Table 3.
Summary of 5-hydroxy saxagliptin (major active metabolite of saxagliptin) pharmacokinetic parameters following administration of a single oral dose of saxagliptin 5 mg to healthy subjects with and without rifampicin (600 mg once daily for 6 days)
| Pharmacokinetic parameter | Saxagliptin 5 mg (n = 13) (reference) | Saxagliptin 5 mg with rifampicin 600 mg (n = 13) (test) | Test : reference ratio (%) | 90% CI |
|---|---|---|---|---|
| Cmax (ng ml−1) | ||||
| Geometric mean (CV%) | 49 (25) | 68 (21) | 139 | 123, 156 |
| tmax (h) | ||||
| Median (min, max) | 1.50 (1.00, 2.98) | 1.02 (0.98, 2.98) | NC | NC |
| AUC0–∞ (ng·h ml−1) | ||||
| Geometric mean (CV%) | 258 (17) | 266 (19) | 103 | 97, 109 |
| t1/2 (h) | ||||
| Mean (SD) | 4.32 (0.65) | 3.89 (0.98) | NC | NC |
| Urinary recovery (%) | ||||
| Mean (SD) | 24 (5) | 26 (3) | NC | NC |
| CLR (ml min−1) | ||||
| Geometric mean (CV%) | 77 (24) | 80 (20) | NC | NC |
| Metabolite : parent ratio | ||||
| Geometric mean (CV%) | 3 (24) | 15 (26) | NC | NC |
AUC0–∞, area under the plasma concentration–time curve from time 0 to infinity; CI, confidence interval; CLR, apparent renal clearance; Cmax, maximum plasma concentration; CV%, coefficient of variation %; NC, not calculated; metabolite : parent ratio, (5-hydroxy saxagliptin AUC0–∞ : saxagliptin AUC0–∞) × (315.42/331.42); t1/2, terminal elimination half-life; tmax, time to reach the Cmax.