Table 1. Pharmacokinetic characteristics of cyclosporine in healthy subjects with different CYP3A4*18B genotypes after 14 days of treatment with placebo or bifendate. bP<0.05 vs placebo group.
| CYP3A4*1/*1 | CYP3A4*1/*18B | CYP3A4*18B/*18B | ||||
|---|---|---|---|---|---|---|
| (n=6) | (n=6) | (n=6) | ||||
| Placebo | Bifendate | Placebo | Bifendate | Placebo | Bifendate | |
| AUC(0–24) (ng·h/mL) | 6826±521 | 6174±610b | 5810±208 | 5159±651b | 6175±505 | 3669±832b |
| AUC(0–∞) (ng·h/mL) | 6927±510 | 6264±630b | 5927±198 | 5308±642b | 6287±562 | 3891±867b |
| Cmax (ng/mL) | 2181±251 | 928±105b | 1998±140 | 795±108b | 870±77 | 546±118b |
| tmax (h) | 1.44±0.17 | 1.66±0.21 | 1.33±0.0 | 1.5±0.26 | 1.77±0.18 | 1.44±0.17 |
| t1/2 (h) | 4.36±0.47 | 4.13±0.50 | 4.38±0.51 | 4.19±0.35 | 4.91±0.59 | 4.55±0.45 |
| CL/F (1/h) | 36.8±2.88 | 40.6±4.41b | 43.1±1.47 | 49.2±6.59b | 40.7±3.36 | 53.7±8.28b |