Ganciclovir (hydrate)

Ganciclovir (BW 759) hydrate, a nucleoside analogue, is an orally active antiviral agent with activity against CMV. Ganciclovir hydrate also has activity in vitro against members of the herpes group and some other DNA viruses. Ganciclovir hydrate inhibits the in vitro replication of human herpes viruses (HSV 1 and 2, CMV) and adenovirus serotypes 1, 2, 4, 6, 8, 10, 19, 22 and 28. Ganciclovir hydrate has an IC₅₀ of 5.2 μM for feline herpesvirus type-1 (FHV-1) and can diffuse into the brain^[1][2][3]. In Vitro:Ganciclovir (BW 759) is an acyclic deoxyguanosine analog structurally similar to acyclovir but with superior activity against CMV. The median Ganciclovir concentration required to inhibit viral replication by 50 percent is 2.15 μM versus 72 μM for acyclovir^[4].
The primary mechanism of Ganciclovir action against CMV is inhibition of the replication of viral DNA by ganciclovir-5'-triphosphate (ganciclovir-TP). This inhibition includes a selective and potent inhibition of the viral DNA polymerase. Ganciclovir is metabolized to the triphosphate form by primarily three cellular enzymes: a deoxyguanosine kinase induced by CMV-infected cells; guanylate kinase; and phosphoglycerate kinase^[5]. In Vivo:Ganciclovir (BW 759) (50 mg/kg; i.p.; twice a day for five injections) significantly decreases white blood cells, red blood cells and platelets in newborn mice, and can diffuse into the brain and the perilymphatic space of the inner ear^[3].
Ganciclovir (1-80 mg/kg; i.h.; daily for 5 days) delays murine cytomegalovirus (MCMV)-induced wasting syndrome and mortality^[6].