Table 5.
Peak area ratios for saxagliptin metabolites from the pooled urine samples 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)
| Peak area (counts) | Peak area ratio | Transition | |||
|---|---|---|---|---|---|
| Analyte in urine | Structural description of analyte in urine | Saxagliptin 5 mg (reference) | Saxagliptin 5 mg with rifampicin 600 mg (test) | Test : reference | Multiple reaction monitoring |
| Saxagliptin | Parent | 5 390 000 | 1 290 000 | 0.24 | 316.0/180.0 |
| D1 | Degradant | 8 080 | 2 080 | 0.26 | 316.0/288.0 |
| M1 | Mono-hydroxy | 64 300 | 50 500 | 0.79 | 332.0/196.0 |
| M2 (5-hydroxy saxagliptin) | Mono-hydroxy (major metabolite) | 3 820 000 | 3 460 000 | 0.91 | 332.0/196.0 |
| M3 | Mono-hydroxy | 394 000 | 206 000 | 0.52 | 332.0/196.0 |
| M5 | Di-hydroxy | 31 100 | 130 000 | 4.18 | 348.0/212.0 |
| M8 | Di-hydroxy | 34 700 | 73 300 | 2.11 | 348.0/212.0 |
| M13 | Mono-hydroxy | 3 460 | 4 030 | 1.16 | 332.0/304.0 |
| M16 | Mono-hydroxy | 31 600 | 35 000 | 1.11 | 332.0/196.0 |
| M17 | Di-hydroxy | 15 700 | 40 400 | 2.57 | 348.0/212.0 |
| M19 | Gluc-mono-hydroxy | 2 870 | 3 220 | 1.12 | 508.0/332.0 |
| M27 | Mono-hydroxy-decyanated | 14 200 | 55 300 | 3.89 | 321.0/196.0 |
| M40 | Gluc-mono-hydroxy | 1 340 | 1 360 | 1.01 | 508.0/332.0 |
| M45 | Sulfate-parent | 2 930 | 673 | 0.23 | 396.0/298.0 |
| M46 | Gluc-parent | 14 300 | 3 080 | 0.22 | 492.0/316.0 |
| M49 | Di-hydroxy | 10 400 | 32 600 | 3.13 | 348.0/212.0 |