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Phase 1 Completed N=27 Randomized

Bioequivalence Study of 2.5-mg Saxagliptin and 500-mg Glucophage in Tablets and a Fixed-dose Combination Tablet in Healthy Participants

Source: ClinicalTrials.gov NCT01068717 ↗
Enrolled (actual)
27
Serious AEs
0.0%
Results posted
Oct 2011
Primary outcomePrimary: Observed Maximum Plasma Concentration (Cmax) of Saxagliptin, Tablets and Fixed-dose Combination (FDC), Administered to Participants in the Fasted and Fed States — 10.54; 11.53; 12.71; 12.79 ng/mL

Summary

To demonstrate the bioequivalence of a 2.5-mg saxagliptin/500-mg metformin fixed-dose combination (FDC) tablet to that of 2.5-mg saxagliptin (Onglyza) and 500-mg metformin (Glucophage, marketed in Canada by Sanofi-Aventis) tablets coadministered to healthy participants in the fasted and fed states.

Outcome Measures

OutcomeResultp-value
PRIMARY
Observed Maximum Plasma Concentration (Cmax) of Saxagliptin, Tablets and Fixed-dose Combination (FDC), Administered to Participants in the Fasted and Fed States
10.54; 11.53; 12.71; 12.79
PRIMARY
Observed Cmax of Metformin, Tablets and FDC, Administered to Participants in the Fasted and Fed States
1058.19; 1044.70; 810.08; 811.94
PRIMARY
Terminal Half-life (t1/2) of Saxagliptin and Metformin, Tablets and FDC, Administered to Participants in the Fasted and Fed States
6.16; 6.69; 5.99; 6.15; 11.05; 13.02
PRIMARY
Area Under the Plasma Concentration-time Curve From Time 0 to the Last Quantifiable Concentration (AUC[0-t]) for Saxagliptin, Tablets and FDC, Given in the Fasted and Fed States
50.28; 51.60; 59.00; 58.94
PRIMARY
AUC[0-t] for Metformin, Tablets and FDC, Given in the Fasted and Fed States
8035.25; 7906.00; 7497.56; 7654.00
PRIMARY
AUC From Time 0 Extrapolated to Infinity (AUC[0-inf]) for Saxagliptin, Tablets and FDC, Given in the Fasted and Fed States
52.17; 53.73; 61.31; 60.88
PRIMARY
AUC[0-inf] for Metformin, Tablets and FDC, Administered in the Fasted and Fed States
8142.68; 8070.25; 7612.94; 7690.69
PRIMARY
Time to Achieve the Observed Maximum Plasma Concentration (Tmax) for Saxagliptin and Metformin, Tablets and FDC, Administered to Participants in the Fasted and Fed States
1.00; 0.75; 1.50; 1.00; 3.00; 3.00
SECONDARY
Number of Participants With Death as Outcome, Serious Adverse Events, and Adverse Events (AEs) Leading to Discontinuation
0; 0; 0; 0; 0; 0
SECONDARY
Number of Participants With Clinically Significant Abnormalities in Hematology, Serum Chemistry, and Urinalysis Laboratory Test Results
0; 0; 0; 0; 0; 0
SECONDARY
Number of Participants With Clinically Significant Abnormalities in Electrocardiogram (ECG) Results
0; 0; 0; 0
SECONDARY
Number of Participants With Clinically Significant Abnormalities in Body Temperature, Blood Pressure, or Heart Rate
0; 0; 0; 0

Eligibility Criteria

Inclusion Criteria

  • Men and women, aged 18 to 55 years, inclusive
  • Healthy participants as determined by a lack of clinically significant deviation from normal in medical history, physical examination, electrocardiograms, and clinical laboratory determinations
  • Body Mass Index of 18 to 32 kg/m^2, inclusive

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 DPP-4 inhibitors or related compounds
  • History of allergy or intolerance to metformin or other similar acting agents
  • Previous exposure to saxagliptin
  • Exposure to metformin within 3 months pervious to study drug administration
  • Estimated creatinine clearance of <80 mL/min using the Cockcroft Gault formula
View full record on ClinicalTrials.gov →

Data sourced from ClinicalTrials.gov (NCT01068717). 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.

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