Adefovir Dipivoxil reduces Liver HBV DNA to <0.1 pg of viral DNA per mg of total DNA (pg/mg) in transgenic mice expressing hepatitis B virus. Adefovir Dipivoxil treatment also reduces serum HBV DNA to 3.5 log10 genomic equivalents (ge)/mL in transgenic mice expressing hepatitis B virus compared to 5.3 log10 ge/mL for the placebo control group. Adefovir Dipivoxil antiviral activity reaches near maximum viral reduction by day 10 in the liver and reaches an endpoint of liver virus inhibition at 1.0 mg/kg/day. Adefovir Dipivoxil works by blocking reverse transcriptase, an enzyme that is crucial for the hepatitis B virus (HBV) to reproduce in the body. Adefovir Dipivoxil is used for treatment of hepatitis B and herpes simplex virus infection.
| Molecular Weight | 501.47 |
| Formula | C20H32N5O8P |
| CAS Number | 142340-99-6 |
| Solubility (25°C) | DMSO 100 mg/mL Water <1 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.
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Azvudine (RO-0622) hydrochloride is a potent nucleoside reverse transcriptase inhibitor (NRTI), with antiviral activity on HIV, HBV and HCV. Azvudine hydrochloride exerts highly potent inhibition on HIV-1 (EC50s ranging from 0.03 to 6.92 nM) and HIV-2 (EC50s ranging from 0.018 to 0.025 nM). Azvudine hydrochloride inhibits NRTI-resistant viral strains. |
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