MedPath

BMS - Safety, Pharmacokinetics (PK) and Pharmacodynamics (PD) of Dapagliflozin in Type 1 Diabetes

Phase 2
Completed
Conditions
Type 1 Diabetes Mellitus
Interventions
Registration Number
NCT01498185
Lead Sponsor
AstraZeneca
Brief Summary

To obtain safety and tolerability information in patients with type 1 diabetes where Dapagliflozin is added on to Insulin (for 14 days)

Detailed Description

Study Classification : Safety, Pharmacokinetics and Pharmacodynamics

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
171
Inclusion Criteria
  • Type 1 diabetes with central lab Glycosylated hemoglobin (A1C) ≥ 7.0% and ≤ 10.0%
  • Insulin use for at least 12 months and initiation immediately after diagnosis of diabetes
  • Method of Insulin administration [multiple daily injections (MDI) or continuous subcutaneous Insulin infusion (CSII)] stable ≥ 3 months
  • Stable basal Insulin dose ≥ 2 weeks
  • Ages 18 to 65 years
  • Central laboratory C-peptide value of < 0.7 ng/mL
  • Body mass index (BMI) 18.5 to 35.0 kg/m2
Exclusion Criteria
  • History of type 2 diabetes mellitus (T2DM), maturity onset diabetes of young (MODY), pancreatic surgery or chronic pancreatitis
  • Oral hypoglycemic agents
  • History of diabetes ketoacidosis (DKA) within 24 weeks
  • History of hospital admission for glycemic control within 6 months
  • Frequent episodes of hypoglycemia (2 unexplained within 3 months) or hypoglycemic unawareness
  • Aspartate aminotransferase (AST), Alanine aminotransferase (ALT) or Serum total bilirubin > 2X Upper limit of normal (ULN)
  • Abnormal Free T4 [if screening Thyroid Stimulating Hormone (TSH) abnormal]
  • Estimated glomerular filtration rate (eGFR) Modification of Diet in Renal Disease (MDRD) formula ≤ 60 mL/min/1.73m2
  • Cardiovascular (CV)/Vascular Diseases within 6 months

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
Arm 1: Dapagliflozin (1 mg)Dapagliflozin-
Arm 3: Dapagliflozin (5 mg)Dapagliflozin-
Arm 4: Dapagliflozin (10 mg)Dapagliflozin-
Arm 5: Placebo matching DapagliflozinPlacebo matching Dapagliflozin-
Arm 2: Dapagliflozin (2.5 mg)Dapagliflozin-
Primary Outcome Measures
NameTimeMethod
Mean Change From Baseline in 7-Point Glucose Monitoring (7-PGM) at Day 7From Baseline to Day 7

7-PGM was measured as milligrams per deciliter (mg/dL) by a central laboratory. Baseline was defined as the assessment on Day -1, prior to the start date and time of the first dose of the double-blind study medication. 7-PGM included the average of all available glucose values before and 2-hour (hr) after each meal (breakfast, lunch, dinner) as well as bedtime. Measurements were on Day -1, and Day 7 in the double-blind period.

Secondary Outcome Measures
NameTimeMethod
Dapagliflozin Pharmacokinetic Parameters on Day 7 - Area Under the Concentration-Time Curve in One Dosing Interval (AUC[TAU])Day 7 (0 hr to 24 hr post dose)

Serial blood samples were collected predose 0 hr, and hr 0.5, 1, 2, 3, 4, 6, 8, 12, and 24 in the double-blind period. Individual subject PK parameter values were derived by non-compartmental methods by a validated PK analysis program, Kinetica®. Actual sampling times were used for PK calculations and nominal times were used for generation of mean plasma concentration-time plots and summaries. Pre-dose sample collection times were changed from negative numbers (based on elapsed time to dose) to zero for the purpose of calculating PK parameters. The concentrations below the lower limit of quantitation (\<LLOQ) were set as "missing" for the calculation of PK parameters as well as summary statistics. AUC\[TAU\], was calculated by a mixture of logand linear-trapezoidal summations.

Dapagliflozin Pharmacokinetic Parameters on Day 7 - Maximum Observed Plasma Concentration (Cmax)Day 7 (0 hr to 24 hr post dose)

Serial blood samples were collected predose 0 hr, and hr 0.5, 1, 2, 3, 4, 6, 8, 12, and 24 in the double-blind period. Individual subject PK parameter values were derived by non-compartmental methods by a validated PK analysis program, Kinetica®. Actual sampling times were used for PK calculations and nominal times were used for generation of mean plasma concentration-time plots and summaries. Pre-dose sample collection times were changed from negative numbers (based on elapsed time to dose) to zero for the purpose of calculating PK parameters. The Cmax was recorded directly from experimental observations.

Dapagliflozin Pharmacokinetic Parameters on Day 7 - Time of Maximum Observed Plasma Concentration (Tmax)Day 7 (0 hr to 24 hr post dose)

Serial blood samples were collected predose 0 hr, and hr 0.5, 1, 2, 3, 4, 6, 8, 12, and 24 in the double-blind period. Individual subject PK parameter values were derived by non-compartmental methods by a validated PK analysis program, Kinetica®. Actual sampling times were used for PK calculations and nominal times were used for generation of mean plasma concentration-time plots and summaries. Pre-dose sample collection times were changed from negative numbers (based on elapsed time to dose) to zero for the purpose of calculating PK parameters. The Tmax was recorded directly from experimental observations.

Dapagliflozin 3-O-glucuronide Pharmacokinetic Parameters on Day 7 - Time of Maximum Observed Plasma Concentration (Tmax)Day 7 (0 hr to 24 hr post dose)

Serial blood samples were collected predose 0 hr, and hr 0.5, 1, 2, 3, 4, 6, 8, 12, and 24 in the double-blind period. Individual subject PK parameter values were derived by non-compartmental methods by a validated PK analysis program, Kinetica®. Actual sampling times were used for PK calculations and nominal times were used for generation of mean plasma concentration-time plots and summaries. Pre-dose sample collection times were changed from negative numbers (based on elapsed time to dose) to zero for the purpose of calculating PK parameters. The Tmax was recorded directly from experimental observations.

Dapagliflozin 3-O-glucuronide Pharmacokinetic Parameters on Day 7 - Area Under the Concentration-Time Curve in One Dosing Interval (AUC[TAU])Day 7 (0 hr to 24 hr post dose)

Serial blood samples were collected predose 0 hr, and hr 0.5, 1, 2, 3, 4, 6, 8, 12, and 24 in the double-blind period. Individual subject PK parameter values were derived by non-compartmental methods by a validated PK analysis program, Kinetica®. Actual sampling times were used for PK calculations and nominal times were used for generation of mean plasma concentration-time plots and summaries. Pre-dose sample collection times were changed from negative numbers (based on elapsed time to dose) to zero for the purpose of calculating PK parameters. The concentrations below the lower limit of quantitation (\<LLOQ) were set as "missing" for the calculation of PK parameters as well as summary statistics. AUC\[TAU\], was calculated by a mixture of logand linear-trapezoidal summations.

Dapagliflozin 3-O-glucuronide Pharmacokinetic Parameters on Day 7 - Maximum Observed Plasma Concentration (Cmax)Day 7 (0 hr to 24 hr post dose)

Serial blood samples were collected predose 0 hr, and hr 0.5, 1, 2, 3, 4, 6, 8, 12, and 24 in the double-blind period. Individual subject PK parameter values were derived by non-compartmental methods by a validated PK analysis program, Kinetica®. Actual sampling times were used for PK calculations and nominal times were used for generation of mean plasma concentration-time plots and summaries. Pre-dose sample collection times were changed from negative numbers (based on elapsed time to dose) to zero for the purpose of calculating PK parameters. The Cmax was recorded directly from experimental observations.

Pharmacokinetic Parameters on Day 7 - Ratio of Metabolite (RM) to Parent AUC[TAU]Day 7 (0 hr to 24 hr post dose)

Serial blood samples were collected predose 0 hr, and hr 0.5, 1, 2, 3, 4, 6, 8, 12, and 24 in the double-blind period. Individual subject PK parameter values were derived by non-compartmental methods by a validated PK analysis program, Kinetica®. Actual sampling times were used for PK calculations and nominal times were used for generation of mean plasma concentration-time plots and summaries. Pre-dose sample collection times were changed from negative numbers (based on elapsed time to dose) to zero for the purpose of calculating PK parameters. The concentrations below the lower limit of quantitation (\<LLOQ) were set as "missing" for the calculation of PK parameters as well as summary statistics. MR was calculated as the ratio of metabolite to parent AUC(TAU), corrected for molecular weights of dapagliflozin and dapagliflozin 3-O-glucuronide (408.82 and 584.99, respectively).

Trial Locations

Locations (12)

La Biomed Research Inst. At Harbor Ucla Med Ctr.

🇺🇸

Torrance, California, United States

Va San Diego Healthcare System

🇺🇸

San Diego, California, United States

Vince And Associates Clinical Research

🇺🇸

Overland Park, Kansas, United States

Central Kentucky Research Associates, Inc.

🇺🇸

Lexington, Kentucky, United States

Jasper Clinic, Inc.

🇺🇸

Kalamazoo, Michigan, United States

Profil Institute For Clinical Research, Inc.

🇺🇸

Chula Vista, California, United States

Compass Research Phase 1, Llc

🇺🇸

Orlando, Florida, United States

Progressive Medical Research

🇺🇸

Port Orange, Florida, United States

Kansas City University Of Medicine And Biosciences

🇺🇸

Kansas City, Missouri, United States

Dallas Diabetes & Endocrine Center

🇺🇸

Dallas, Texas, United States

Louisiana Research Associates, Inc.

🇺🇸

New Orleans, Louisiana, United States

Regional Medical Clinic-Endocrinology

🇺🇸

Rapid City, South Dakota, United States

© Copyright 2025. All Rights Reserved by MedPath