TABLE 1

EC₅₀, E_max, F₂, and percentage of positive control (% PC) rifampicin response obtained with CYP3A4 mRNA expression induction data from three lots of human hepatocytes

Test Drug	Test Concentration Range	Lot 295				Lot 312				Lot 318
Test Drug	Test Concentration Range	EC₅₀	E_max	F₂	% PC	EC₅₀	E_max	F₂	% PC	EC₅₀	E_max	F₂	% PC
	μM	μM	Fold	μM		μM	Fold	μM		μM	Fold	μM
Rifampicin	0.01–50	0.12	7.3	0.046	100	1.4	16	0.20	100	0.44	7.4	0.11	100
Phenytoin	0.23–500	14	3.6	7.9	40	13	4.6	12	23	9.5	4.1	8.3	44
Carbamazepine	0.23–500	17	4.4	13	52	27	6.4	9.3	28	4.3	14	2.5	218
Phenobarbital	0.91–2000	237	7.2	116	96	83	6.1	14	34	138	8.3	78	106
Troglitazone	0.03–20	4.4	10	0.75	139	1.0	3.7	0.48	20	5.7	5.1	3.2	59
Terbinafine	0.05–100	2.6	3.4	1.3	39	2.2	3.1	1.3	14	8.6	2.8	6.3	27
Pleconaril	0.05–100	2.9	1.4	18	6	3.4	3.0	2.7	13	6.4	1.9	11	12
Sulfinpyrazone	0.09–200	13	14	3.1	186	28	19	3.1	119	8.2	5.8	3.1	69
Probenecid	0.05–300	39	4.6	32	56	123	9.2	78	55	77	6.6	29	80
Pioglitazone	0.05–100	2.9	1.8	4.1	13	3.9	3.5	3.3	17	3.5	3.2	3.2	31
Dexamethasone	0.11–250	31	8.4	18	114	22	7.4	14	44	25	3.8	15	41
Rosiglitazone	0.05–100	8.5	4.1	3.4	47	7.8	7.5	2.7	44	10	7.3	5.0	90
Omeprazole	0.05–100	8.0	1.9	6.5	13	4.8	2.8	3.5	12	NA	2.2	NA	17
Clotrimazole	0.005–10	3.3	7.8	1.6	104	2.6	6.3	1.1	36	4.1	5.3	3.5	62
Nifedipine	0.05–100	8.0	7.7	3.2	104	13	5.7	8.8	32	6.3	3.3	4.4	33
Flumazenil	0.023–50	NI	NI	22	NA	23	2.5	25	10	NI	NI	NI	NI
Quinidine	0.11–250	11	1.5	11	7	15	6.9	8.04	31	NA	NA	NA	24
Primaquine	0.04–40	NI	NI	NI	NI	NI	NI	NI	NI	NI	NI	NI	NI
Methotrexate	0.2–20	NI	NI	NI	NI	NI	NI	NI	NI	NI	NI	NI	NI
Digoxin	0.0002–0.2	NI	NI	NI	NI	NI	NI	NI	NI	NI	NI	NI	NI

NA, not applicable, insufficient response for a reliable estimate; NI, no induction was found at the concentrations tested.