Penciclovir: profile and news

Recent Developments in the Treatment of Cutaneous Viral Infections Apr 20, 2006
Nucleoside analogues, including acyclovir, valacyclovir, penciclovir, and famciclovir, are currently the primary antiviral medications used in the management ... - Medscape (subscription)

Barrier Therapeutics Announces First Quarter 2006 Financial ... May 2, 2006
Execution of an agreement with Novartis Consumer Health Canada, Inc., under which Barrier will market and distribute Denavir® (penciclovir cream) 1% in ... - Market Wire (press release)

Other information

Indication
Used to treat recurrent cold sores on the lips and face.

Pharmacology
Penciclovir is the active metabolite of the oral product famciclovir. The more favorable results observed with topical penciclovir versus topical acyclovir for the treatment of herpes labialis may be due to the longer intracellular half-life of penciclovir in HSV-infected cells.

Mechanism Of Action
Penciclovir has in vitro activity against herpes simplex virus types 1 (HSV-1) and 2 (HSV-2). In cells infected with HSV-1 or HSV-2, viral thymidine kinase phosphorylates penciclovir to a monophosphate form. The monophosphate form of the drug is then converted to penciclovir triphosphate by cellular kinases. The intracellular triphosphate of penciclovir is retained in vitro inside HSV-infected cells for 10-20 hours, compared with 0.7-1 hour for acyclovir. in vitro studies show that penciclovir triphosphate selectively inhibits viral DNA polymerase by competing with deoxyguanosine triphosphate. Inhibition of DNA synthesis of virus-infected cells inhibits viral replication. In cells not infected with HSV, DNA synthesis is unaltered. Resistant mutants of HSV can occur from qualitative changes in viral thymidine kinase or DNA polymerase. The most commonly encountered acyclovir-resistant mutants that are deficient in viral thymidine kinase are also resistant to penciclovir.

Drug Category
Antivirals; ATC:D06BB06; ATC:J05AB13

Brand Names/Synonyms
Denavir; PE2; Penciclovir; Penciclovir [Usan:Ban:Inn]; Penciclovirum [Inn-Latin]

Dosage Forms
Topical cream

Absorption
Measurable penciclovir concentrations were not detected in plasma or urine of healthy male volunteers (n= 12) following single or repeat application of the 1% cream at a dose of 180 mg penciclovir daily.

Interactions
Interactions for Penciclovir:

No information provided.

Chemical IUPAC Name
2-amino-9-[4-hydroxy-3-(hydroxymethyl)butyl]-3,9-dihydropurin-6-one

Chemical Formula
C10H15N5O3

Half Life
2 hours

Drug Type
Approved Drug

# Accession No
APRD00041

CAS Registry Number
39809-25-1