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

Lenacapavir: a first-in-class HIV-1 capsid inhibitor Purpose of reviewThis 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 findingsLenacapavir 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.SummaryOngoing 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. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Current Opinion in HIV and Aids Wolters Kluwer Health

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

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Publisher
Wolters Kluwer Health
Copyright
Copyright © 2021 The Author(s). Published by Wolters Kluwer Health, Inc.
ISSN
1746-630X
eISSN
1746-6318
DOI
10.1097/coh.0000000000000713
Publisher site
See Article on Publisher Site

Abstract

Purpose of reviewThis 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 findingsLenacapavir 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.SummaryOngoing 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.

Journal

Current Opinion in HIV and Aids – Wolters Kluwer Health

Published: Jan 1, 2022

References

  • Life expectancy of HIV-positive people after starting combination antiretroviral therapy: a meta-analysis
  • Antiretroviral therapy for the prevention of HIV-1 transmission
  • Strategies to improve HIV treatment adherence in developed countries: clinical management at the individual level
  • Clinical targeting of HIV capsid protein with a long-acting small molecule
  • Structural and mechanistic bases for a potent HIV-1 capsid inhibitor
  • Absence of lenacapavir (GS-6207) phenotypic resistance in HIV Gag cleavage site mutants and in isolates with resistance to existing drug classes
  • Frequency of capsid substitutions associated with GS-6207 in vitro resistance in HIV-1 from antiretroviral-naive and -experienced patients