Mean ± SD pharmacokinetic parameters1-a for drug-related material, delavirdine, and desalkyl delavirdine after single oral dose administration of [14C-carboxamide]delavirdine mesylate
| Dose (mg/kg) | Sex/N | Analyte1-b | AUC1-c (μM/hr) | Cmax (μM) | tmax(hr) | t1/2 (hr) |
|---|---|---|---|---|---|---|
| 10 | M /3 | DRM | 123 | 13.5 ± 4.4 | 0.5 | 7.3 |
| DLV | 1.01 | 0.81 ± 0.40 | 0.5 | 0.81 | ||
| Desalkyl DLV | 97.5 | 10.8 ± 0.3 | 3.0 | 7.4 | ||
| 10 | F /3 | DRM | 120 | 12.5 ± 3.3 | 0.5 | 7.2 |
| DLV | 1.01 | 1.25 ± 0.45 | 0.5 | 0.84 | ||
| Desalkyl DLV | 115 | 9.15 ± 2.16 | 2.0 | 8.0 | ||
| 250 | M /3 | DRM | 2640 | 247 ± 60 | 2.0 | 6.5 |
| DLV | 288 | 108 ± 35 | 1.0 | 1.9 | ||
| Desalkyl DLV | 1920 | 178 ± 22 | 2.0 | 8.8 | ||
| 250 | F /3 | DRM | 3330 | 228 ± 45 | 4.0 | 5.7 |
| DLV | 389 | 103 ± 42 | 1.0 | 3.2 | ||
| Desalkyl DLV | 2440 | 168 ± 63 | 4.0 | 6.6 |
↵1-a Pharmacokinetic parameters were determined from dose normalized mean concentrations. Pharmacokinetic parameters for individual mice and SD for mean data could not be calculated since only one blood draw per mouse could be obtained.
↵1-b DRM, drug-related material; DLV, delavirdine.
↵1-c AUC(0–48) for DRM, DLV, and desalkyl DLV.