Table 2.
Test species | Drug dosage | Population | Frequencya | Food | PK sampling dose | n |
Cmax (μg/ml) |
AUC0–24 (mg · h/liter) |
t1/2 (h) |
|||
---|---|---|---|---|---|---|---|---|---|---|---|---|
Median | Range | Median | Range | Median | Range | |||||||
Guinea pig | 50 mg/kg | Healthy | D1 | Yes | Single | 3 | 3.16 | 2.35–3.89 | 30.25 | 23.52–45.85 | 15.61 | 11.37–21.45 |
Guinea pig | 100 mg/kg | Healthy | D1 | Yes | Single | 6 | 11.58 | 3.55–22.26 | 187.50 | 67.32–297.90 | 21.87 | 9.05–41.03 |
Mouseb | 10 mg/kg | Healthy | D1 | Yes | Single | 6 | 19.26 | 18.05–21.92 | 321.49 | 292.46–354.43 | 20.56 | 15.24–22.66 |
Mousec | 10 mg/kg | Healthy | D1 | Yes | Single | 3 | 28.23 | 28.14–29.87 | 282.44 | 264.09–304.54 | 25.58 | 18.98–33.63 |
Moused | 10 mg/kg | Healthy | D1 | Yes | Single | 3 | 14.77 | 11.41–15.24 | 237.25 | 236.14–240.20 | 21.65 | 18.98–39.05 |
Mousee | 10 mg/kg | Healthy | SS | Yes | 2 wk | 3 | 18.25 | 17.15–23.68 | 345.08 | 267.14–396.40 | 20.22 | 19.21–20.46 |
Humanf | 600 mg | TB | SS | No | Weekly | 15 | 13.36 | 6.52–25.54 | 182.14 | 104.28–434.88 | 13.86 | 10.33–20.45 |
Humanf | 900 mg | TB | SS | No | Weekly | 7 | 15.14 | 6.57–36.91 | 229.08 | 101.81–504.84 | 16.08 | 11.99–18.91 |
Humanf | 1,200 mg | TB | SS | No | Weekly | 13 | 18.95 | 6.76–54.16 | 286.96 | 95.74–706.79 | 15.30 | 10.50–19.09 |
D1, once daily; SS, steady state.
Data from reference 6.
Data from E. L. Nuermberger, unpublished data.
Data from reference 30.
Data from I. M. Rosenthal, R. Tasneen, C. A. Peloquin, M. Zhang, D. Almeida, K. Mdluli, P. C. Karakousis, J. H. Grosset, and E. L. Nuermberger, submitted for publication.
Data from reference 36.