Fluorine in anti-HIV drugs approved by FDA from 1981 to 2023

Sheng Han; Yiming Lu

doi:10.1016/j.ejmech.2023.115586

Fluorine in anti-HIV drugs approved by FDA from 1981 to 2023

Eur J Med Chem. 2023 Oct 5:258:115586. doi: 10.1016/j.ejmech.2023.115586. Epub 2023 Jun 27.

Authors

Sheng Han¹, Yiming Lu²

Affiliations

¹ School of Medicine, Shanghai University, Shanghai, China. Electronic address: hansheng@shu.edu.cn.
² School of Medicine, Shanghai University, Shanghai, China; Department of Critical Care Medicine, Shanghai Tenth People's Hospital, School of Medicine, Tongji University, Shanghai, China. Electronic address: bluesluyi@sina.com.

PMID: 37393791
DOI: 10.1016/j.ejmech.2023.115586

Abstract

Human immunodeficiency virus (HIV) is the etiological agent of acquired immunodeficiency syndrome (AIDS). Nowadays, FDA has approved over thirty antiretroviral drugs grouped in six categories. Interestingly, one-third of these drugs contain different number of fluorine atoms. The introduction of fluorine to obtain drug-like compounds is a well-accepted strategy in medicinal chemistry. In this review, we summarized 11 fluorine-containing anti-HIV drugs, focusing on their efficacy, resistance, safety, and specific roles of fluorine in the development of each drug. These examples may be of help for the discovery of new drug candidates bearing fluorine in their structures.

Keywords: AIDS; FDA-Approved drugs; Fluorine; HIV.

Publication types

Review

MeSH terms

Acquired Immunodeficiency Syndrome* / drug therapy
Anti-HIV Agents* / chemistry
Fluorine / chemistry
HIV Infections* / drug therapy
HIV-1*
Humans

Substances

Fluorine
Anti-HIV Agents