Lenacapavir: a first-in-class HIV-1 capsid inhibitor
- PMID: 34871187
- DOI: 10.1097/COH.0000000000000713
Lenacapavir: a first-in-class HIV-1 capsid inhibitor
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.
Copyright © 2021 Wolters Kluwer Health, Inc. All rights reserved.
Similar articles
-
Lenacapavir: A novel injectable HIV-1 capsid inhibitor.Int J Antimicrob Agents. 2024 Jan;63(1):107009. doi: 10.1016/j.ijantimicag.2023.107009. Epub 2023 Oct 14. Int J Antimicrob Agents. 2024. PMID: 37844807 Review.
-
Lenacapavir: a first-in-class capsid inhibitor for HIV treatment and prevention.Curr Opin Infect Dis. 2025 Jun 1;38(3):208-213. doi: 10.1097/QCO.0000000000001113. Epub 2025 Apr 23. Curr Opin Infect Dis. 2025. PMID: 40276818 Review.
-
Lenacapavir and the novel HIV-1 capsid inhibitors: an emerging therapy in the management of multidrug-resistant HIV-1 virus.Curr Opin Infect Dis. 2023 Feb 1;36(1):15-19. doi: 10.1097/QCO.0000000000000896. Curr Opin Infect Dis. 2023. PMID: 36753704 Review.
-
Impact of HIV-1 capsid polymorphisms on viral infectivity and susceptibility to lenacapavir.mBio. 2025 May 14;16(5):e0018725. doi: 10.1128/mbio.00187-25. Epub 2025 Apr 17. mBio. 2025. PMID: 40243329 Free PMC article.
-
Lenacapavir: A first-in-class capsid inhibitor for the treatment of highly treatment-resistant HIV.Am J Health Syst Pharm. 2023 Dec 5;80(24):1774-1780. doi: 10.1093/ajhp/zxad223. Am J Health Syst Pharm. 2023. PMID: 37767713 Review.
Cited by
-
The Challenge of Adherence to a Complex Antiretroviral Therapy Regimen in an Individual With Multidrug-Resistant HIV.Top Antivir Med. 2024 Apr 18;32(2):437-444. Top Antivir Med. 2024. PMID: 39141922 Free PMC article.
-
Cost thresholds for anticipated long-acting HIV pre-exposure prophylaxis products in Eastern and Southern Africa: a mathematical modelling study.J Int AIDS Soc. 2025 Feb;28(2):e26427. doi: 10.1002/jia2.26427. J Int AIDS Soc. 2025. PMID: 39995017 Free PMC article.
-
Exploring HIV-1 Maturation: A New Frontier in Antiviral Development.Viruses. 2024 Sep 6;16(9):1423. doi: 10.3390/v16091423. Viruses. 2024. PMID: 39339899 Free PMC article. Review.
-
The significance of chirality in contemporary drug discovery-a mini review.RSC Adv. 2024 Oct 22;14(45):33429-33448. doi: 10.1039/d4ra05694a. eCollection 2024 Oct 17. RSC Adv. 2024. PMID: 39439836 Free PMC article. Review.
-
Impact of Combination Antiretroviral Treatment on Liver Metabolic Health in HIV-Infected Persons.Viruses. 2023 Dec 15;15(12):2432. doi: 10.3390/v15122432. Viruses. 2023. PMID: 38140673 Free PMC article. Review.
References
-
- Teeraananchai S, Kerr SJ, Amin J, et al. Life expectancy of HIV-positive people after starting combination antiretroviral therapy: a meta-analysis. HIV Med 2017; 18:256–266.
-
- Cohen MS, Chen YQ, McCauley M, et al. Antiretroviral therapy for the prevention of HIV-1 transmission. N Engl J Med 2016; 375:830–839.
-
- Enriquez M, McKinsey DS. Strategies to improve HIV treatment adherence in developed countries: clinical management at the individual level. HIV AIDS (Auckl) 2011; 3:45–51.
-
- Link JO, Rhee MS, Tse WC, et al. Clinical targeting of HIV capsid protein with a long-acting small molecule. Nature 2020; 584:614–618.
-
- Bester SM, Wei G, Zhao H, et al. Structural and mechanistic bases for a potent HIV-1 capsid inhibitor. Science 2020; 370:360–364.
Publication types
MeSH terms
Substances
LinkOut - more resources
Full Text Sources
Other Literature Sources
Medical
Research Materials