Table 3. CYP Inhibition Activity of TG8-260 (2f) in Pooled Human Liver Microsomesa.
| CYP IC50 (μM) |
|||||||
|---|---|---|---|---|---|---|---|
| compound | 1A2 | 2B6 | 2C8 | 2C19 | 2D6 | 3A4 (M or T) | 3A4 (T) |
| TG8-260 (2f) | >100 | <0.046 | 0.2 | <0.046 | 0.09 | 0.7 | 0.9 |
| TG8-242 (2c) | ND | ND | ND | ND | >3b (0% at 3 μM) | >3 (18% at 3 μM) | ND |
| TG10-251(2i) | ND | ND | ND | ND | >3b (30% at 3 μM) | >3 (0% at 3 μM) | ND |
a
Studies were carried out at (CROs) AMRI Laboratories, Rochester, NY.
b
Studies were carried out at Sai-Life Laboratories (India). CYP3A substrates were midazolam (M) or testosterone (T, testosterone).