For research use only.
CAS No. 124832-27-5
Valaciclovir HCl, an aciclovir prodrug, inhibits activity of virus DNA polymerase, used to treat infections caused by herpes simplex virus (HSV) and varicella zoster virus, and for prophylaxis against cytomegalovirus (CMV).
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Choose Selective CMV Inhibitors
|Description||Valaciclovir HCl, an aciclovir prodrug, inhibits activity of virus DNA polymerase, used to treat infections caused by herpes simplex virus (HSV) and varicella zoster virus, and for prophylaxis against cytomegalovirus (CMV).|
Valaciclovir inhibits the uptake of substrates of dipeptide transporters, such as cefalexin. The metabolism of Valaciclovir to Aciclovir probably occurs within the gut lumen prior to absorption, in the small intestine after uptake but before entry into the portal blood system, and in the liver before entry into systemic circulation.  Valaciclovir (Valtrex, Zelitrex), the L-valine ester of aciclovir, increases aciclovir bioavailability by 3- to 5-fold over that achievable with oral aciclovir. Valaciclovir extends the efficacy of aciclovir in the treatment of herpes zoster and genital HSV infections, using less frequent dose regimens but retaining the highly acceptable safety profile established for aciclovir. Valaciclovir is rapidly absorbed and extensively converted to aciclovir and L-valine, the essential amino acid after oral administration. 
|In vivo||Valaciclovir, the L-valyl ester of acyclovir (ZOVIRAX), demonstrates good oral absorption and nearly complete conversion to acyclovir incynomolgus monkeys, indicating its suitability as an orally administered prodrug.  Valaciclovir demonstrates good oral absorption, rapid distribution and elimination, and extensive biotransformation to acyclovir in male CD rats. Valaciclovir is more efficiently metabolized when administered orally, indicating first-pass intestinal and/or hepatic metabolism. Rapid hydrolysis of Valaciclovir in rat liver and intestinal homogenates further suggested the significance of presystemic metabolism. |
|In vitro||Water||72 mg/mL (199.55 mM)|
|DMSO||14 mg/mL (38.8 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02997982||Completed||Drug: Valaciclovir 500Mg Tablet||Alzheimer Disease|Mild Cognitive Impairment|Herpes Simplex||Hugo Lovheim|Umeå University||December 2016||Phase 2|
|NCT01633476||Unknown status||Drug: Valaciclovir||ANCA Associated Vasculitis|CMV Infection||Professor Lorraine Harper|Wellcome Trust|University of Birmingham||July 2013||Phase 2|
|NCT01364792||Completed||Drug: Valaciclovir||Schizophrenia|Psychosis||University Medical Center Groningen|Stanley Medical Research Institute||April 2011||Phase 2|
|NCT01390805||Completed||Drug: Valaciclovir Hydrochloride.||Genital Herpes||GlaxoSmithKline||November 2006||--|
|NCT00169416||Completed||Drug: valaciclovir HCl granules||Varicella||GlaxoSmithKline||March 2005||Phase 3|
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