Table 4.
Summary of plasma DPP-4 % inhibition pharmacodynamic 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)
| Pharmacodynamic parameter | Saxagliptin 5 mg (n = 13) (reference) | Saxagliptin 5 mg with rifampicin 600 mg (n = 13) (test) | Point estimate (90% CI) Ratio of geometric means test : reference |
|---|---|---|---|
| %Imax Mean (SD) | 83.07 (3.50) | 83.22 (2.14) | 1.00 (0.98, 1.03) |
| tmax (effect) (h) Median (min, max) | 2.00 (1.00, 8.00) | 2.00 (1.00, 12.00) | |
| AUEC0–24 (% inhibited·h) Mean (SD) | 1711.61 (71.82) | 1603.97 (111.20) | 0.94 (0.90, 0.97) |
| t1/2 (effect) (h) Mean (SD) | 25.85 (10.64) | 14.46 (4.23) |
AUEC0–24, area under the DPP-4 % inhibition (effect)−time curve from time 0 to the last measured time point 24 h post-dose; CI, confidence interval; %Imax, peak DPP-4 % inhibition; tmax (effect), time to reach peak DPP-4 % inhibition; t1/2 (effect), apparent effect terminal half-life.