Valganciclovir

Valganciclovir is an orally bioavailable prodrug of ganciclovir, a synthetic guanosine nucleoside analogue, primarily used to treat cytomegalovirus (CMV) retinitis in AIDS patients and prevent CMV disease in high-risk transplant recipients.[1][2][4][6] After ingestion, it undergoes rapid hydrolysis by intestinal and hepatic esterases to ganciclovir, achieving ~60% bioavailability—far higher than oral ganciclovir alone.[1][4][9] In CMV-infected cells, viral UL97 kinase phosphorylates ganciclovir to its monophosphate, followed by cellular kinases to the active triphosphate, which competes with dGTP for viral DNA polymerase incorporation, halting viral DNA elongation and replication.[1][2][9] This selective activation in infected cells minimizes impact on host DNA synthesis, though side effects like bone marrow suppression and nephrotoxicity limit use, requiring monitoring.[1][2] Valganciclovir belongs to the ATC class J05AB14 (nucleosides/nucleotides excluding reverse transcriptase inhibitors) and is approved for induction/maintenance therapy in CMV infections.[2][5][1]

Other names

ValcyteL-Valine 2-[(2-amino-1,6-dihydro-6-oxo-9H-purin-9-yl)methoxy]-3-hydroxypropyl esterganciclovir L-valyl esterRo-1079070/194Cymeval

Converted by esterases to ganciclovir; ganciclovir is phosphorylated by viral UL97 protein kinase (in CMV-infected cells) to triphosphate form, which competitively inhibits viral DNA polymerase, incorporates into viral DNA, and causes chain termination