Table 3.
In Vitro Metabolic Stability for Selected Compounds in Mouse Liver Microsomes (MLMs)
| (DMPK) MLMa | ||
|---|---|---|
| compound ID | T1/2 (min) | CLint (mL/min/mg) |
| 11 b | 1.15 | 208.8 |
| 12 b | 12.11 | 57.26 |
| 13 b | 77.96 | 0.89 |
| 19c | 24.61 | 28.16 |
| 19e | 26.51 | 41.58 |
| 26a | 3.96 | 157.5 |
| 26b | 17.93 | 38.66 |
| 26e | 5.07 | 136.8 |
| 26f | 265 | 2.67 |
| 26h | >360 | ~0 |
| 5 (enzalutamide) | 10.04 hc | 86.3d |
Compounds were incubated together with mouse liver microsomes (MLMs) with cofactors for phases I and II provided, as described in the Experimental Section.
Reported previously using the same method as in the Experimental Section.38,40
T1/2 (h) after oral administration in humans as previously reported in ref 43.
CL (mL/h/kg) after oral administration in humans as previously reported.43