Phase 1
Completed N=24
Bioequivalence Study of Saxagliptin and Glucophage Combination Formulations in Healthy Subjects (A)
Source: ClinicalTrials.gov NCT00899470 ↗Enrolled (actual)
24
Serious AEs
0.0%
Results posted
Mar 2011
Primary outcomePrimary: Saxagliptin Mean Maximum Observed Plasma Concentration (Cmax) — 8.57; 8.61; 11.36; 11.51 ng/mL
Summary
To demonstrate bioequivalence of a 2.5 mg saxagliptin/500 mg metformin (glucophage) immediate release (IR) fixed dose combination (FDC) tablet to the 2.5 mg saxagliptin tablet and 500 mg metformin IR tablet co-administered to healthy subjects in a fasted and in a fed state.
Outcome Measures
| Outcome | Result | p-value |
|---|---|---|
| PRIMARY Saxagliptin Mean Maximum Observed Plasma Concentration (Cmax) |
8.57; 8.61; 11.36; 11.51 | — |
| PRIMARY Saxagliptin Mean Area Under the Plasma Concentration Time Curve From Time Zero To Time of Last Quantifiable Concentration (AUC [0-T]} |
48.57; 49.69; 54.59; 55.83 | — |
| PRIMARY Saxagliptin Mean Area Under the Plasma Concentration Time Curve From Time Zero To Infinity (AUC [0-INF]) |
50.66; 51.74; 56.56; 57.86 | — |
| PRIMARY Saxagliptin Mean Plasma Half-life (T-half) and Mean Time of Maximum Observed Plasma Concentration (T-max) |
5.86; 5.55; 5.75; 5.72; 1.78; 1.23 | — |
| PRIMARY Metformin Mean Cmax |
1030.22; 1042.52; 993.32; 1027.70 | — |
| PRIMARY Metformin Mean AUC (0-T) |
7403.01; 7575.23; 7176.78; 7502.46 | — |
| PRIMARY Metformin Mean AUC(0-INF) |
7494.67; 7689.57; 7246.89; 7574.17 | — |
| PRIMARY Metformin T-half and T-max |
9.87; 12.03; 8.62; 8.61; 3.18; 3.08 | — |
| SECONDARY BMS-510849 Mean Cmax |
16.32; 16.10; 18.40; 18.72 | — |
| SECONDARY BMS-510849 Mean AUC (0-T) |
112.35; 113.87; 120.31; 123.05 | — |
| SECONDARY BMS-510849 Mean AUC (0-INF) |
120.72; 122.74; 129.02; 131.88 | — |
| SECONDARY BMS-510849 Mean T-half and T-max |
6.53; 6.93; 6.73; 6.62; 2.40; 2.30 | — |
| SECONDARY Number of Participants With at Least 1 Adverse Event (AE), Death, Serious AE (SAE), or AEs Leading to Discontinuation |
6; 3; 4; 1; 7; 0 | — |
| SECONDARY Number of Participants With Laboratory Marked Abnormalities |
0; 0; 1; 0; 1; 0 | — |
| SECONDARY Number of Participants With Clinically Relevant Electrocardiogram (ECG) Abnormalities |
0; 0; 0; 0 | — |
| SECONDARY Number of Participants With Clinically Relevant Vital Sign Abnormalities |
0; 0; 0; 0 | — |
| SECONDARY Number of Participant With Clinically Relevant Physical Examination Abnormalities |
0; 0; 0; 0 | — |
Eligibility Criteria
Inclusion Criteria
- Men and women ages 19 to 45 inclusive
- Healthy subjects as determined by no clinically significant deviation from normal in medical history, physical examination, electrocardiograms (ECGs), and clinical laboratory determinations
- Body Mass Index (BMI) of 18 to 32 kg/m2, inclusive. BMI = weight (kg)/ [height (m)]2
Exclusion Criteria
- Women of child-bearing potential (WOCBP) who are unwilling or unable to use acceptable barrier methods (condoms and spermicides) to avoid pregnancy for the entire study period and for up to 8 weeks after the last dose of investigational product
- Any significant acute or chronic medical illness
- Current or recent (within 3 months) gastrointestinal disease
- Any major surgery within 4 weeks of study drug administration
- History of allergy to Dipeptidyl peptidase 4 (DPP4) inhibitor or related compounds
- History of allergy or intolerance to metformin or other similar acting agents
- Prior exposure to saxagliptin
- Prior exposure to metformin within 3 months of study drug administration.
- Estimated creatinine clearance (Clcr) of < 80ml/min using the Cockcroft Gault formula
Data sourced from ClinicalTrials.gov (NCT00899470). Outcome figures and adverse-event rates are extracted automatically from the registry's posted results and are provided for clinician reference, not as a substitute for the primary publication. Informational only — not medical advice.