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. 2012 Dec;40(12):2221–2230. doi: 10.1124/dmd.112.048298

TABLE 1.

Comparison of metabolic ratios of CYP3A5 and its mutants with those of CYP3A4

The enzymes indicated were transiently expressed in COS-7 cells. Metabolism experiments for maraviroc were performed, and oxidative metabolites M1, M2, and M3 were measured as described under Materials and Methods. Metabolic ratios (M1/M2 and M1/M3) are presented as means ± S.D.

Name M1/M2 M1/M3
CYP3A5 24.4 ± 1.3 30.4 ± 4.2
L57F 11.8 ± 1.2 13.6 ± 1.4
S107P 24.1 ± 2.7 10.9 ± 4.0
L108F 1.29 ± 0.05 1.7 ± 0.03
F146V 20.0 ± 2.9 25.6 ± 4.0
G186S 25.4 ± 1.5 38.9 ± 3.2
S206N 34.0 ± 2.1 47.6 ± 3.6
G214D 6.14 ± 0.2 4.6 ± 0.03
L219F 17.9 ± 0.4 16.7 ± 0.1
S239C 27.3 ± 4.0 42.3 ± 3.9
L240V 13.3 ± 6.3 14.9 ± 4.9
V369I 18.2 ± 4.5 25.1 ± 2.8
I371M 20.3 ± 2.8 15.0 ± 1.5
S392V 22.5 ± 0.1 18.8 ± 2.3
T478L 25.6 ± 2.7 38.1 ± 2.7
Q479G 25.6 ± 2.2 23.4 ± 1.1
CYP3A4 1.5 ± 0.5 1.6 ± 0.8