Stavudine (d4T, brand name Zerit) is an orally bioavailable nucleoside analog reverse transcriptase inhibitor (NARTI) active against HIV. Stavudine triphosphate inhibits the HIV reverse transcriptase in vitro by competing with natural substrate, thymidine triphosphate. Stavudine also causes termination of DNA replication by incorporating into the DNA strand. In clinical studies, stavudine has excellent oral bioavailability in excess of 80%.
Molecular Weight | 224.21 |
Formula | C10H12N2O4 |
CAS Number | 3056-17-5 |
Solubility (25°C) | DMSO 40 mg/mL Water 20 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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