Table 4

Midazolam hydroxylation phenotype as a function ofCYP3A5 genotype

All GenotypesCYP3A54-1501/4-1501CYP3A54-1501/4-1503CYP3A54-1503/4-1503
Liver microsomal activity(n  =  60)(n  =  1)(n  =  13)(n  =  36)
 1′-Hydroxylation (pmol/min/mg)880   (174–4842)44431893 (505–4842)660  (174–3597)4-160
 4-Hydroxylation (pmol/min/mg)148   (26–850)  502294 (40–850)124  (26–699)
 1′-/4-Hydroxymidazolam ratio6.1  (4.8–13.5)  8.96.4  (5.7–13.5)5.4  (4.8–6.8)
 Total activity (pmol/min/mg)1026   (200–5692)48442188 (545–5692)787  (317–4348)4-150
Jejunal homogenate activity(n  =  31)(n  =  2)(n  =  2)(n  =  27)
 1′-Hydroxylation (pmol/min/mg)148   (28–348)295  (278,311)65.5  (41,90)148  (28–348)
 4-Hydroxylation (pmol/min/mg)26.1  (2–60.6)35.9  (29.3,42.5)5.8  (4.8,6.8)26.1  (2–60.6)
 1′-/4-Hydroxymidazolam ratio6.8  (4.0–13.1)8.4  (7.3,9.5)10.9  (8.6,13.1)6.3  (4.0–7.9)
 Total activity (pmol/min/mg)173   (30–409)330  (307,353)71.0  (46,96)173  (30–409) 

Data are reported as median (range).

    • 4-150p < 0.01 comparingCYP3A5*1 carriers and CYP3A5*3/*3individuals.

    • 4-160p < 0.001 comparing CYP3A5*1carriers and CYP3A5*3/*3 individuals