The Holý Trinity: the acyclic nucleoside phosphonates.

Abstract

The Holý Trinity was named after Dr Antonín Holý (the Holý Trinity being an Unesco recognized monument in Olomouc, Czech Republic), who together with Dr John C. Martin (Gilead Sciences) and myself pioneered a new class of antiviral agents, the acyclic nucleoside phosphonates. These compounds have revolutionized the antiviral drug field with several drugs that have been approved for the treatment of various DNA virus infections (cidofovir), hepatitis B (adefovir), and AIDS (HIV infection; tenofovir). The latter is also available as its oral prodrug, tenofovir disoproxil fumarate, for the treatment of hepatitis B and in combination with emtricitabine ((-)FTC) for the treatment and prophylaxis of HIV infections and in combination with (-)FTC and other HIV inhibitors, that is, efavirenz, rilpivirine, or elvitegravir (and a pharmacoenhancer thereof, cobicistat), for the treatment of AIDS.

• Authors: Erik De Clercq
• Journal: Advances in pharmacology (San Diego, Calif.) (Adv Pharmacol) Vol. 67 Pg. 293-316 ( 2013) ISSN: 1557-8925 [Electronic] United States
• PMID: 23886004 (Publication Type: Journal Article, Review)
• Copyright: © 2013 Elsevier Inc. All rights reserved.

Chemical References

• Antiviral Agents
• Nucleosides
• Organophosphonates
• Prodrugs
• adefovir
• Cytosine
• Tenofovir
• 9-(S)-(3-hydroxy-2-(phosphonomethoxy)propyl)adenine
• Adenine
• Cidofovir

Topics

• Adenine (analogs & derivatives, therapeutic use)
• Antiviral Agents (administration & dosage, therapeutic use)
• Cidofovir
• Cytosine (analogs & derivatives, therapeutic use)
• Drug Therapy, Combination
• Humans
• Nucleosides (administration & dosage, therapeutic use)
• Organophosphonates (administration & dosage, therapeutic use)
• Prodrugs (therapeutic use)
• Tenofovir
• Virus Diseases (drug therapy)