Expanding therapeutic options: lenacapavir + bictegravir as a potential treatment for HIV

Expert Opin Pharmacother. 2023 Sep-Dec;24(18):1949-1956. doi: 10.1080/14656566.2023.2294918. Epub 2024 Jan 5.

Abstract

Introduction: Treatment for people with HIV/AIDS has radically evolved since the introduction of the first antiretrovirals. One newly approved antiretroviral is lenacapavir, which targets the viral capsid. Lenacapavir is currently approved as a therapeutic addition for subjects who are treatment-experienced, and who have developed resistance to multiple antiretrovirals. It is available both as a daily oral tablet and a once every 6-month subcutaneous injection. It is currently undergoing clinical trials in combination with the integrase inhibitor bictegravir as a dual therapy option, both for treatment experienced and treatment naïve individuals.

Areas covered: We reviewed published articles, conference proceedings, and clinical trial databases to assess the current status of the research into lenacapavir and bictegravir. While the clinical trials are ongoing, with little published data to date, this combination shows promise for the treatment of both treatment experienced and naïve patients. We review the studies relevant to the pharmacokinetic/pharmacodynamic properties of the drugs.

Expert opinion: The new combination with bictegravir will be beneficial for treatment experienced patients, as it represents a dual therapy modality with high barriers of resistance. As a therapy for treatment naïve patients, its use is likely more niche, as other combinations are available.

Keywords: Antiretroviral; HIV-1; bictegravir; capsid inhibitor; lenacapavir.

Publication types

  • Review

MeSH terms

  • Amides / therapeutic use
  • Anti-HIV Agents* / pharmacology
  • Anti-HIV Agents* / therapeutic use
  • Anti-Retroviral Agents / therapeutic use
  • HIV Infections* / drug therapy
  • Heterocyclic Compounds, 3-Ring / pharmacology
  • Heterocyclic Compounds, 3-Ring / therapeutic use
  • Heterocyclic Compounds, 4 or More Rings
  • Humans
  • Pyridones / therapeutic use

Substances

  • bictegravir
  • Anti-HIV Agents
  • Amides
  • Heterocyclic Compounds, 3-Ring
  • Pyridones
  • Anti-Retroviral Agents
  • Heterocyclic Compounds, 4 or More Rings