The acyclic nucleoside phosphonates (ANPs): Antonín Holý's legacy.

Abstract

The name of Antonín Holý has become synonymous for the era of acyclic nucleoside phosphonates (ANPs), which started with (S)-HPMPA as the prototype and (S)-HPMPC (cidofovir) as the first marketed compound. It has now evolved to a number of compounds clinically used in the treatment of HIV and hepatitis B virus infections, either as such [tenofovir disoproxil fumarate (TDF, Viread®)] or in combination [Truvada®, Atripla®, Complera®, Stribild®]. Truvada has also been approved for the prevention of HIV infections. Forthcoming is a new formulation of tenofovir (TAF: tenofovir alafenamide). Also forthcoming are several "quad" drug combinations containing either TDF or TAF. Other ANPs, based on either an alkoxy side chain or 5-azacytosine heterocycle seem highly promising and worth further pursuing.

• Authors: Erik De Clercq
• Journal: Medicinal research reviews (Med Res Rev) Vol. 33 Issue 6 Pg. 1278-303 (Nov 2013) ISSN: 1098-1128 [Electronic] United States
• PMID: 23568857 (Publication Type: Journal Article, Review)
• Copyright: © 2013 Wiley Periodicals, Inc.

Chemical References

• Antiviral Agents
• Nucleosides
• Organophosphonates

Topics

• Antiviral Agents (chemistry, pharmacology)
• Humans
• Nucleosides (chemistry, pharmacology)
• Organophosphonates (chemistry, pharmacology)
• Plant Viruses (drug effects)