Cidofovir is an injectable antiviral medication for the treatment of cytomegalovirus (CMV) retinitis, which suppresses virus replication by selective inhibition of viral DNA synthesis.
Cidofovir is a synthetic nucleotide analog with potent antiviral activity against a wide range of herpes viruses. Cidofovir dihydrate (1-((S)-3-Hydroxy-2-(phosphonomethoxy)propyl) cytosine dihydrate) is the active intracellular metabolite of cidofovir that can inhibit cytomegalovirus DNA polymerase[1]. In A549 cells, the analysis of 50% inhibitory dose (ID50) of cidofovir dihydrate in different strains and serotypes of adenovirus showed that the mean ID50 values for Ad5 wide-type, Ad5 McEwen, Ad14 and Ad8 are 9.5, 7.3, 5.4, and 4.7 μg/mL, respectively[2]. In MRC-5 cells, the ED50 values of cidofovir dihydrate against Hmc wild type, SC16, BW-S, BW-R, MS wild type are 6.5 ± 2.5, 9.3 ± 1.8, 8.5 ± 1.0, 1.1 ± 0.9, and 9.1 ± 1.8 μM, respectively[3].. A graded decrease in the severity of acute conjunctivitis was observed in rabbits received the treatment of 0.1% cidofovir dihydrate, whereas the concentrations at 0.5% and 1% caused a moderate grade of acute conjunctivitis. A significantly reduction in Ad5 ocular titers was shown in 0.5% and 1% cidofovir dihydrate-treated groups compared to the placebo group. The duration of viral ocular shedding in 0.1%, 0.5%, and 1% cidofovir dihydrate-treated groups were 6, 4, and 4 days, compared to 7-day duration in placebo group. The mean ELISA antibody titer was decreased by 0.5% and 1% cidofovir dihydrate 21 days post the inoculation[2].
作用机制
Cidofovir dihydrate is the active form of cidofovir and it inhibits viral DNA polymerases as an acyclic nucleoside phosphonate[2].
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