Selected drugs for ISEF validation
| Drugs | Major Metabolizing Enzyme | Determination of Metabolizing-Enzyme Contribution | Reference |
|---|---|---|---|
| Metoprolol | CYP2D6, 3A4 | Metabolite formation Vmax and Km in HLM | Simcyp |
| Sildenafil | CYP3A4, 2C9 | CLint in rhP450, converted by software | Simcyp |
| Imipramine | CYP2D6, 2C19 | Metabolite formation Vmax and Km in HLM | Simcyp |
| Carbamazepine | CYP3A4 | Metabolite formation in HLM with inhibitory antibody | Kerr et al. (1994) |
| Rosiglitazone | CYP2C8, 2C9 | CLint in HLM with chemical inhibitors | Simcyp |
| Mirtazapine | CYP1A2, 2D6, 3A4 | Metabolite formation Vmax and Km in rhP450 and extrapolated using RAF and HLM with inhibitors | Störmer et al. (2000a,b) |
| Omeprazole | CYP2C19, 3A4 | Metabolite formation Vmax and Km in rhP450 | Simcyp |
| Fluoxetine | CYP2D6, 2C9, 3A4 | Metabolite formation Vmax and Km in rhP450 scaled using P450 content and HLM with chemical inhibition | Margolis et al. (2000) |
| Tolterodine | CYP2D6, 3A4 | Metabolite formation Vmax and Km in HLM | Simcyp |
| Harmine | CYP1A2, 2C9, 2D6 | Metabolite formation in HLM with monoclonal antibodies | Yu et al. (2003) |