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Lenacapavir, a first-in-class, long-acting capsid inhibitor approved for both HIV-1 treatment and prevention

Year: 2025

Type: article

Abstract: Lenacapavir is a first-in-class, long-acting HIV-1 capsid inhibitor and represents a significant advancement in both the treatment and prevention of HIV-1 infection. It is highly effective against both wild-type and multidrug-resistant strains of the virus. It has a unique mechanism of action involving the disruption of HIV-1 capsid assembly and nuclear import, which ultimately prevents the virus from integrating its genetic material into the host cell’s DNA and hinders viral replication. This review covers lenacapavir’s discovery and development, with a focus on its target validation, lead optimization, chemical synthesis, pharmacokinetic properties, safety profile, and clinical applications.

Source: Medicinal Chemistry Research

DOI: 10.1007/s00044-025-03495-1

Authors: Zi Hui, Xiang-Yang Ye, Yuting Zhang, Longqin Hu, Tian Xie, Zhao-Qian Liu

Institutions: Central South University, Hangzhou Normal University, Rutgers, The State University of New Jersey

Language: English

Topic: HIV/AIDS drug development and treatment

Subfield: Infectious Diseases

Field: Medicine

Domain: Health Sciences

SDG: Good health and well-being

Open Access status: hybrid

Estimated APC paid: $3,990