TABLE 2.
Observed RTV dispositions in combination with each concomitant PI and comparison between RTV and concomitant PI effect on viral protease
| Parameter | Median (interquartile range) for concomitant PI |
||||
|---|---|---|---|---|---|
| ATV | DRV600a | DRV800b | LPV | TPV | |
| No. of samples | 40 | 22 | 4 | 21 | 16 |
| RTV intra-PBMC concn (μM) | 0.90 (0.61–1.40) | 2.96 (1.82–4.95) | 1.45 (1.16–4.47) | 2.60 (1.86–3.76) | 1.65 (0.93–2.30) |
| RTV plasma concn (μM) | 0.09 (0.06–0.19) | 0.48 (0.26–0.55) | 0.17 (0.14–0.61) | 0.39 (0.22–0.65) | 0.38 (0.20–0.70) |
| RTV intra-PBMC/plasma ratio | 9.07 (5.97–12.83) | 7.59 (6.20–9.97) | 7.561 (6.60–11.11) | 7.21 (5.71–10.45) | 5.27 (3.12–6.39) |
| Intracellular [RTV]/[PI] | 0.42 (0.29–0.64) | 4.04 (2.48–8.03) | 2.49 (1.49–5.35) | 0.57 (0.29–0.76) | 0.19 (0.13–0.25) |
| [I]/Ki (RTV)/[I]/Ki (PI) (high RTV Ki) | 0.35 (0.24–0.54) | 0.59 (0.36–1.17) | 0.36 (0.22–0.78) | 0.05 (0.03–0.07) | 0.19 (0.13–0.25) |
| [I]/Ki (RTV)/[I]/Ki (PI) (mean RTV Ki) | 0.49 (0.36–0.80) | 0.91 (0.61–2.24) | 0.53 (0.32–1.14) | 0.07 (0.06–0.10) | 0.29 (0.25–0.37) |
| Reaction speed ratio with/without RTV | 0.74 (0.65–0.80) | 0.63 (0.46–0.74) | 0.74 (0.57–0.82) | 0.95 (0.94–0.96) | 0.84 (0.80–0.88) |
| Fraction of antiviral effect accounted for by RTV (%) | 26 (20–35) | 37 (26–54) | 26 (18–43) | 5 (4–6) | 16 (12–20) |
a
DRV600, DRV-RTV 600 and 100 mg BID.
b
DRV800, DRV-RTV 800 and 100 mg QD.