Phase 1
Completed N=24
Bioequivalence Study of Saxagliptin and Glucophage Combination Formulations in Healthy Subjects (B)
Source: ClinicalTrials.gov NCT00897390 ↗Enrolled (actual)
24
Serious AEs
0.0%
Results posted
Jan 2011
Primary outcomePrimary: Saxagliptin Pharmacokinetic (PK) Parameter Area Under the Plasma Concentration-Time Curve From Time Zero Extrapolated to Infinite Time (AUC[INF]) — 47.25; 48.91; 52.89; 51.11 ng*h/mL
Summary
To demonstrate bioequivalence of a 2.5 mg saxagliptin/1000 mg metformin (glucophage) immediate release (IR) fixed dose combination (FDC) tablet to the 2.5 mg saxagliptin tablet and 1000 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 Pharmacokinetic (PK) Parameter Area Under the Plasma Concentration-Time Curve From Time Zero Extrapolated to Infinite Time (AUC[INF]) |
47.25; 48.91; 52.89; 51.11 | — |
| PRIMARY Saxagliptin PK Parameter Area Under the Plasma Concentration-time Curve From Time Zero to the Time of the Last Quantifiable Plasma Concentration (AUC[0-T]) |
44.90; 46.57; 50.50; 49.09 | — |
| PRIMARY Saxagliptin PK Parameter Maximum Observed Plasma Concentration (Cmax) |
8.58; 9.09; 10.97; 10.80 | — |
| PRIMARY Saxagliptin PK Parameter Plasma Terminal Half-life (T-HALF) |
6.66; 6.34; 6.47; 5.78 | — |
| PRIMARY Saxagliptin PK Parameter Time of Maximum Observed Plasma Concentration (Tmax) |
1.50; 0.75; 1.00; 1.50 | — |
| PRIMARY Metformin PK Parameter AUC(INF) |
13363.46; 12677.92; 12357.87; 12126.19 | — |
| PRIMARY Metformin PK Parameter AUC(0-T) |
13238.43; 12400.41; 12124.31; 11996.88 | — |
| PRIMARY Metformin PK Parameter Cmax |
2004.99; 1830.76; 1666.55; 1642.90 | — |
| PRIMARY Metformin PK Parameter T-HALF |
8.43; 10.58; 11.78; 7.63 | — |
| PRIMARY Metformin PK Parameter Tmax |
2.00; 2.98; 4.00; 4.00 | — |
| SECONDARY BMS-510849 PK Parameter AUC(INF) |
118.54; 116.19; 127.67; 127.25 | — |
| SECONDARY BMS-510849 PK Parameter AUC(0-T) |
108.31; 106.11; 117.42; 117.43 | — |
| SECONDARY BMS-510849 PK Parameter Cmax |
16.77; 15.17; 18.24; 18.58 | — |
| SECONDARY BMS-510849 PK Parameter T-Half |
8.05; 7.31; 7.48; 7.35 | — |
| SECONDARY BMS-510849 PK Parameter T-Max |
2.00; 2.00; 2.00; 2.00 | — |
| SECONDARY Deaths, Serious Adverse Events (SAEs), Adverse Events (AEs), and Discontinuations Due to AEs |
0; 0; 0; 0; 0; 0 | — |
| SECONDARY AEs of Special Interest |
0; 0; 0; 0 | — |
| SECONDARY Number of Participants With Marked Laboratory Abnormalities (MA) |
0; 0; 0; 1; 1; 1 | — |
| SECONDARY Number of Participants With Marked Urinalysis Abnormalities |
0; 0; 0; 0; 0; 0 | — |
| SECONDARY Electrocardiogram (ECG), Vital Sign, and Physical Finding Abnormalities |
0; 0; 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 (NCT00897390). 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.