Phase 1
Completed N=30
Bioequivalence Study of the Fixed Dose Combination of 5 mg Saxagliptin and 500 mg Metformin XR Tablet (Manufactured in Mt Vernon, IN) Relative to 5 mg Saxagliptin Tablet and 500 mg Metformin XR Tablet (Manufactured in Evansville, IN)
Source: ClinicalTrials.gov NCT01192139 ↗Enrolled (actual)
30
Serious AEs
0.0%
Results posted
May 2011
Primary outcomePrimary: Saxagliptin Area Under the Plasma Concentration Versus Time Curve From Time 0 Extrapolated to Infinity (AUC[0-inf]) — 107.28; 111.72; 103.35 ng*hr/mL
Summary
The purpose of this study is to demonstrate bioequivalence (BE) of a 5 mg saxagliptin/500 mg metformin extended release (XR) fixed-dose combination (FDC) tablet (manufactured in Mt Vernon, Indiana [IN]) to coadministered 5 mg saxagliptin and 500 mg metformin XR tablet (manufactured in Evansville, IN) in fed healthy subjects.
Outcome Measures
| Outcome | Result | p-value |
|---|---|---|
| PRIMARY Saxagliptin Area Under the Plasma Concentration Versus Time Curve From Time 0 Extrapolated to Infinity (AUC[0-inf]) |
107.28; 111.72; 103.35 | — |
| PRIMARY Saxagliptin Observed Maximum Plasma Concentration (Cmax) |
26.84; 27.25; 28.85 | — |
| PRIMARY Metformin AUC(0-inf) |
5865.92; 5516.97; 5073.70 | — |
| PRIMARY Metformin Cmax |
629.73; 586.87; 657.23 | — |
| SECONDARY Saxagliptin Terminal Half-life (T1/2) |
8.46; 8.56; 9.21 | — |
| SECONDARY Saxagliptin Area Under the Plasma Concentration Versus Time Curve From Time 0 to the Time of the Last Quantifiable Concentration (AUC[0-t]) |
105.47; 109.88; 101.52 | — |
| SECONDARY Time to Achieve the Observed Maximum Saxagliptin Plasma Concentration (Tmax) |
1.65; 1.48; 0.65 | — |
| SECONDARY Saxagliptin Fraction of AUC(0-inf) Contributed by AUC(0-t) (AUC[0-t]/AUC[0-inf]) |
0.983; 0.983; 0.982 | — |
| SECONDARY Active Metabolite BMS-510849 AUC(0-inf) |
291.72; 295.94; 289.06 | — |
| SECONDARY Active Metabolite BMS-510849 AUC(0-t) |
284.46; 289.03; 281.79 | — |
| SECONDARY Active Metabolite BMS-510849 Cmax |
49.71; 49.28; 49.09 | — |
| SECONDARY Active Metabolite BMS-510849 T1/2 |
13.88; 13.65; 14.04 | — |
| SECONDARY Active Metabolite BMS-510849 Tmax |
2.38; 2.42; 1.46 | — |
| SECONDARY Active Metabolite BMS-510849 AUC(0-t)/AUC(0-inf) |
0.974; 0.975; 0.974 | — |
| SECONDARY Metformin AUC(0-t) |
5617.39; 5200.46; 4896.95 | — |
| SECONDARY Metformin T1/2 |
10.7; 12.6; 14.9 | — |
| SECONDARY Metformin Tmax |
4.78; 4.90; 4.11 | — |
| SECONDARY Metformin Fraction of AUC(0-inf) Contributed by AUC(0-t)(AUC[0-t]/AUC[0-inf]) |
0.979; 0.970; 0.965 | — |
| SECONDARY Safety: Adverse Events (AEs), Discontinuations Due to AEs, Deaths, and Serious AEs (SAEs) |
3; 2; 4; 0; 0; 0 | — |
| SECONDARY Safety: Clinically Significant Laboratory, Vital Sign, Physical Examination, and Electrocardiogram (ECG) Abnormalities |
0; 0; 0; 0; 0; 0 | — |
Eligibility Criteria
Inclusion Criteria
- Healthy male and female subjects as determined by no clinically significant deviation from normal in medical history, physical examination, electrocardiogram (ECG), and clinical laboratory determinations
- Body Mass Index (BMI) of 18 to 32 kg/m2, inclusive
- Ages 18 to 45, inclusive
Exclusion Criteria
- Evidence of organ dysfunction or any clinically significant deviation from normal in physical examination, vital signs, ECG or clinical laboratory determinations beyond what is consistent with the target population
- Major surgical procedure within 4 weeks prior to randomization
- Positive serology test for human immunodeficiency virus (HIV), hepatitis B virus (HBV) or hepatitis C virus (HCV)
- Clinically significant history or presence of any of the following conditions: heart, liver, or kidney disease, neurologic or psychiatric disease
- History of gastrointestinal disease within the past 3 months
- Any clinically significant medical condition that could potentially affect your participation in the study and/or personal well-being, as judged by the investigator
- Donated blood or blood products to a blood bank, blood transfusion or participated in a clinical study (except a screening visit) requiring withdrawal of blood within 4 weeks prior to randomization
- Unable to tolerate oral and/or intravenous (IV) medications
- Unable to tolerate the puncturing of veins for drawing of blood
- Known allergy or hypersensitivity to any component of the study medication
- History of any significant drug allergies (such as anaphylaxis or hepatotoxicity)
- Used any prescription drugs or over the counter products to control acid (for example, Prevacid, Mylanta or Rolaids) within 4 weeks prior to randomization
- Used any other drugs including over the counter medications and herbal preparations within 1 week prior to randomization
- Taken any investigational drug or placebo (inactive drug) within 4 weeks prior to randomization
Data sourced from ClinicalTrials.gov (NCT01192139). 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.