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Efficacy of Alogliptin With Pioglitazone (Actos®) in Subjects With Type 2 Diabetes Mellitus

Phase 3
Completed
Conditions
Diabetes Mellitus
Interventions
Registration Number
NCT00395512
Lead Sponsor
Takeda
Brief Summary

The purpose of this study is to evaluate the combination of alogliptin, once daily (QD), and pioglitazone in patients with type 2 diabetes mellitus who are inadequately controlled with diet and exercise alone.

Detailed Description

There are approximately 19 million people in the United States who have been diagnosed with diabetes mellitus, of which 90% to 95% is type 2. The prevalence of type 2 diabetes varies among racial and ethnic populations and has been shown to correlate with age, obesity, family history, history of gestational diabetes, and physical inactivity. Over the next decade, a marked increase in the number of adults with diabetes mellitus is expected, placing an ever-increasing burden on families and the health care system.

Current pharmacologic interventions for type 2 diabetes mellitus include a diverse range of antidiabetic medications with different mechanisms of action including insulin and insulin analogues, sulfonylureas, metformin, meglitinides, thiazolidinediones, inhibitors of alpha- glucosidase, analogs of glucagon-like peptide-1, and synthetic analogues of human amylin. Despite the variety of medications, many have clinically important or potentially life-threatening side effects, restricted use in many subpopulations, concerns with long-term tolerability, and challenges related to compliance due to side effects and route of administration. All of these reasons contribute to the difficulties patients have reaching the target glycosylated hemoglobin level less than 7%.

SYR-322 (alogliptin) is a selective, orally available inhibitor of the dipeptidyl peptidase-4 enzyme. Dipeptidyl peptidase-4 enzyme is thought to be primarily responsible for the in vivo degradation of 2 peptide hormones released in response to nutrient ingestion, namely glucagon-like peptide-1 and glucose-dependent insulinotropic peptide. Both peptides exert important effects on islet beta cells to stimulate glucose-dependent insulin secretion as well as regulating beta cell proliferation and cytoprotection. Glucagon-like peptide-1, but not glucose-dependent insulinotropic peptide, inhibits gastric emptying, glucagon secretion, and food intake. Glucose-dependent insulinotropic peptide has been shown to enhance insulin secretion by direct interaction with a glucose-dependent insulinotropic peptide -specific receptor on islet beta cells. The glucose-lowering actions of glucagon-like peptide-1, but not glucose-dependent insulinotropic peptide, are preserved in patients with type 2 diabetes mellitus.

Pioglitazone (ACTOS®) is a thiazolidinedione developed by Takeda Chemical Industries, Ltd. (Osaka, Japan) that is approved for the treatment of type 2 diabetes mellitus. Pioglitazone is a selective peroxisome proliferator-activated receptor-gamma agonist that decreases insulin resistance in the periphery and liver resulting in increased insulin-dependent glucose disposal and decreased hepatic glucose output.

As the rate of newly diagnosed cases of type 2 diabetes mellitus continues to grow, so does the need for products that will provide better glycemic control and improved safety and tolerability. Alogliptin and pioglitazone have complementary actions. Alogliptin inhibits the degradation of glucagon-like peptide-1 by inhibiting the enzyme dipeptidyl peptidase IV, thus augmenting glucose-dependent insulin secretion while pioglitazone is a peripheral and hepatic insulin sensitizer. Given the complementary mechanisms of action of alogliptin (stimulates insulin secretion) and pioglitazone (enhances insulin sensitivity), the addition of combination therapy in treatment naïve type 2 diabetes patients may potentially allow the patients to reach and maintain their glycosylated hemoglobin goal more effectively.

The aim of this study is to evaluate the effectiveness of the combination of alogliptin with pioglitazone in patients who are inadequately controlled on diet and exercise alone. Study participation is anticipated to be approximately 8.5 months.

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
655
Inclusion Criteria

Not provided

Exclusion Criteria

Not provided

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
Alogliptin 25 mg QDAlogliptinAlogliptin 25 mg, tablets, orally, once daily and pioglitazone placebo-matching tablets, orally, once daily for up to 26 weeks.
Alogliptin 25 mg QDPlaceboAlogliptin 25 mg, tablets, orally, once daily and pioglitazone placebo-matching tablets, orally, once daily for up to 26 weeks.
Pioglitazone 30 mg QDPlaceboPioglitazone 30 mg, tablets, orally, once daily and alogliptin placebo-matching tablets, orally, once daily for up to 26 weeks.
Pioglitazone 30 mg QDPioglitazonePioglitazone 30 mg, tablets, orally, once daily and alogliptin placebo-matching tablets, orally, once daily for up to 26 weeks.
Alogliptin 25 mg QD+ Pioglitazone 30 mg QDAlogliptinAlogliptin 25 mg, tablets, orally, once daily and pioglitazone 30 mg, tablets, orally, once daily for up to 26 weeks.
Alogliptin 12.5 mg QD + Pioglitazone 30 mg QDAlogliptinAlogliptin 12.5 mg, tablets, orally, once daily and pioglitazone 30 mg, tablets, orally, once daily for up to 26 weeks.
Alogliptin 25 mg QD+ Pioglitazone 30 mg QDPioglitazoneAlogliptin 25 mg, tablets, orally, once daily and pioglitazone 30 mg, tablets, orally, once daily for up to 26 weeks.
Alogliptin 12.5 mg QD + Pioglitazone 30 mg QDPioglitazoneAlogliptin 12.5 mg, tablets, orally, once daily and pioglitazone 30 mg, tablets, orally, once daily for up to 26 weeks.
Primary Outcome Measures
NameTimeMethod
Change From Baseline to Week 26 in Glycosylated Hemoglobin (HbA1c)Baseline and Week 26

The change from Baseline to Week 26 in HbA1c (the concentration of glucose bound to hemoglobin as a percent of the absolute maximum that can be bound).

Secondary Outcome Measures
NameTimeMethod
Change From Baseline in HbA1c Over TimeBaseline and Weeks 4, 8, 12, 16 and 20.

The change from Baseline in HbA1c (the concentration of glucose bound to hemoglobin as a percent of the absolute maximum that can be bound) at 4 week intervals during the study. Least Squares Means were from an Analysis of Covariance (ANCOVA) model with treatment and geographic region as class variables and baseline HbA1c as a covariate.

Change From Baseline in Fasting Plasma Glucose Over TimeBaseline and Weeks 1, 2, 4, 8, 12, 16, 20 and 26.

The change from Baseline in fasting plasma glucose was assessed at weeks 1, 2, 4, 8, 12, 16, 20 and 26. Least Squares Means were from an ANCOVA model with treatment and geographic region as class variables and baseline plasma glucose as a covariate.

Percentage of Participants With Marked HyperglycemiaWeeks 1, 2, 4, 8, 12, 16, 20 and 26.

Marked Hyperglycemia is defined as fasting plasma glucose greater than or equal to 200 mg/dL. Study week windows are defined to place hyperglycemia into visit categories.

Change From Baseline in High-Density Lipoprotein CholesterolBaseline and Weeks 4, 8, 12, 16, 20 and 26.

Change from Baseline in high-density lipoprotein cholesterol (HDL-C) was assessed at Weeks 4, 8, 12, 16, 20 and 26. Least squares means are from an ANCOVA model with treatment and geographic region as class variables and baseline HDL cholesterol as a covariate.

Percentage of Participants Meeting Rescue CriteriaWeeks 4, 8, 12, 16, 20 and 26.

Rescue was defined as meeting 1 of the following criteria, confirmed by a 2nd sample drawn within 5 days after the first sample and analyzed by the central laboratory:

1. After more than 4 weeks of treatment but prior to the Week 8 Visit: a single fasting plasma glucose ≥310 mg/dL (≥17.5 mmol/L);

2. From the Week 8 Visit but prior to the Week 12 Visit: a single fasting plasma glucose ≥275 mg/dL (≥15.27 mmol/L);

3. From the Week 12 Visit through the End-of-Treatment Visit: HbA1c ≥8.5% and ≤0.5% reduction in HbA1c as compared with the Baseline HbA1c.

Percentage of Participants With Glycosylated Hemoglobin Less Than or Equal to 6.5%Week 26

Clinical response at Week 26 was assessed by the percentage of participants with HbA1c ≤6.5%.

Percentage of Participants With Glycosylated Hemoglobin Less Than or Equal to 7.0%Week 26

Clinical response at Week 26 was assessed by the percentage of participants with HbA1c ≤ 7%.

Percentage of Participants With Glycosylated Hemoglobin Less Than or Equal to 7.5%Week 26

Clinical response at Week 26 was assessed by the percentage of participants with HbA1c ≤ 7.5%.

Percentage of Participants With a Decrease in Glycosylated Hemoglobin Greater Than or Equal to 0.5%Baseline and Week 26

Clinical response at Week 26 was assessed by the percentage of participants with a decrease from Baseline in HbA1c of ≥ 0.5%.

Percentage of Participants With a Decrease in Glycosylated Hemoglobin Greater Than or Equal to 1.0%Baseline and Week 26

Clinical response at Week 26 was assessed by the percentage of participants with a decrease from Baseline in HbA1c of ≥ 1%.

Percentage of Participants With a Decrease in Glycosylated Hemoglobin Greater Than or Equal to 1.5%.Baseline and Week 26

Clinical response at Week 26 was assessed by the percentage of participants with a decrease from Baseline in HbA1c of ≥ 1.5%.

Percentage of Participants With a Decrease in Glycosylated Hemoglobin Greater Than or Equal to 2.0%Baseline and Week 26

Clinical response at Week 26 was assessed by the percentage of participants with a decrease from Baseline in HbA1c of ≥ 2.0%.

Change From Baseline in Fasting ProinsulinBaseline and Weeks 4, 8, 12, 16, 20 and 26.

Proinsulin is a precursor to insulin, and was measured as an indicator of pancreatic function. The change from Baseline in fasting proinsulin was assessed at Weeks 4, 8, 12, 16, 20 and 26. Least Squares Means were from an ANCOVA model with treatment and geographic region as class variables and baseline proinsulin as a covariate.

Change From Baseline in InsulinBaseline and Weeks 4, 8, 12, 16, 20 and 26.

The change from Baseline in fasting insulin was assessed at Weeks 4, 8, 12, 16, 20 and 26. Least Squares Means were from an ANCOVA model with treatment and geographic region as class variables and baseline insulin as a covariate.

Change From Baseline in Proinsulin/Insulin RatioBaseline and Weeks 4, 8, 12, 16, 20 and 26.

The ratio of proinsulin to insulin was calculated as proinsulin (pmol/L) / insulin (μIU/mL) at weeks 4, 8, 12, 16, 20 and 26 relative to the Baseline value. Least squares means were from an ANCOVA model with treatment and geographic region as class variables and Baseline proinsulin/insulin ratio as a covariate.

Change From Baseline in C-peptide LevelsBaseline and Weeks 4, 8, 12, 16, 20 and 26.

C-peptide is a byproduct created when the hormone insulin is produced and is measured by a blood test. Change from Baseline was assessed at Weeks 4, 8, 12, 16, 20 and 26. Least squares means are from an ANCOVA model with treatment and geographic region as class variables and baseline C-peptide as a covariate.

Change From Baseline in Calculated Homeostatic Model Assessment Insulin ResistanceBaseline and Weeks 12 and 26.

The Homeostasis Model Assessment of insulin resistance (HOMA IR) measures insulin resistance based on fasting glucose and insulin measurements:

HOMA IR = fasting plasma insulin (µIU/mL) \* fasting plasma glucose (mmol/L) / 22.5

A higher number indicates a greater degree of insulin resistance. The change from Baseline in HOMA IR was assessed at Weeks 12 and 26. Least squares means are from an ANCOVA model with treatment and geographic region as class variables and baseline HOMA IR as a covariate.

Change From Baseline in Homeostatic Model Assessment Beta Cell FunctionBaseline and Weeks 12 and 26.

The Homeostasis Model Assessment (HOMA) estimates steady state beta cell function (%B) as a percentage of a normal reference population.

HOMA %B = 20 \* insulin (µIU/mL) / fasting plasma glucose (mmol/L) - 3.5

The change from Baseline in the homeostasis model assessment of beta cell function was assessed at Weeks 12 and 26. Least squares means are from an ANCOVA model with treatment and geographic region as class variables and baseline HOMA beta cell function as a covariate.

Change From Baseline in Body WeightBaseline and Weeks 8, 12, 20 and 26.

Change from Baseline in body weight was assessed at Weeks 8, 12, 20 and 26. Least squares means are from an ANCOVA model with treatment and geographic region as class variables and Baseline weight as a covariate.

Change From Baseline in Total Cholesterol LevelBaseline and Weeks 4, 8, 12, 16, 20 and 26.

Change from Baseline in total cholesterol level was assessed at Weeks 4, 8, 12, 16, 20 and 26. Least squares means are from an ANCOVA model with treatment and geographic region as class variables and baseline total cholesterol as a covariate.

Change From Baseline in Low-Density Lipoprotein CholesterolBaseline and Weeks 4, 8, 12, 16, 20 and 26.

Change from Baseline in low-density lipoprotein cholesterol (LDL-C) was assessed at Weeks 4, 8, 12, 16, 20 and 26. Least squares means are from an ANCOVA model with treatment and geographic region as class variables and baseline LDL cholesterol as a covariate.

Change From Baseline in Triglyceride LevelsBaseline and Weeks 4, 8, 12, 16, 20 and 26.

Change from Baseline in triglycerides was assessed at Weeks 4, 8, 12, 16, 20 and 26. Least squares means are from an ANCOVA model with treatment and geographic region as class variables and baseline triglycerides as a covariate.

Change From Baseline in Free Fatty AcidsBaseline and Weeks 12 and 26.

Change from Baseline in free fatty acids (FFA) was assessed at Weeks 12 and 26. Least squares means are from an ANCOVA model with treatment and geographic region as class variables and baseline free fatty acid as a covariate.

Change From Baseline in Plasminogen Activator Inhibitor-1Baseline and Weeks 12 and 26.

Change from Baseline in plasminogen activator inhibitor-1 was assessed at Weeks 12 and 26. Least squares means are from an ANCOVA model with treatment and geographic region as class variables and baseline plasminogen activator inhibitor-1 as a covariate.

Change From Baseline in High-sensitivity C-Reactive ProteinBaseline and Weeks 12 and 26.

Change from Baseline in high-sensitivity C-Reactive Protein (hsCRP) was assessed at Weeks 12 and 26. Least squares means are from an ANCOVA model with treatment and geographic region as class variables and baseline hsCRP as a covariate.

Change From Baseline in AdiponectinBaseline and Weeks 12 and 26.

Change from Baseline in adiponectin was assessed at Weeks 12 and 26. Least squares means are from an ANCOVA model with treatment and geographic region as class variables and baseline adiponectin as a covariate.

Change From Baseline in Apolipoprotein A1Baseline and Weeks 12 and 26.

Change from Baseline in Apolipoprotein A1 was assessed at Weeks 12 and 26. Least squares means are from an ANCOVA model with treatment and geographic region as class variables and Baseline apolipoprotein A1 as a covariate.

Change From Baseline in Apolipoprotein A2Baseline and Weeks 12 and 26.

Change from Baseline in apolipoprotein A2 was assessed at Weeks 12 and 26. Least squares means are from an ANCOVA model with treatment and geographic region as class variables and baseline apolipoprotein A2 as a covariate.

Change From Baseline in Apolipoprotein BBaseline and Weeks 12 and 26.

Change from Baseline in apolipoprotein B was assessed at Weeks 12 and 26. Least squares means are from an ANCOVA model with treatment and geographic region as class variables and baseline apolipoprotein B as a covariate.

Change From Baseline in Apolipoprotein C-IIIBaseline and Weeks 12 and 26.

Change from Baseline in apolipoprotein C-III was assessed at Weeks 12 and 26. Least squares means are from an ANCOVA model with treatment and geographic region as class variables and baseline apolipoprotein C-III as a covariate.

Change From Baseline in Nuclear Magnetic Resonance Lipid Fractionation Total TriglyceridesBaseline and Weeks 12 and 26.

Nuclear Magnetic Resonance (NMR) lipid fractionation was used to assess the change from Baseline in total triglyceride levels at Weeks 12 and 26. Least squares means are from an ANCOVA model with treatment and geographic region as class variables and baseline NMR total triglycerides as a covariate.

Change From Baseline in Very Low Density Lipoprotein (VLDL) / Chylomicron ParticlesBaseline and Weeks 12 and 26.

The change from Baseline in levels of total VLDL/chylomicron particles and large VLDL/chylomicron particles was assessed by NMR lipid fractionation at Weeks 12 and 26.

Least squares means are from an ANCOVA model with treatment and geographic region as class variables and baseline VLDL/chylomicron particles as a covariate.

Change From Baseline in VLDL / Chylomicron TriglyceridesBaseline and Weeks 12 and 26.

The change from Baseline in levels of VLDL/chylomicron triglycerides was assessed by NMR lipid fractionation at Weeks 12 and 26.

Least squares means are from an ANCOVA model with treatment and geographic region as class variables and baseline VLDL/chylomicron triglycerides as a covariate.

Change From Baseline in VLDL ParticlesBaseline and Weeks 12 and 26.

The change from Baseline in levels of medium VLDL particles and small VLDL particles was assessed by NMR fractionation at Weeks 12 and 26.

Least squares means are from an ANCOVA model with treatment and geographic region as class variables and baseline VLDL particles as a covariate.

Change From Baseline in Mean VLDL Particle SizeBaseline and Weeks 12 and 26.

Change from Baseline in mean VLDL particle size was assessed by NMR lipid fractionation at Weeks 12 and 26. Least squares means are from an ANCOVA model with treatment and geographic region as class variables and baseline mean VLDL particle size as a covariate.

Change From Baseline in Intermediate Density Lipoprotein (IDL) ParticlesBaseline and Weeks 12 and 26.

The change from Baseline in levels of IDL particles was assessed by NMR fractionation at Weeks 12 and 26.

Least squares means are from an ANCOVA model with treatment and geographic region as class variables and baseline IDL particles as a covariate.

Change From Baseline in Low Density Lipoprotein (LDL) ParticlesBaseline and Weeks 12 and 26.

The change from Baseline in levels of total, large, medium-small, total small and very small LDL particles was assessed by NMR fractionation at Weeks 12 and 26.

Least squares means are from an ANCOVA model with treatment and geographic region as class variables and baseline LDL particles as a covariate.

Change From Baseline in Mean LDL Particle SizeBaseline and Weeks 12 and 26.

Change from Baseline in mean LDL particle size was assessed by NMR lipid fractionation at Weeks 12 and 26. Least squares means are from an ANCOVA model with treatment and geographic region as class variables and baseline mean LDL particle size as a covariate.

Change From Baseline in High Density Lipoprotein (HDL) ParticlesBaseline and Weeks 12 and 26.

The change from Baseline in levels of total, large, medium and small HDL particles was assessed by NMR fractionation at Weeks 12 and 26.

Least squares means are from an ANCOVA model with treatment and geographic region as class variables and baseline HDL particles as a covariate.

Change From Baseline in Mean HDL Particle SizeBaseline and Weeks 12 and 26.

Change from Baseline in mean HDL particle size was assessed by NMR lipid fractionation at Weeks 12 and 26. Least squares means are from an ANCOVA model with treatment and geographic region as class variables and baseline mean HDL particle size as a covariate.

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