Table 6.
In Vitro Metabolic Stability for Selected Compounds in MLMs
| MLMa | ||
|---|---|---|
| compound ID | T1/2 (min) | CLint (mL/min/mg) |
| 10 (4-F)b | 77.96 | 0.89 |
| 16b (3-F) | 64.07 | 1.02 |
| 16g (4-CF3) | >360 | 0 |
| 16h (3-CF3) | 330 | 0 |
| 16i (4-CN) | >360 | 0 |
| 16m (4-phenyl) | 48.45 | 14.31 |
| 21a (4-F) | >360 | 0 |
| 26a (3-F, 4-Br) | >360 | 0 |
| 29b (4-F) | >360 | 0 |
| 8b/9b | 1.15/12.11 | 208.8/57.26 |
| 4 (enzalutamide) | 10.04 hc | 86.3d |
a
Compounds were incubated together with MLMs with cofactors for phases I and II provided, as described in the Experimental Section.
b
Reported previously in using the same method as in the Experimental Section.1,2
c
T1/2 (h) after oral administration in humans as previously reported in ref. 58
d
CL (mL/h/kg) after oral administration in humans as previously reported.58