2021年12月13日 · Islatravir (MK-8591) is Merck’s investigational nucleoside reverse transcriptase translocation inhibitor under evaluation for the treatment and prevention of HIV-1. About PIFELTRO™ and DELSTRIGO™.

Islatravir (4′-ethynyl-2-fluoro-2′-deoxyadenosine, EFdA, or MK-8591) is an investigational drug for the treatment of HIV infection. [1] It is classified as a nucleoside reverse transcriptase translocation inhibitor (NRTTI). [2] Merck is developing a subdermal drug-eluting implant to administer islatravir. [3] [4]

2021年10月4日 · Islatravir (MK-8591) is a highly potent type 1 human immunodeficiency virus (HIV-1) nucleoside reverse transcriptase translocation inhibitor with a long intracellular...

2023年2月22日 · MK-8591A-051 – A Phase 3, Randomized, Active-Controlled, Open-Label Clinical Study to Evaluate a Switch to Doravirine/Islatravir (DOR/ISL 100 mg/0.25 mg) Once-Daily in Participants With HIV-1 Who Are Virologically Suppressed on Antiretroviral Therapy

islatravir是默沙东在研的一款新型口服核苷逆转录酶易位抑制剂（NRTTI），用于与其他抗逆转录病毒药物联合治疗HIV-1感染者。 这些研究的详细结果将在未来的科学大会上公布，并将成为全球监管申请的基础。 默沙东研究实验室传染病全球临床开发副总裁Joan Butterton博士表示：“默沙东致力于研究潜在的治疗方案，以帮助满足HIV感染者不断变化的需求。 我们对3期ILLUMINATE SWITCH A和B试验的结果感到鼓舞，其中DOR/ISL固定剂量片剂的疗效与某些常用的三药方案 …

2019年7月23日 · Islatravir (formerly MK-8591) is Merck’s investigational nucleoside reverse transcriptase translocation inhibitor (NRTTI) currently being evaluated in clinical trials for the treatment of HIV-1 infection in combination with other antiretrovirals, as well as for pre-exposure prophylaxis (PrEP) of HIV-1 infection as a single investigational ...

Islatravir (原名MK-8591或EFdA)是第一种核苷 逆转录酶 易位抑制剂 (NRTTI)。 它在体内的半衰期很长，最初显示出对长效HIV治疗和预防的希望。 作为每日一次的抗逆转录病毒治疗的组成部分，Islatravir与默克公司的 核苷逆转录酶抑制剂 多拉韦林联合使用是安全有效的。 此外，它与默克公司的实验性长效药物NNRTI MK-8507和 吉利德科学公司 的HIV衣壳抑制剂lenacapavir (Sunlenca，最近在欧洲获得批准)联合使用，有望成为每周一次的治疗药物。 Islatravir也被用 …

Islatravir (MK-8591) is a potent anti-HIV-1 agent, acting as a nucleoside reverse transcriptase inhibitor, with EC 50 s of 0.068 nM, 3.1 nM and 0.15 nM for HIV-1 (WT), HIV-1 (M184V), HIV-1 (MDR), respectively.

2020年1月3日 · Islatravir (also known as ISL and MK-8591) is a unique nucleoside reverse transcriptase translocation inhibitor in clinical development for treatment of people with HIV-1 infection. In preclinical studies, intracellular islatravir-triphosphate exhibits a long half-life and prolonged virological effects.

Purpose of review: 4'-Ethynyl-2-fluoro-2'-deoxyadenosine (EFdA) is a nucleoside reverse transcriptase inhibitor (NRTI) with a novel mechanism of action, unique structure, and amongst NRTIs, unparalleled anti-HIV-1 activity.