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Description: Valaciclovir (INN) or valacyclovir (USAN) is an antiviral drug used in the management of herpes simplex and herpes zoster (shingles). It is a prodrug, being converted in vivo to aciclovir. It is marketed by GlaxoSmithKline under the trade name Valtrex or Zelitrex. [Wikipedia]
Drug Type: Small Molecule; Approved; Investigational
Pharmacology: Valaciclovir (INN) or Valacyclovir (USAN) is a prodrug and synthetic purine nucleoside analogue with inhibitory activity against herpes simplex virus types 1 (HSV-1), 2 (HSV-2), varicella-zoster virus (VZV), Epstein-Barr virus (EBV), and cytomegalovirus (CMV). Valaciclovir is almost completely converted to acyclovir and L-valine. The inhibitory activity of valaciclovir is highly selective due to its affinity for the enzyme thymidine kinase (TK) encoded by HSV and VZV. This viral enzyme converts acyclovir into acyclovir monophosphate, which is then converted into acyclovir diphosphate and triphosphate by cellular enzymes. Acyclovir is selectively converted to the active triphosphate form by cells infected with herpes viruses.
Mechanism of Action: Valaciclovir is phosphorylated by viral thymidine kinase to acyclovir triphosphate (the active metabolite) which then inhibits herpes viral DNA replication by competitive inhibition of viral DNA polymerase, and by incorporation into and termination of the growing viral DNA chain. When used as a substrate for viral DNA polymerase, acyclovir triphosphate competitively inhibits dATP leading to the formation of 'faulty' DNA. This is where acyclovir triphosphate is incorporated into the DNA strand replacing many of the adenosine bases. This results in the prevention of DNA synthesis, as phosphodiester bridges can longer to be built, destabilizing the strand.
Indication: For the treatment or suppression of cold sores (herpes labialis), herpes zoster (shingles), genital herpes in immunocompetent individuals, and recurrent genital herpes in HIV-infected individuals.
Half Life: 2.5-3.3 hours
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Associated Researchers

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Thought leaders and organizations working on research involving Valtrex.

View All Author iconAuthors
  • Anna Wald
  • B Garré
  • Terri Warren
  • Jennifer Almekinder
  • S Croubels
View All Clinical trial sponsors icon Clinical Trials Sponsors
  • GlaxoSmithKline
  • National Institute of Allergy and Infectious Diseases (NIAID)
  • University of Washington
  • Glaxo Wellcome
  • Advantagene, Inc.
View All Affiliations icon Organizations
  • University of Washington
  • Ghent University
  • Indiana University School of Medicine
  • Charles University Medical School and Teaching Hospital
  • Harvard University

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