TABLE 4

EC₅₀ and E_max data for CYP3A4 induction in human hepatocytes HH205 and HH215

	Activity											mRNA
	HH205					HH215					HH205					HH215
Compound	EC₅₀	E_max	E_max	EC₅₀	E_max	E_max	EC₅₀	E_max	E_max	EC₅₀	E_max	E_max
	μM	-fold	% rif	μM	-fold	% rif	μM	-fold	% rif	μM	-fold	% rif
Carbamazepine	40	7.7	39		6.3	63	42	23	30		31	94
CITCO		1.7	9		3.1	31		5.4	7		7.8	24
Clotrimazole		1.9	10		1.7	17		13	17		4.1	12
Dexamethasone	43	8.6	43	12	3.4	34	43	71	93	39	13	39
Efavirenz		2.6	13		6.6	66		5.1	7		22	67
Hyperforin	0.3	3.2	16	0.1	11	110	0.3	12	16	0.3	13.5	41
Lansoprazole	6.8	7.3	37	3.1	6.8	68	6.9	42	55	3.3	8.6	26
Mifepristone		1.1	6		1	10		2	3		1.5	5
Nifedipine		1.8	9		5.1	51		20	26		9.6	29
Omeprazole		1.3	7		2.8	28		21	28		7.1	22
Paclitaxel		4	20	0.3	4.5	45		46	61	2.6	12	36
Phenobarbital	23	14	70		13	130	142	17	22		11	33
Phenytoin	19	16	80	13	11	110	18	15	20	12	12	36
Pioglitazone	8.5	10	50	5	12	120	9.2	18	24	7.2	18	55
Quinidine		0.8	4		0.5	5		9.8	13		7.2	22
Reserpine	0.6	1.4	7		3.8	38	1.9	78	103		24	73
Rifabutin	0.3	3.4	17		6.1	61	1.6	57	75		30	91
Rifampicin	0.6	20	100	0.6	10	100	0.1	76	100	0.4	33	100
Rifapentine	0.9	16	80	0.7	10	100	1.4	109	143	1.2	22	67
Ritonavir		0.3	2		0.5	5		25	33		15	45
β-Naphthoflavone		0.9	5		0.6	6		1.7	2		0.5	2
Sulfinpyrazone	17	7.3	37	1.7	6.8	68	23	103	136	7.2	25	76
Troglitazone		2.4	12	0.2	3.2	32		4	5	0.8	8.7	26
Troleandomycin		2.1	11		1.2	12		27	36		15	45
Verapamil		0.6	3		0.4	4		49	64		29	88

-fold, -fold induction; % rif, percentage CYP3A4 induction of positive control rifampicin.