Cidofovir (Vistide) is an injectable antiviral medication for the treatment of cytomegalovirus (CMV) retinitis (IC50 = 0.94 μM). Cidofovir suppresses CMV replication by selective inhibition of viral DNA polymerase and therefore prevention of viral replication and transcription.
Antiviral Res. 2020 Apr;176:104754.
Acyclovir, Cidofovir, and Amenamevir Have Additive Antiviral Effects on Herpes Simplex Virus TYPE 1
Cidofovir purchased from AbMole
Cell Experiment | |
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Cell lines | Madin–Darby Canine Kidney or Vero cells |
Preparation method | In vitro efficacy of cidofovir against CHV-1 Madin–Darby Canine Kidney or Vero cells were plated into 96-well plates at 1*104 cells/well and maintained in Dulbecco’s minimal essential medium with 1 g/L glucose, l-glutamine, and sodium pyruvate (Cell Grow; Corning, Manassas, VA) containing 10% fetal bovine serum (Atlanta Biological, Flowery Branch, GA) and penicillin (200 U/mL)/ streptomycin (200 mg/mL) (Life Technologies, Grand Island, NY) for 24 h until confluent. Monolayers were infected with 5 PFU/well CHV-1 (a previously described field strain that was also utilized during the in vivo experimental study evaluating cidofovir) or HSV-1 strain F, respectively. After 2 h of incubation at 37 C, virus supernatants were removed, cells were rinsed once with phosphate-buffered saline (PBS), and 100 mL of sequential 2-fold serial dilutions of cidofovir (starting at 625 mM) was added to each well. Infection controls without cidofovir and noninfected drug-treated controls were also included. Plates were incubated at 37 C until a cytopathic effect (CPE) was visible in the infected nontreated controls, which was *72 hours postinfection (hpi) for CHV-1 and 48 hpi for HSV-1, respectively. Plates were rinsed 3 times with PBS, fixed in 80% ethanol for 10 min at -20 C, and stained with crystal violet (Fisher Scientific, Fair Lawn, NJ). Virusinduced CPE was scored as the percent of wells per dilution with observable plaque formation, and EC50 values were calculated using GraphPad Prism. |
Concentrations | 0~625µM |
Incubation time | 72 hours postinfection (hpi) for CHV-1 and 48 hpi for HSV-1 |
Animal Experiment | |
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Animal models | Recurrent ocular CHV-1 infection in dogs by administration of systemic prednisolone (3.0 mg/kg PO q24 h) for 7 consecutive days beginning on study day 1. |
Formulation | 0.9% sodium chloride solution |
Dosages | 1 drop of 0.5% cidofovir ophthalmic solution |
Administration | eyes drop |
Molecular Weight | 279.19 |
Formula | C8H14N3O6P |
CAS Number | 113852-37-2 |
Solubility (25°C) | DMSO |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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