TABLE 1.
Inhibitory effects of TBI-166 on human CYP activity determined by in vitro screening.
| C max (μg/mL), p.o. dosage a | Inhibition, IC50 (μM) a | |
|---|---|---|
| CYP1A2 | 0.70 (1.19 μM, Cmax observed at human equivalent dose of 20 mg) | 0.55 |
| CYP2A6 | 1.38 | |
| CYP2B6 | 4.35 | |
| CYP2C8 | >50 | |
| CYP2C9 | 5.45 | |
| CYP2C19 | 4.49 | |
| CYP2D6 | 1.60 | |
| CYP2J2 | >50 | |
| CYP2E1 | 0.93 | |
| CYP3A4 MDZ | 17.36 | |
| CYP3A4 TEST | 2.65 |
a
Positive controls: for CYP1A2, α-naphthoflavone (IC50), 0.33 µM; for CYP2C9, sulfaphenazole (IC50), 0.40 µM; for CYP2C19, nootkatone (IC50), 48.41 µM; for CYP2D6, quinidine (IC50), 0.017 µM; for CYP3A4 (MDZ), ketoconazole (IC50), 0.18 µM; CYP3A4 (TEST), ketoconazole (IC50), 0.45 µM. MDZ: midazolam; TEST: testosterone.