TABLE 1

Characteristics of the subjects, the parameter values from regression analysis based on a mechanism-based CYP2C8 inhibition model, and the observed maximum fold increase in repaglinide AUC0-∞, when 0.25 mg of repaglinide was given to each subject 1 h after a single 30-, 100-, 300-, or 900-mg dose of gemfibrozil, compared with placebo

Subject no.AgeSexWeightBMICYP2C8 GenotypeSLCO1B1 GenotypeGemfibrozil 1-O-β-Glucuronide Ch,u/Cp,totRepaglinide fm,CYP2C8Repaglinide Maximum AUCi/AUCc
yrkgkg/m2
126Male6421*1/*1*1A/*1A0.3250.8807.7
225Male8426*1/*1*1A/*150.0630.8806.0
325Male6822*1/*1*1A/*1B0.3300.8868.2
421Male6721*1/*1*1A/*1B0.1890.8657.0
524Male6021*1/*1*1A/*1A0.2280.9119.9
620Female6724*1/*1*1A/*1B0.1180.8867.6
724Male8227*1/*1*1A/*150.5010.8978.9
821Male8223*3/*3*1A/*150.2390.91510.8
922Male8825*1/*1*1A/*1A0.5190.8386.0
1022Male7224*1/*3*1B/*150.3340.91511.4
Mean ± S.D.23 ± 273 ± 1023 ± 20.285 ± 0.1490.887 ± 0.0248.4 ± 1.9
  • BMI, body mass index.