Phase 1
Completed N=24
Bioequivalence Study of Fixed Dose Combination of 2.5 mg Saxagliptin/850 mg Metformin Tablet Relative to 2.5 mg Onglyza and 850 mg Glucophage Tablets Co-Administered
Source: ClinicalTrials.gov NCT01068743 ↗Enrolled (actual)
24
Serious AEs
0.0%
Results posted
Feb 2012
Primary outcomePrimary: Saxagliptin Pharmacokinetic (PK) Parameter Area Under the Plasma Concentration Versus Time Curve From Time 0 Extrapolated to Infinity (AUC[0-inf]) — 49.23; 49.94; 52.50; 53.15 ng*hr/mL
Summary
To demonstrate bioequivalence of a 2.5 mg saxagliptin/850 mg metformin fixed dose combination (FDC) tablet relative to the 2.5 mg saxagliptin tablet and 850 mg metformin (Glucophage Marketed by Merck-Serono) tablet co-administered to healthy subjects in the fasted and fed condition.
Outcome Measures
| Outcome | Result | p-value |
|---|---|---|
| PRIMARY Saxagliptin Pharmacokinetic (PK) Parameter Area Under the Plasma Concentration Versus Time Curve From Time 0 Extrapolated to Infinity (AUC[0-inf]) |
49.23; 49.94; 52.50; 53.15 | — |
| PRIMARY Saxagliptin PK Parameter Observed Maximum Plasma Concentration (Cmax) |
9.73; 9.97; 10.25; 10.88 | — |
| PRIMARY Metformin PK Parameter AUC(0-inf) |
11998.00; 12271.61; 11988.30; 11838.11 | — |
| PRIMARY Metformin PK Parameter Cmax |
1724.38; 1715.79; 1571.21; 1541.76 | — |
| SECONDARY 5-hydroxy Saxagliptin PK Parameter AUC(0-inf) |
118.58; 119.54; 121.99; 125.54 | — |
| SECONDARY 5-hydroxy Saxagliptin PK Parameter Cmax |
16.83; 16.72; 17.35; 18.59 | — |
| SECONDARY 5-hydroxy Saxagliptin PK Parameter Area Under the Plasma Concentration Versus Time Curve From Time 0 to the Time of the Last Quantifiable Concentration (AUC[0-t]) |
109.60; 110.61; 113.15; 117.04 | — |
| SECONDARY 5-hydroxy Saxagliptin PK Parameter Terminal Half-life (T 1/2) |
7.58; 7.58; 7.48; 7.22 | — |
| SECONDARY 5-hydroxy Saxagliptin PK Parameter Time to Achieve the Observed Maximum Plasma Concentration (Tmax) |
2.21; 1.86; 2.65; 2.46 | — |
| SECONDARY Safety: Adverse Events (AEs), Discontinuations Due to AEs, Deaths, and Serious AEs (SAEs). |
4; 5; 3; 4; 1; 0 | — |
| SECONDARY Safety: Clinically Significant Laboratory, Vital Sign, Physical Examination, and/or 12-Lead Electrocardiogram (ECG) Abnormalities |
0; 0; 1; 0; 0; 0 | — |
Eligibility Criteria
Inclusion Criteria
- Men and women ages 18 to 55 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/m^2, inclusive. BMI = weight (kg)/ [height (m)]^2
Exclusion Criteria
- 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 a dipeptidyl peptidase-IV (DPP4) inhibitor or related compound
- 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 < 80 mL/min using the Cockcroft Gault formula
Data sourced from ClinicalTrials.gov (NCT01068743). 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.