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Description

Ganciclovir is a synthetic acyclic nucleoside analogue of 2'-deoxyguanosine active against cytomegalovirus. Ganciclovir has been shown to be active against cytomegalovirus (CMV) and herpes simplex virus (HSV) in humans. To achieve anti-CMV activity, ganciclovir is phosphorylated first to the monophosphate form by a CMV-encoded (UL97 gene) protein kinase homologue, then to the di- and triphosphate forms by cellular kinases. Ganciclovir triphosphate concentrations may be 100-fold greater in CMV-infected than in uninfected cells, indicating preferential phosphorylation in infected cells. Ganciclovir triphosphate, once formed, persists for days in the CMV-infected cell. Ganciclovir triphosphate is believed to inhibit viral DNA synthesis by (1) competitive inhibition of viral DNA polymerases; and (2) incorporation into viral DNA, resulting in eventual termination of viral DNA elongation. Ganciclovir is indicated for the treatment of CMV retinitis in immunocompromised patients, including patients with acquired immunodeficiency syndrome (AIDS) and for the treatment of acute herpetic keratitis.

CNS Activity

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency
0.08 µM [EC50]

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
ZIRGAN
Primary
CYTOVENE
Primary
VALCYTE
Primary
VALCYTE

Cmax

ValueDoseCo-administeredAnalytePopulation
4.8 mg/L
1 g 3 times / day multiple, oral
GANCICLOVIR plasma
Homo sapiens
13.3 μg/mL
5 mg/kg single, intravenous
GANCICLOVIR plasma
Homo sapiens

AUC

ValueDoseCo-administeredAnalytePopulation
35.4 mg × h/L
1 g 3 times / day multiple, oral
GANCICLOVIR plasma
Homo sapiens
53.8 μg × h/mL
5 mg/kg single, intravenous
GANCICLOVIR plasma
Homo sapiens

T1/2

ValueDoseCo-administeredAnalytePopulation
5.2 h
5 mg/kg single, intravenous
GANCICLOVIR plasma
Homo sapiens

Doses

AEs

Overview

CYP3A4CYP2C9CYP2D6hERG

OverviewOther

Other InhibitorOther SubstrateOther Inducer









Drug as victim

Tox targets

PubMed

Sample Use Guides

In Vivo Use Guide
Unknown
Route of Administration: Unknown
In Vitro Use Guide
Unknown
Substance Class Mixture
Record UNII
GCU97FKN3R
Record Status Validated (UNII)
Record Version
All of the following components must be present:
Definition References
(3)