Stavudine exposures in selected toxicology studies in mice, rats, and rabbits
| Type of Study | Species | Dose5-a | Mean (SD) Parameter Value | |
|---|---|---|---|---|
| Cmax5-b | AUC5-c | |||
| (mg/kg/day) | (μg/ml) | (μg · h/ml) | ||
| Fertility and reproduction | Rat | 100 | 30.5 (3.4) | ND5-d |
| (N = 4) | 300 | 89.3 (7.6) | ND | |
| 600 | 142 (41.7) | ND | ||
| Teratology | Rat | 50 | 16.2 (0.7) | ND |
| (N = 4) | 250 | 93.6 (12.4) | ND | |
| 1000 | 262 (80.2) | ND | ||
| Rabbit | 60 | 11.5 (2.3) | ND | |
| (N = 3) | 300 | 26.3 (16.9) | ND | |
| 600 | 120 (34.5) | ND | ||
| Neurotoxicity (part 1) | Rabbit | 600 | 140 (19.9) | 1245 (737) |
| (N = 3) | 1500 | 427 (1.4) | 3126 (129) | |
| Neurotoxicity (part 2) | Rabbit | 750 | 289 (65.7) | ND |
| (N = 5) | 1500 | 724 (133) | ND | |
| Carcinogenicity5-e | Mouse | 80 | 1.64 | 29.9 |
| (N = 3) | 400 | 5.05 | 92.1 | |
| 2000 | 31.9 | 587 | ||
| Rat | 100 | 4.07 | 79.2 | |
| (N = 3) | 600 | 26.8 | 394 | |
| 2000 | 155 | 1723 | ||
↵5-a Doses were administered by gavage approximately 4 to 6 h apart.
↵5-b Except for the neurotoxicity study, Cmax was sampled at 0.5 h; in the neurotoxicity study, Cmax occurred at 1.0 h.
↵5-c Area under the curve in a 24-h interval.
↵5-d ND, not determined.
↵5-e Standard deviations are missing because composite plasma profiles were obtained; Cmax occurred between 2 and 10 h.