Table 5.
Single compartment first order elimination PK parameters for cyclopropavir (5) after IV dosing of prodrug (6) in mice. The last three data points were used to model the elimination rate constant.a
| Parameter | Best Fit |
|---|---|
| Rate constant of elimination phase, β, min.−1 | 0.0092 |
| Half-life based on termin.al elimination phase, T1/2(β), min. | 75.5 |
| Time of maximum plasma concentration, Tmax, min. | 10 |
| Maximum plasma concentration, Cmax, mg/L | 5.59 |
| Volume of distribution based on the termin.al phase, Vz, L | 1.94 |
| Area under the curve at infinity, AUC∞, mg.min/L | 902 |
| Total plasma clearance (Cl), L/min. | 0.018 |
a
In this analysis a complete conversion of the prodrug (6) to cyclopropavir (5) was assumed, which would result in a equivalent dose of cyclopropavir (5) of 16.2 mg/kg.