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. Author manuscript; available in PMC: 2022 Feb 12.
Published in final edited form as: J Med Chem. 2021 Jul 16;64(15):11045–11062. doi: 10.1021/acs.jmedchem.1c00439

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
a

Compounds were incubated together with mouse liver microsomes (MLMs) with cofactors for phases I and II provided, as described in the Experimental Section.

b

Reported previously using the same method as in the Experimental Section.38,40

c

T1/2 (h) after oral administration in humans as previously reported in ref 43.

d

CL (mL/h/kg) after oral administration in humans as previously reported.43