TABLE 4

IC₅₀ values for fluvoxamine and ketoconazole against CLZ oxidation pathways, CYP activity ratios, and CYP1A2 genotypes in human livers

Liver	IC₅₀							IC₅₀ Ratio
		Ketoconazole			Fluvoxamine			(Fluvoxamine/Ketoconazole)			CYP Activity Ratio^a	CYP1A2 Alleles
		NorCLZ	CLZ N-Oxide	NorCLZ	CLZ N-Oxide	NorCLZ	CLZ N-Oxide				CYP Activity Ratio^a	CYP1A2 Alleles
	μM
HL12	11	0.33	9.6	195	0.87	590	14.7
HL16	96	4.2	1.3	110	0.012	26	18.2
HL21	0.55	4.2	54	72	98	17	4.7	^* 1C, ^* 1D
HL22	0.61	0.16	58	55	95	344	3.0
HL24	0.35	0.23	61	116	174	504	4.2
HL27	1.2	0.68	4	>250	3.3	N.D.	13.0	^* 1F
HL28	18	6.8	5.6	>250	0.31	N.D.	23.5
HL29	45	0.34	7.9	66	0.18	194	14.9	^* 1F
HL30	3.7	2.6	100	55	27	21	11.1
HL35	2.5	0.28	66	>250	26	N.D.	11.2
HL36	65	2.0	21	14	0.32	7.0	14.2
HL37	33	3.3	16	73	0.49	22	20.7	^* 1D
HL38	130	1.6	66	66	0.51	41	13.1
HL40	52	1.3	1.9	160	0.037	123	10.3

N.D., not determined
↵ a Ratio of EROD/testosterone 6β-hydroxylation activities in microsomal fractions (Table 1)