{"title":"依曲韦林（TMC-125）：治疗 HIV-1 感染的证据。","authors":"Hans-Jürgen Stellbrink","doi":"10.2147/ce.s6009","DOIUrl":null,"url":null,"abstract":"<p><strong>Introduction: </strong>Etravirine is a novel nonnucleoside reverse transcriptase inhibitor (NNRTI) specifically designed to suppress the replication of viruses resistant to the three currently approved NNRTIs efavirenz, nevirapine, and delavirdine.</p><p><strong>Aims: </strong>To assess the evidence for the place of etravirine in the treatment of HIV-1 infection.</p><p><strong>Evidence review: </strong>In combination with a ritonavir-boosted protease inhibitor etravirine has demonstrated high antiviral activity against strains exhibiting up to three NNRTI resistance mutations. The drug appears to be well tolerated, with only nausea and rash occuring significantly more frequently with etravirine compared with placebo. Of note, neuropsychologic side effects that frequently limit the use of efavirenz were not reported more frequently with etravirine.</p><p><strong>Place in therapy: </strong>Given its high activity against most NNRTI-resistant strains and its very good tolerability, etravirine is of high value for pretreated patients with NNRTI resistance and protease inhibitor exposure. Efforts should be made to demonstrate activity in switching strategies (due to toxicity) and earlier lines of failure or in the setting of primary NNRTI resistance in order to explore the potential of the drug beyond salvage therapy.</p>","PeriodicalId":10764,"journal":{"name":"Core Evidence","volume":"4 ","pages":"149-58"},"PeriodicalIF":0.0000,"publicationDate":"2010-06-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2899779/pdf/","citationCount":"0","resultStr":"{\"title\":\"Etravirine (TMC-125): The evidence for its place in the treatment of HIV-1 infection.\",\"authors\":\"Hans-Jürgen Stellbrink\",\"doi\":\"10.2147/ce.s6009\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><strong>Introduction: </strong>Etravirine is a novel nonnucleoside reverse transcriptase inhibitor (NNRTI) specifically designed to suppress the replication of viruses resistant to the three currently approved NNRTIs efavirenz, nevirapine, and delavirdine.</p><p><strong>Aims: </strong>To assess the evidence for the place of etravirine in the treatment of HIV-1 infection.</p><p><strong>Evidence review: </strong>In combination with a ritonavir-boosted protease inhibitor etravirine has demonstrated high antiviral activity against strains exhibiting up to three NNRTI resistance mutations. The drug appears to be well tolerated, with only nausea and rash occuring significantly more frequently with etravirine compared with placebo. Of note, neuropsychologic side effects that frequently limit the use of efavirenz were not reported more frequently with etravirine.</p><p><strong>Place in therapy: </strong>Given its high activity against most NNRTI-resistant strains and its very good tolerability, etravirine is of high value for pretreated patients with NNRTI resistance and protease inhibitor exposure. Efforts should be made to demonstrate activity in switching strategies (due to toxicity) and earlier lines of failure or in the setting of primary NNRTI resistance in order to explore the potential of the drug beyond salvage therapy.</p>\",\"PeriodicalId\":10764,\"journal\":{\"name\":\"Core Evidence\",\"volume\":\"4 \",\"pages\":\"149-58\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2010-06-15\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2899779/pdf/\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Core Evidence\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.2147/ce.s6009\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Core Evidence","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.2147/ce.s6009","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
Etravirine (TMC-125): The evidence for its place in the treatment of HIV-1 infection.
Introduction: Etravirine is a novel nonnucleoside reverse transcriptase inhibitor (NNRTI) specifically designed to suppress the replication of viruses resistant to the three currently approved NNRTIs efavirenz, nevirapine, and delavirdine.
Aims: To assess the evidence for the place of etravirine in the treatment of HIV-1 infection.
Evidence review: In combination with a ritonavir-boosted protease inhibitor etravirine has demonstrated high antiviral activity against strains exhibiting up to three NNRTI resistance mutations. The drug appears to be well tolerated, with only nausea and rash occuring significantly more frequently with etravirine compared with placebo. Of note, neuropsychologic side effects that frequently limit the use of efavirenz were not reported more frequently with etravirine.
Place in therapy: Given its high activity against most NNRTI-resistant strains and its very good tolerability, etravirine is of high value for pretreated patients with NNRTI resistance and protease inhibitor exposure. Efforts should be made to demonstrate activity in switching strategies (due to toxicity) and earlier lines of failure or in the setting of primary NNRTI resistance in order to explore the potential of the drug beyond salvage therapy.
期刊介绍：
Core Evidence evaluates the evidence underlying the potential place in therapy of drugs throughout their development lifecycle from preclinical to postlaunch. The focus of each review is to evaluate the case for a new drug or class in outcome terms in specific indications and patient groups The emerging evidence on new drugs is reviewed at key stages of development and evaluated against unmet needs
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