title: 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.affiliation: Rega Institute for Medical Research, KU Leuven, B-3000, Leuven, Belgium. erik.declercq@rega.kuleuven.ac.be
authors.forename: Erik
authors.initials: E
authors.lastname: De Clercq
mesh_terms: D000998:Antiviral Agents / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D009705:Nucleosides / Q000737:chemistry / Q000494:pharmacology*; D063065:Organophosphonates / Q000737:chemistry / Q000494:pharmacology*; D010942:Plant Viruses / Q000187:drug effects
chemical_list: D000998:Antiviral Agents; D009705:Nucleosides; D063065:Organophosphonates
keywords: HIV; cidofovir; nucleoside phosphonates; tenofovir; truvada