Drug intelligence / Profile preview

valganciclovir + ganciclovir

Development stage
Unknown
Lead developer
Roche
Modality
Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
Administration
Oral, Intravenous
01

Overview

Valganciclovir + ganciclovir is a combination of two antiviral drugs used primarily for the prevention and treatment of cytomegalovirus (CMV) infections, especially in immunocompromised patients such as those undergoing organ or stem cell transplantation. Valganciclovir is an oral prodrug that is rapidly converted to ganciclovir in the body, providing higher oral bioavailability compared to direct oral administration of ganciclovir. Both drugs act as acyclic guanine nucleoside analogues and inhibit viral DNA synthesis by being phosphorylated within infected cells to their active triphosphate forms, which then competitively inhibit viral DNA polymerase, leading to chain termination and inhibition of viral replication[6][7][8]. This combination may be considered in clinical scenarios where both intravenous (ganciclovir) and oral (valganciclovir) routes are needed or when transitioning between formulations for optimal management of CMV infection[1][3]. The primary indications include prophylaxis and treatment of CMV disease in transplant recipients and other high-risk populations.

Brand names
ValcyteCytovene
Other names
Valganciclovir/Ganciclovir
02

Targets

Human cellular DNA polymeraseUL97 (HCMV UL97 kinase)DNA polymerase familyCMV DNA polymerase (Human cytomegalovirus DNA polymerase)HSV DNA pol (Herpes simplex virus DNA polymerase)

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