期刊
CURRENT OPINION IN HIV AND AIDS
卷 15, 期 1, 页码 27-32出版社
LIPPINCOTT WILLIAMS & WILKINS
DOI: 10.1097/COH.0000000000000599
关键词
HIV nucleoside reverse transcriptase translocation inhibitor; Islatravir; long acting oral and implantable
Purpose of review To discuss the potential role of islatravir (ISL), a novel reverse transcriptase translocation inhibitor, in the treatment and prevention of human immunodeficiency virus type 1 (HIV-1) infection. Recent findings Islatravir (4 '-ethynyl-2-fluoro-2 '-deoxyadenosine, MK-8591) is a long-acting first-in-class nucleoside reverse transcriptase translocation inhibitor with the potential for versatile dosing routes and dosing intervals. It demonstrated robust antiviral activity when dosed once daily and once weekly in HIV-1-infected individuals and SIV-infected rhesus macaques. In clinical trials of ISL in combination with doravirine and lamivudine, daily oral administration resulted in high levels of virologic suppression in HIV-infected individuals. In preclinical studies, ISL dosed orally once-weekly as preexposure prophylaxis (PrEP), protected rhesus macaques against SHIV infection via the mucosal route in the low-dose rectal challenge model. Most recently, data in healthy HIV-1-uninfected individuals demonstrated the feasibility of formulating of ISL as an implant. In these studies, levels of intracellular ISL-triphosphate were consistent with the potential for a once-yearly implantable administration of ISL as PrEP. Islatravir is a promising new agent for both the treatment and prevention of HIV-1 infection.
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