Table 1

Relative levels of CYP3A4 protein and mRNA, and rates of cyclosporine A oxidation in microsomes prepared from six different human hepatocyte cultures

	FT103	FT105	FT110	FT112	FT113	FT127	Mean ± S.D.
CYP3A4 protein^1-a
UT	8.8	und	und	und	und	und	1.5 ± 3.6
RIF	100	100	100	100	100	100	100
ELT5	N.D.	N.D.	N.D.	N.D.	und	und	und
ELT25	N.D.	34	und	53	und	10	19.3 ± 23.3^1-150
ELT50	76	32	und	100	und	12	36.9 ± 42.4^1-150
CYP3A4 mRNA^1-a
UT	N.D.	N.D.	28	und	19	N.D.	23 ± 10.0
RIF	N.D.	N.D.	100	100	100	N.D.	100
ELT5	N.D.	N.D.	N.D.	N.D.	25	N.D.	25.2
ELT25	N.D.	N.D.	100	65	82	N.D.	82.4 ± 17.5^1-160
ELT50	N.D.	N.D.	127	62	104	N.D.	97.9 ± 32.7^1-160
CSAO^1-a
UT	5.8	19	46	und	20	20	18.4 ± 15.8
RIF	100	100	100	100	100	100	100
ELT5	N.D.	N.D.	N.D.	N.D.	2.0	16	8.9 ± 9.8
ELT25	N.D.	25	25	46	11	25	26.2 ± 12.4^1-165
ELT50	19	50	10	71	20	28	33.0 ± 22.9^1-165

N.D., not determined; und, below level of detection.
↵1-a Relative levels of CYP3A4 protein and mRNA and rates of cyclosporine A oxidation (CSAO) in untreated cells (UT) or in cells treated with 5, 25, or 50 μM eletriptan (ELT), with respect to the corresponding data in RIF-treated cells (arbitrarily taken as 100).
↵1-150 Levels of CYP3A4 protein: in ELT25- and ELT50-treated cells, significantly lower than in RIF-treated cells, P = .0015 and .015, respectively, and in untreated cells, significantly lower than in RIF-treated cells, P < .0001.
↵1-160 Levels of CYP3A4 mRNA: in ELT25- and ELT50-treated cells, significantly greater than in untreated cells, P = .0006 and .01, respectively, and in RIF-treated cells, significantly greater than in untreated cells, P = .02.
↵1-165 Rates of cyclosporine A oxidation: in ELT25- and ELT50-treated cells, significantly lower than in RIF-treated cells, P = .0002 and .0008, respectively, and in untreated cells, significantly lower than in RIF-treated cells, P < .0001. For absolute rates of cyclosporine A oxidation, see Fig.2.