Mean pharmacokinetic parameters for saxagliptin, M2, and radioactivity after administration of a single oral dose of [14C]saxagliptin
| PK Parameter | Saxagliptin | M2a | Radioactivity |
|---|---|---|---|
| Cmax, ng/ml | 279 | 606 | 779 |
| Mean, %CV | (13) | (11) | (10) |
| AUC(INF), ng · h/ml | 845 | 2943 | 3874 |
| Mean, %CV | (17) | (7) | (9) |
| Tmax, h | 0.50 | 1.50 | 1.50 |
| Median (min, max) | (0.25, 0.50) | (1.00, 2.00) | (1.00, 1.50) |
| T-HALF, h | 2.45 | 2.69 | 2.77 |
| Mean (S.D.) | (0.31) | (0.31) | (0.22) |
| CLR, ml/min | 234 | 102 | 165 |
| Mean (S.D.)b | (23) | (10) | (14) |
| %Urinary excretion | 23.5 | 35.7 | 74.9 |
| Mean (S.D.)b | (3.1) | (3.0) | (5.1) |
| %Fecal excretion | 0.5 | 8.4 | 22.1 |
| Mean (S.D.) | (N.A.)c | (N.A.)c | (9.5) |
%CV, percentage coefficient of variation; N.A., not applicable.
↵a Values reported for M2 may include small amounts of other hydroxylated metabolite isomers.
↵b n = 5; CLR and urinary excretion values do not include data for subject 6.
↵c Determined via biotransformation profiling of pooled 0- to 168-h urine or fecal samples; therefore, S.D. was not determined.