Amprenavir is an human immunodeficiency virus (HIV) protease inhibitor with IC50 of 14.6 ?12.5 ng/ml for wild-type HIV isolates. Like all HIV protease inhibitors, amprenavir interrupts the maturation phase of the HIV replicative cycle by forming an inhibitor-enzyme complex, which prevents HIV protease from binding with its normal substrates. It has an enzyme inhibition constant (Ki = 0.6 nM) that falls within the Ki range of the other protease inhibitors.
Molecular Weight | 505.63 |
Formula | C25H35N3O6S |
CAS Number | 161814-49-9 |
Solubility (25°C) | DMSO 10 mg/mL Ethanol 100 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.
[2] Brian M Sadler, et al. Clinical pharmacology and pharmacokinetics of amprenavir
[3] S Noble, et al. Amprenavir: a review of its clinical potential in patients with HIV infection
[4] H B Fung, et al. Amprenavir: a new human immunodeficiency virus type 1 protease inhibitor
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