Lenacapavir: a first-in-class HIV-1 capsid inhibitor

Curr Opin HIV AIDS. 2022 Jan 1;17(1):15-21. doi: 10.1097/COH.0000000000000713.

Abstract

Purpose of review: This review summarizes available data for lenacapavir, an investigational first-in-class agent that disrupts functioning of HIV capsid protein across multiple steps in the viral life cycle.

Recent findings: Lenacapavir demonstrated picomolar potency in vitro with no cross resistance to existing antiretroviral classes and potent antiviral activity in persons with HIV-1. In persons with HIV-1, there was no preexisting resistance to lenacapavir regardless of treatment history. Lenacapavir can be administered orally either daily or weekly and subcutaneously up to every 6 months. In heavily treatment-experienced persons with multidrug-resistant HIV-1 and in treatment-naive persons with HIV-1, lenacapavir in combination with other antiretroviral agents led to high rates of virologic suppression and was well tolerated.

Summary: Ongoing studies are evaluating long-acting dosing of lenacapavir for treating HIV-1 in combination with other antiretrovirals and preventing HIV-1 as a single agent.

Publication types

  • Review

MeSH terms

  • Anti-HIV Agents* / pharmacology
  • Anti-HIV Agents* / therapeutic use
  • Capsid
  • Capsid Proteins
  • Drug Resistance, Viral
  • HIV Infections* / drug therapy
  • HIV-1*
  • Humans

Substances

  • Anti-HIV Agents
  • Capsid Proteins