TABLE 5

Relative contributions of cytochrome P450 enzymes to tropifexor oxidative metabolism in HLM using cytochrome P450–selective chemical inhibition

Enzyme	Inhibition	CL_int	Experimental fm	Corrected fm_CYP^a	Normalized fm_CYP^b
		ml/h per mg protein	%
	No inhibition	0.223
CYP2C8	Montelukast (2 µM)	0.145	34.9	12.8	15
CYP2C9	Sulfaphenazole (5 µM)	0.209	6.07	−1.16	0^c
CYP3A	Ketoconazole (1 µM)	0.0577	74.1	72.6	85

^aExperimental fm_CYP was corrected with inhibitor crossreactivity as described in the Materials and Methods. ^bCorrected fm_CYP was normalized to a total of 100%.
^cNegative fm_CYP values after correction were considered to be analytical artifacts and set as 0.