Parameter | Rat | Dog | Human | ||||
---|---|---|---|---|---|---|---|
Oral | IV | ||||||
Male | Female | Male | Female | Oral | IV | Oral | |
Total 14C | |||||||
Cmax(μg eq/ml) | 1.43 | 3.70 | 3.86 | 5.02 | 18.82 | 20.43 | 14.0 |
Tmax (hr) | 6 | 8 | 0.1 | 0.1 | 1 | 0.1 | 4.4 |
AUC (μg eq · hr/ml) | 12.68 | 30.73 | 6.59 | 9.47 | 151.6 | 48.13 | 135.0 |
[14C]Ritonavir | |||||||
Cmax (μg eq/ml) | 1.43 | 3.70 | 3.84 | 5.02 | 17.91 | 20.02 | 13.70 |
Tmax (hr) | 6 | 8 | 0.1 | 0.1 | 1 | 0.1 | 4.4 |
AUC (μg eq · hr/ml) | 12.68 | 30.73 | 3.85 | 5.10 | 71.09 | 22.83 | 95.64 |
M-1 | |||||||
Cmax (μg eq/ml) | — | — | 0.08 | 0.037 | 0.70 | 1.17 | — |
Tmax(hr) | — | — | 2 | 1.5 | 1 | 3 | — |
AUC (μg eq · hr/ml) | — | — | 0.06 | 0.03 | 3.34 | 2.64 | — |
M-2 | |||||||
Cmax (μg eq/ml) | — | — | — | — | 0.28 | 0.22 | 0.67 |
Tmax(hr) | — | — | — | — | 3 | 1.5 | 8.8 |
AUC (μg eq · hr/ml) | — | — | — | — | 0.97 | 0.32 | 3.19 |
G-1 | |||||||
Cmax (μg eq/ml) | — | — | — | — | 0.13 | 0.26 | — |
Tmax(hr) | — | — | — | — | 1–2 | 0.5 | — |
AUC (μg eq · hr/ml) | — | — | — | — | 0.33 | 0.34 | — |
All total radioactivity values were determined over a 0–72 hr (rat and dog) or 0–24 hr (human) plasma time course. All values of [14C]ritonavir and metabolites were determined over a 0–2 (rat) or 0–3 (dog) hr plasma time course after intravenous dosing and a 0–8 (rat), 0–6 (dog) and 2–12 (human) hr plasma time course after oral dosing.
— = metabolite not detected.