{"title":"islatravir在HIV治疗和预防中的作用:最新进展。","authors":"Abdallah Derbalah, Hayley Christine Karpick, Holly Maize, Preston Skersick, Mackenzie Cottrell, Gauri G Rao","doi":"10.1097/COH.0000000000000740","DOIUrl":null,"url":null,"abstract":"<p><strong>Purpose of review: </strong>To summarize recent updates on the potential role of islatravir for HIV treatment and prevention.</p><p><strong>Recent findings: </strong>Islatravir is an investigational antiretroviral agent with unique pharmacologic properties that facilitate flexible dosing regimens. Islatravir has demonstrated potent antiviral activity and a high barrier to resistance when combined with doravirine and lamivudine. A simplified two-drug HIV treatment regimen of islatravir combined with doravirine has also demonstrated comparable efficacy to standard of care three-drug regimens. The long half-life and high potency of islatravir's active metabolite may support its use as a long-acting option for HIV preexposure prophylaxis (PrEP). A once monthly oral dose of islatravir maintains effective concentrations of its active metabolite over the entire dosing interval. Furthermore, an investigational implantable formulation has been projected to provide efficacious concentrations for at least a year and exhibits comparable distribution into vaginal and rectal tissues making it a promising PrEP option for male and female individuals. Islatravir has minimal risks of drug interactions as it is not a substrate, inducer, or inhibitor of major drug metabolizers and transporters. Finally, clinical trials demonstrate islatravir's favorable safety profile revealing only mild and transient adverse events.</p><p><strong>Summary: </strong>Leveraging the unique pharmacological properties of islatravir offers opportunities for simplified HIV treatment regimens and long-acting PrEP making it a valuable addition to the antiretroviral arsenal.</p>","PeriodicalId":10949,"journal":{"name":"Current Opinion in HIV and AIDS","volume":" ","pages":"240-246"},"PeriodicalIF":4.5000,"publicationDate":"2022-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Role of islatravir in HIV treatment and prevention: an update.\",\"authors\":\"Abdallah Derbalah, Hayley Christine Karpick, Holly Maize, Preston Skersick, Mackenzie Cottrell, Gauri G Rao\",\"doi\":\"10.1097/COH.0000000000000740\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><strong>Purpose of review: </strong>To summarize recent updates on the potential role of islatravir for HIV treatment and prevention.</p><p><strong>Recent findings: </strong>Islatravir is an investigational antiretroviral agent with unique pharmacologic properties that facilitate flexible dosing regimens. Islatravir has demonstrated potent antiviral activity and a high barrier to resistance when combined with doravirine and lamivudine. A simplified two-drug HIV treatment regimen of islatravir combined with doravirine has also demonstrated comparable efficacy to standard of care three-drug regimens. The long half-life and high potency of islatravir's active metabolite may support its use as a long-acting option for HIV preexposure prophylaxis (PrEP). A once monthly oral dose of islatravir maintains effective concentrations of its active metabolite over the entire dosing interval. Furthermore, an investigational implantable formulation has been projected to provide efficacious concentrations for at least a year and exhibits comparable distribution into vaginal and rectal tissues making it a promising PrEP option for male and female individuals. Islatravir has minimal risks of drug interactions as it is not a substrate, inducer, or inhibitor of major drug metabolizers and transporters. Finally, clinical trials demonstrate islatravir's favorable safety profile revealing only mild and transient adverse events.</p><p><strong>Summary: </strong>Leveraging the unique pharmacological properties of islatravir offers opportunities for simplified HIV treatment regimens and long-acting PrEP making it a valuable addition to the antiretroviral arsenal.</p>\",\"PeriodicalId\":10949,\"journal\":{\"name\":\"Current Opinion in HIV and AIDS\",\"volume\":\" \",\"pages\":\"240-246\"},\"PeriodicalIF\":4.5000,\"publicationDate\":\"2022-07-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Current Opinion in HIV and AIDS\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://doi.org/10.1097/COH.0000000000000740\",\"RegionNum\":3,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q2\",\"JCRName\":\"IMMUNOLOGY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Current Opinion in HIV and AIDS","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1097/COH.0000000000000740","RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"IMMUNOLOGY","Score":null,"Total":0}
Role of islatravir in HIV treatment and prevention: an update.
Purpose of review: To summarize recent updates on the potential role of islatravir for HIV treatment and prevention.
Recent findings: Islatravir is an investigational antiretroviral agent with unique pharmacologic properties that facilitate flexible dosing regimens. Islatravir has demonstrated potent antiviral activity and a high barrier to resistance when combined with doravirine and lamivudine. A simplified two-drug HIV treatment regimen of islatravir combined with doravirine has also demonstrated comparable efficacy to standard of care three-drug regimens. The long half-life and high potency of islatravir's active metabolite may support its use as a long-acting option for HIV preexposure prophylaxis (PrEP). A once monthly oral dose of islatravir maintains effective concentrations of its active metabolite over the entire dosing interval. Furthermore, an investigational implantable formulation has been projected to provide efficacious concentrations for at least a year and exhibits comparable distribution into vaginal and rectal tissues making it a promising PrEP option for male and female individuals. Islatravir has minimal risks of drug interactions as it is not a substrate, inducer, or inhibitor of major drug metabolizers and transporters. Finally, clinical trials demonstrate islatravir's favorable safety profile revealing only mild and transient adverse events.
Summary: Leveraging the unique pharmacological properties of islatravir offers opportunities for simplified HIV treatment regimens and long-acting PrEP making it a valuable addition to the antiretroviral arsenal.
期刊介绍:
Published bimonthly and offering a unique and wide ranging perspective on the key developments in the field, each issue of Current Opinion in HIV and AIDS features hand-picked review articles from our team of expert editors. With six disciplines published across the year – including HIV and ageing, a HIV vaccine, and epidemiology – every issue also contains annotated reference detailing the merits of the most important papers.