The estimated t½ and intrinsic clearance (CL) values of TG100435 in pooled human liver microsomes and pooled human cryopreserved hepatocytes in the absence and the presence of 1-aminobenzotriazole, ketoconazole, or a mixture of ketoconazole and methimazole
Liver Microsomes | Hepatocytes | |||||
|---|---|---|---|---|---|---|
| t½ | CL | TG100435 Depletion at 1 h | CL | |||
| min | ml/min/kg | % | ml/min/kg | |||
| No inhibitor | 124 | 2.9 | 32.7 | 3 | ||
| Ketoconazole | 290 | 1.3 | 17.4 | |||
| 1-Aminobenzotrizole | 250 | 1.4 | 16.4 | |||
| Mixture | N.D. | N.D. | 0 |
| ||
N.D., undeterminable.