Department of Pharmacy Practice, Faculty of Pharmacy, Helwan University, Cairo, Egypt.
UNC Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, North Carolina, USA.
Curr Opin HIV AIDS. 2022 Jul 1;17(4):240-246. doi: 10.1097/COH.0000000000000740.
To summarize recent updates on the potential role of islatravir for HIV treatment and prevention.
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.
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.
总结伊拉司他韦在 HIV 治疗和预防方面的潜在作用的最新进展。
伊拉司他韦是一种具有独特药理特性的研究性抗逆转录病毒药物,可实现灵活的给药方案。当与多拉韦林和拉米夫定时,伊拉司他韦表现出强大的抗病毒活性和高耐药屏障。伊拉司他韦联合多拉韦林的简化两药 HIV 治疗方案也显示出与标准护理三药方案相当的疗效。伊拉司他韦的活性代谢物半衰期长、效力高,可能支持其作为长效 HIV 暴露前预防 (PrEP) 的选择。每月口服一次伊拉司他韦可在整个给药间隔内保持其活性代谢物的有效浓度。此外,一种研究性的可植入制剂预计可提供至少一年的有效浓度,并表现出类似的分布到阴道和直肠组织中,使其成为男性和女性个体有前途的 PrEP 选择。伊拉司他韦与药物相互作用的风险极小,因为它不是主要药物代谢酶和转运体的底物、诱导剂或抑制剂。最后,临床试验显示伊拉司他韦具有良好的安全性,仅显示轻微和短暂的不良反应。
利用伊拉司他韦独特的药理特性,为简化 HIV 治疗方案和长效 PrEP 提供了机会,使其成为抗逆转录病毒武器库中的宝贵补充。