无环核苷膦酸（ANPs）的优雅，谨向于 2012 年 7 月 16 日逝世的 Antonín Holý 致敬，值此他逝世十周年之际。

The Elegance of the Acyclic Nucleoside Phosphonates (ANPs), Honorary Tribute to Antonín Holý, Who Passed Away on 16 July 2012, at the 10th Anniversary of His Death.

机构信息

Rega Institute for Medical Research, Herestraat 49, B-3000 Leuven, Belgium.

出版信息

Viruses. 2022 Sep 7;14(9):1978. doi: 10.3390/v14091978.

DOI:10.3390/v14091978

PMID:36146783

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9503179/

Abstract

My collaboration with Prof. Antonín Holý, that spans a period of 3-4 decades (1976-2012), led to the discovery of several acyclic nucleoside phosphonates (ANPs) which were clinically developed by Gilead Sciences: cidofovir, adefovir, and tenofovir. The latter was further converted to two orally bioavailable prodrug forms, TDF and TAF, and both TDF and TAF were further combined with other antiviral drugs, thus giving rise to a broad array of antiviral drug combinations for the treatment of HIV infections. TDF and TAF are both available for the treatment of hepatitis B virus (HBV) infections, and, in combination with emtricitabine, also applicable as Truvada and Descovy, respectively, for the prophylaxis of HIV infections.

摘要

我与 Antonín Holý 教授的合作跨越了 3-4 十年（1976-2012），在此期间发现了几种非循环核苷膦酸酯（ANPs），这些物质后来由吉利德科学公司（Gilead Sciences）开发为临床应用：西多福韦、阿德福韦和替诺福韦。替诺福韦进一步转化为两种可口服生物利用的前药形式，即替诺福韦酯（TDF）和替诺福韦艾拉酚胺（TAF），并且 TDF 和 TAF 都与其他抗病毒药物进一步结合，从而产生了广泛的抗病毒药物组合，用于治疗 HIV 感染。TDF 和 TAF 均可用于治疗乙型肝炎病毒（HBV）感染，并且与恩曲他滨联合使用时，分别作为特鲁瓦达（Truvada）和 Descovy，可用于预防 HIV 感染。