TABLE 6.
HIV-1 virus | Projected dosec |
Cmin,ss (ng/ml)
|
Equation of protein-corrected EC50 (ng/ml)b | p10/EC50 ratio | |
---|---|---|---|---|---|
Mean | p10e | ||||
Wild type | 75 mg QD | 171.97 | 67.88 | 0.5 × 2 = 1.0 | 68 |
100 mg QD | 229.29 | 90.51 | 91 | ||
150 mg QD | 261.12 | 103.07 | 103 | ||
K103N/Y181C mutant | 150 mg QD | 261.12 | 103.07 | 2.0 × 2 = 4.0 | 26 |
75 mg BID | 392.49 | 173.68 | 43 (65)d | ||
100 mg BID | 523.32 | 231.57 | 58 | ||
150 mg BID | 595.96 | 263.71 | 66 |
Cmin,ss values are projected from simulation and were adjusted downward by 36% for BID dose regimens to account for the overestimation of the Cmin,ss in the model. p10, 10th percentile.
The serum shift factor is twofold. EC50 values are from in vitro data.
Each dose regimen is accompanied by 100 mg RTV QD (QD regimens) or 100 mg BID RTV (BID regimens).
The value in parentheses is the 25th percentile for 75 mg BID.
p10, 10th percentile of the projected plasma concentration.