Tomeglovir is a novel nonnucleosidic inhibitor of human cytomegalovirus replication. Tomeglovir is a potent anti-CMV agent, inhibiting processing of viral DNA-concatemers, with IC50s of 0.34 μM and 0.039 μM for HCMV and MCMV.
Tomeglovir (3, 10, 30, 100 mg/kg; p.o.) dose-dependently reduces MCMV-DNA in salivary glands, livers and kidneys of MCMV-infected NOD-SCID mice, and prolongs the survival of the mice. Tomeglovir (10, 25 and 50 mg/kg) shows antiviral activity in the hollow fiber mouse model.
| Molecular Weight | 441.54 |
| Formula | C23H27N3O4S |
| CAS Number | 233254-24-5 |
| Solubility (25°C) | DMSO ≥ 90 mg/mL |
| 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.
[4] Vincent C Emery, et al. Focus on new drugs in development against human cytomegalovirus
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