Citation: Kai Tang, Guochao Wei, Peng Zhan. Breaking the impossible: The evolutionary journey of lenacapavir, a long-acting anti-HIV drug[J]. Chinese Chemical Letters, ;2025, 36(7): 110500. doi: 10.1016/j.cclet.2024.110500 shu

Breaking the impossible: The evolutionary journey of lenacapavir, a long-acting anti-HIV drug

Kai Tang ^a ,
Guochao Wei ^{b, c, *,} ,
Peng Zhan ^{a, *,}

a.
Department of Medicinal Chemistry, Key Laboratory of Chemical Biology, Ministry of Education, School of Pharmaceutical Sciences, Shandong University, Ji'nan 250012, China
b.
Department of Microbiology and Infectious Disease Center, School of Basic Medical Sciences, Peking University Health Science Center, Beijing 100191, China
c.
Shenzhen Blood Center, Shenzhen 518035, China

weiguochao@hsc.pku.edu.cn

zhanpeng1982@sdu.edu.cn

Received Date: 16 July 2024
Revised Date: 20 September 2024
Accepted Date: 24 September 2024
Available Online: 24 September 2024

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Oral antiretroviral drugs have been a fundamental component of human immunodeficiency virus (HIV) treatment for over three decades, and their continuously improving safety and efficacy have directly contributed to reversing the initially devastating course of the HIV epidemic. Long-acting antiretroviral (ARV) regimens are necessary to sustain viral suppression in people living with HIV who express a strong desire to alleviate pill fatigue or avoid the potential stigma associated with daily oral regimens. The development of innovative long-acting ARVs remains an unmet requirement in the fields of HIV treatment and prevention. In this review, we provide an overview of lenacapavir, a first-in-class picomolar long-acting capsid inhibitor for HIV-1 that operates through multiple stages without any known cross-resistance to other existing antiretroviral drug classes.
- HIV-1,
- Capsid,
- Lenacapavir,
- Long-acting,
- Pharmacokinetic properties
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