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Viruses-Basel

Publication date: 2022-09-01
Volume: 14
Publisher: Multidisciplinary Digital Publishing Institute (MDPI)

Author:

De Clercq, Erik

Keywords:

Science & Technology, Life Sciences & Biomedicine, Virology, HIV, ANPs, cidofovir, adefovir, tenofovir, TDF, TAF, HBV, PrEP, HEPATITIS-B-VIRUS, HYDROLASE INHIBITORS, INFECTION, ANALOGS, DERIVATIVES, FOSCARNET, PATIENT, PRODRUG, POTENT, PURINE, Anniversaries and Special Events, Anti-HIV Agents, Antiviral Agents, Cidofovir, Emtricitabine, Emtricitabine, Tenofovir Disoproxil Fumarate Drug Combination, HIV Infections, Hepatitis B, Hepatitis B virus, Humans, Nucleosides, Organophosphonates, Prodrugs, Tenofovir, 0605 Microbiology, 3107 Microbiology

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.