Posit Hlth Program, AAHIVE, San Francisco, CA 94110 USA
[2] Univ Calif San Francisco, Sch Pharm, San Francisco, CA 94143 USA
[3] Virginia Commonwealth Univ, Med Ctr, Dept Pharm, Richmond, VA USA
[4] Virginia Commonwealth Univ, Div Infect Dis, Richmond, VA USA
来源
PHARMACOTHERAPY | 2009年 / 29卷 / 03期
关键词
human immunodeficiency virus; HIV; nonnucleoside reverse transcriptase inhibitor; NNRTI; etravirine; TMC125; rilpivirine; TMC278; EXPERIENCED HIV-1-INFECTED PATIENTS; ANTIVIRAL ACTIVITY; DIARYLPYRIMIDINE ANALOGS; TMC125; ETRAVIRINE; DRUG-RESISTANCE; DOUBLE-BLIND; DARUNAVIR/RITONAVIR; PHARMACOKINETICS; PREVALENCE; EFFICACY;
D O I
10.1592/phco.29.3.281
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
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.
引用
收藏
页码:281 / 294
页数:14
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