The clinical potential of the acyclic (and cyclic) nucleoside phosphonates: the magic of the phosphonate bond.

The use of the acyclic nucleoside phosphonates, starting with (S)-HPMPA as the prototype, yielded three clinically approved antiviral drugs, cidofovir for the treatment of CMV retinitis in AIDS patients, adefovir dipivoxil for the treatment of chronic hepatitis B and tenofovir disoproxil fumarate for the treatment of HIV infections (AIDS) and HBV infections. This era has now grown to many more acyclic (and cyclic) nucleoside phosphonates (such as the "open ring" DAPy and Fd4A phosphonates) and alkoxyalkyl and phosphonoamidate prodrugs thereof, as well as new clinical applications, including new drug combination regimens for the treatment of AIDS, the chemoprophylaxis of HIV infections, and the anticancer potential against some malignant disorders.
AuthorsErik De Clercq
JournalBiochemical pharmacology (Biochem Pharmacol) Vol. 82 Issue 2 Pg. 99-109 (Jul 15 2011) ISSN: 1873-2968 [Electronic] England
PMID21501598 (Publication Type: Journal Article, Review)
CopyrightCopyright © 2011 Elsevier Inc. All rights reserved.
Chemical References
  • Antineoplastic Agents
  • Antiviral Agents
  • GS-9131
  • GS-9148
  • Organophosphonates
  • Prodrugs
  • Guanosine
  • Cytosine
  • Tenofovir
  • Adenine
  • cidofovir
  • adefovir dipivoxil
  • Adenine (analogs & derivatives, therapeutic use)
  • Antineoplastic Agents (pharmacology, therapeutic use)
  • Antiviral Agents (pharmacology, therapeutic use)
  • Cytosine (analogs & derivatives, therapeutic use)
  • Guanosine (analogs & derivatives, therapeutic use)
  • HIV Infections (drug therapy, prevention & control)
  • Hepatitis B (drug therapy)
  • Humans
  • Organophosphonates (pharmacology, therapeutic use)
  • Prodrugs (therapeutic use)
  • Structure-Activity Relationship
  • Tenofovir

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