Ganciclovir (GCV)

Ganciclovir is a synthetic purine nucleoside analog of 2'-deoxyguanosine that exhibits potent activity against members of the herpesvirus family, most notably Cytomegalovirus (CMV) (PubChem). It is primarily indicated for the treatment of CMV retinitis in immunocompromised patients and for the prevention of CMV disease in transplant recipients (FDA). The molecule functions as a prodrug, requiring initial activation via phosphorylation by the viral protein kinase UL97 in CMV-infected cells, followed by conversion to the active triphosphate form by cellular kinases (StatPearls). Once activated, ganciclovir triphosphate competitively inhibits the incorporation of deoxyguanosine triphosphate into viral DNA by viral DNA polymerase, leading to the termination of viral DNA elongation (NIH). Despite its clinical utility, ganciclovir is associated with significant, dose-limiting myelosuppression and potential reproductive toxicity, requiring careful hematological monitoring and renal dose adjustments (Wikipedia).

Other names

9-(1,3-dihydroxy-2-propoxymethyl)guanine2'-Deoxy-2'-(hydroxymethyl)guanosineDHPGBW 759UCytoveneVitrasert

Ganciclovir is a prodrug that is first phosphorylated to ganciclovir monophosphate by a viral kinase (UL97 in cytomegalovirus or thymidine kinase in herpes simplex virus); it is then further phosphorylated by host cell kinases to ganciclovir triphosphate, which acts as a competitive inhibitor of viral DNA polymerase and is incorporated into the viral DNA strand, causing premature chain termination.