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Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
Information
Valaciclovir HCl, an aciclovir prodrug, inhibits activity of virusDNA polymerase, used to treat infections caused by herpes simplex virus (HSV) and varicella zoster virus, and for prophylaxis against cytomegalovirus (CMV).
In vitro
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.
Cell Data
cell lines:Cell lines:
Concentrations:
Incubation Time:
Powder Purity:≥98%
| Isomeric SMILES | CC(C)[C@@H](C(=O)OCCOCN1C=NC2=C1N=C(NC2=O)N)N.Cl |
|---|---|
| Molecular Weight | 360.8 |
| Reaxy-Rn | 14444341 |
| Reaxys-RN_link_address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=14444341&ln= |
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