An orally bioavailable prodrug form of penciclovir
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Famciclovir is an oral prodrug of penciclovir [1].
Famciclovir is an oral prodrug of anti- herpesvirus drug penciclovir since penciclovir is poorly absorbed when given orally to rodents. Famciclovir is a diester derivative of 6-deoxy-penciclovir. It can be quickly absorbed and converted to the antiviral drug efficiently both in rat tissues and fluids and in human tissues and fluids. Besides that, famciclovir is relatively stable in the duodenal contents and can give consistent levels of penciclovir in blood. Currently, famciclovir is approved to be used for the treatment of herpes zoster, herpes labialis, genital herpes in immunocompetent adult patients and HSV in immunocompromised adults [1, 2].
参考文献:
[1] Hodge R A V, Sutton D, Boyd M R, et al. Selection of an oral prodrug (BRL 42810; famciclovir) for the antiherpesvirus agent BRL 39123 [9-(4-hydroxy-3-hydroxymethylbut-l-yl) guanine; penciclovir]. Antimicrobial agents and chemotherapy, 1989, 33(10): 1765-1773.
[2] Sáez-Llorens X, Yogev R, Arguedas A, et al. Pharmacokinetics and safety of famciclovir in children with herpes simplex or varicella-zoster virus infection. Antimicrobial agents and chemotherapy, 2009, 53(5): 1912-1920.
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