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Safety, Tolerability, Pharmacokinetics And Pharmacodynamics Study Of PF-06291874 As Oral Monotherapy To Treat Adults With Type 2 Diabetes Mellitus

Phase 2
Completed
Conditions
Diabetes Mellitus, Type II
Interventions
Drug: Placebo
Registration Number
NCT02175121
Lead Sponsor
Pfizer
Brief Summary

This study is going to assess the safety and tolerability of PF-06291874 in adults with Type 2 Diabetes Mellitus as monotherapy, to evaluate the significance of overall glycemic control in these subjects.

Detailed Description

Not available

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
172
Inclusion Criteria
  • Male subjects and non-childbearing potential female subjects between the ages of 18 and 70 years old.

  • Body Mass Index of 18.0 to 45.4 kg/m2; and a total body weight of >50 kg

  • HbA1c value at the screening visit meeting once of the following criteria:

    • Currently taking acceptable oral antiglycemic drug therapy within 6.5 to 9.5%
    • Not currently taking any oral antiglycemic drug therapy within 7 to 10.5%
  • Fasting plasma glucose concentrations<270mg/dL at the screening and run-in visit, confirmed by a single repeat, if deemed necessary.

  • Subjects must be willing and able to perform self-tests of blood glucose at least 4 times per day, and maintain a diary for the duration of participation in the study; and therefore, subjects must be literate.

Exclusion Criteria
  • History of Type 1 diabetes mellitus or secondary forms of diabetes

  • One or more self-reported hypoglycemic episodes of sever intensity within 3 months of screening; or 2 or more self-reported hypoglycemic episodes of severe intensity within the previous 6 months.

  • History of myocardial infarction, unstable angina, arterial revascularization, stroke, New York Heart Association Functional Class II-IV heart failure, or transient ischemic attach within 6 months of screening.

  • History or evidence of diabetic complications with significant end organ damage, such as

    • Proliferative retinopathy and/or macular edema;
    • Diabetic neuropathy complicated by neuropathic ulcers;
  • Screening seated systolic blood pressure >160 mm Hg and/or diastolic blood pressure >100 mm Hg after at least a 5 minute seated rest. If the blood pressure exceeds this limit, the blood pressure may be repeated 2 more times following approximately 2 minutes of rest between measurements and the median of the 3 values should be used to determine subject eligibility;

  • Male subjects with partners currently pregnant; or male subjects capable of conceiving children who are unwilling or unable to use a highly effective method of contraception as outlined in this protocol for the duration of the study and for at least 28 days after the last dose of investigational product.

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
Treatment A- PlaceboPlacebo-
Treatment B- PF-06291874PF-06291874-
Treatment D- PF-06291874PF-06291874-
Treatment E- PF-06291874PF-06291874-
Treatment C- PF-06291874PF-06291874-
Primary Outcome Measures
NameTimeMethod
Number of Participants With Treatment-Emergent Adverse Events (TEAEs), or Serious Adverse Events (SAEs), or Hypoglycemic Adverse Events (HAE) or Withdrawals Due to Adverse Events (AEs)Baseline up to 10-14 days after last dose of study drug, up to 42 days

An AE was any untoward medical occurrence attributed to study drug in a participant who received study drug. An SAE was an AE resulting in any of the following outcomes or deemed significant for any other reason: death; life threatening (immediate risk of death); initial or prolonged inpatient hospitalization; persistent or significant disability/incapacity; congenital anomaly/birth defect. An HAE was identified by characteristic symptoms or blood glucose levels. TEAEs are events between first dose of study drug and up to 10-14 days after last dose of study drug that were absent before treatment or that worsened relative to pre-treatment state.

Number of Participants With Laboratory Test AbnormalitiesBaseline up to 10-14 days after last dose of study drug, up to 42 days

The total number of participants with laboratory test abnormalities (without regard to baseline abnormality) was assessed. Clinical laboratory tests included hematology, chemistry, urinalysis, and some other tests.

Number of Participants With Change From Baseline and Absolute Values in Vital Signs Meeting Criteria of Potential Clinical ConcernBaseline up to 10-14 days after last dose of study drug, up to 42 days

Vital Signs included seated supine systolic and diastolic blood pressure (BP) and pulse rate. Vital signs criteria of potential clinical concern were 1), BP: systolic (SBP) greater than or equal to (\>=) 30 millimeters of mercury (mm Hg) change from baseline, systolic less than (\<) 90 mm Hg; diastolic BP (DBP) \>=20 mm Hg change from baseline, diastolic \<50 mm Hg; 2), pulse rate \<40 or greater than (\>) 120 beats per minute (bpm).

Number of Participants With Electrocardiogram (ECG) Data Meeting Criteria of Potential Clinical ConcernBaseline up to 10-14 days after last dose of study drug, up to 42 days

ECG criteria of potential clinical concern were 1), time from ECG Q wave to the end of the S wave corresponding to ventricle depolarization (QRS interval): \>=140 msec; \>=50% increase from baseline; 2), the interval between the start of the P wave and the start of the QRS complex, corresponding to the time between the onset of the atrial depolarization and onset of ventricular depolarization (PR interval): \>=300 milliseconds (msec); \>=25 percent (%) increase when baseline \>200 msec; or increase \>=50% when baseline less than or equal to (\<=)200 msec; 3), time from ECG Q wave to the end of the T wave corresponding to electrical systole corrected for heart rate using Fridericia's formula (QTcF interval): absolute value \>=450 - \<480 msec, \>=480-\<500 msec, \>=500 msec; increase from baseline \>=30 - \<60, \>=60 msec.

Secondary Outcome Measures
NameTimeMethod
Change From Baseline in Mean Daily GlucoseBaseline and Day 28

The mean daily glucose was determined from the area under the concentration (AUC) of the glucose concentrations measured at nominal times 0, 0.5, 1, 1.5, 2, 4, 6, 10, 12, 15 and 24 hours post dose. Mean daily glucose change from baseline (defined as Day 0) on Day 28.

Change From Baseline in Fasting Plasma GlucoseBaseline, Day 14 and the mean of Days 28 and 29

Fasting plasma glucose response change from baseline (defined as the mean of Day 0 and Day 1 pre-dose) on Day 14, and the mean of Days 28 and 29.

Percent Change From Baseline in TriglyceridesBaseline, Day 14 and the mean of Days 28 and 29

Triglycerides percent change from baseline (defined as the mean of Day 0 and Day 1 pre-dose) on Day 14, and the mean of Days 28 and 29.

Percent Change From Baseline in Total CholesterolBaseline, Day 14 and the mean of Days 28 and 29

Total cholesterol percent change from baseline (defined as the mean of Day 0 and Day 1 pre-dose) on Day 14, and the mean of Days 28 and 29.

Percent Change From Baseline in Low Density Lipoprotein-Cholesterol (LDL-C)Baseline, Day 14 and the mean of Days 28 and 29

LDL-C percent change from baseline (defined as the mean of Day 0 and Day 1 pre-dose) on Day 14, and the mean of Days 28 and 29.

Percent Change From Baseline in High Density Lipoprotein-Cholesterol (HDL-C)Baseline, Day 14 and the mean of Days 28 and 29

HDL-C percent change from baseline (defined as the mean of Day 0 and Day 1 pre-dose) on Day 14, and the mean of Days 28 and 29.

Percent Change From Baseline in Non-HDL-CBaseline, Day 14 and the mean of Days 28 and 29

Non-HDL-C percent change from baseline (defined as the mean of Day 0 and Day 1 pre-dose) on Day 14, and the mean of Days 28 and 29.

Percent Change From Baseline in Oxidized LDLBaseline and the mean of Days 28 and 29

Oxidized LDL percent change from baseline (defined as the mean of Day 0 and Day 1 pre-dose) on Day 28 (the mean of Days 28 and 29).

Percent Change From Baseline in Large LDL ParticlesBaseline and the mean of Days 28 and 29

Large LDL particles percent change from baseline (defined as the mean of Day 0 and Day 1 pre-dose) on Day 28 (the mean of Days 28 and 29).

Percent Change From Baseline in Medium Small LDL ParticlesBaseline and the mean of Days 28 and 29

Medium small LDL particles percent change from baseline (defined as the mean of Day 0 and Day 1 pre-dose) on Day 28 (the mean of Days 28 and 29).

Percent Change From Baseline in Small LDL ParticlesBaseline and the mean of Days 28 and 29

Small LDL particles percent change from baseline (defined as the mean of Day 0 and Day 1 pre-dose) on Day 28 (the mean of Days 28 and 29).

Percent Change From Baseline in Very Small LDL ParticlesBaseline and the mean of Days 28 and 29

Very small LDL particles percent change from baseline (defined as the mean of Day 0 and Day 1 pre-dose) on Day 28 (the mean of Days 28 and 29).

Percent Change From Baseline in Total LDL ParticlesBaseline and the mean of Days 28 and 29

Total LDL particles percent change from baseline (defined as the mean of Day 0 and Day 1 pre-dose) on Day 28 (the mean of Days 28 and 29).

Percent Change From Baseline in LDL SizeBaseline and the mean of Days 28 and 29

The LDL size percent change from baseline (defined as the mean of Day 0 and Day 1 pre-dose) on Day 28 (the mean of Days 28 and 29).

Percent Change From Baseline in Apolipoprotein B100Baseline and the mean of Days 28 and 29

The Apolipoprotein B100 was calculated as the difference between total Apolipoprotein B and Apolipoprotein B48 and analyzed the percent change from baseline (defined as mean of Day 0 and Day 1) on Day 28 (mean of Days 28 and 29).

Percent Change From Baseline in Lipoprotein ABaseline and the mean of Days 28 and 29

The Lipoprotein A percent change from baseline (defined as the mean of Day 0 and Day 1 pre-dose) on Day 28 (mean of Days 28 and 29).

Maximum Plasma Concentration (Cmax)Day 28 (samples taken at 0, 2, 4, 8 and 24 hours after Day 28 dose)

Maximum PF-06291874 plasma concentration.

Time to Reach Cmax (Tmax)Day 28 (samples taken at 0, 2, 4, 8 and 24 hours after Day 28 dose)

Time to maximum PF-06291874 plasma concentration.

Area Under the Concentration-Time Profile From Zero to Time Tau (AUCtau) (Where Tau=24 Hours)Day 28 (samples taken at 0, 2, 4, 8 and 24 hours after Day 28 dose)

Area under the PF-06291874 plasma concentration-time profile from time zero to time tau, the dosing interval, where tau=24 hours.

Minimum Plasma Concentration (Cmin)Day 28 (samples taken at 0, 2, 4, 8 and 24 hours after Day 28 dose)

Minimum PF-06291874 plasma concentration.

Apparent Clearance (CL/F)Day 28 (samples taken at 0, 2, 4, 8 and 24 hours after Day 28 dose)

Apparent oral clearance of PF-06291874.

Trial Locations

Locations (18)

Compass Research, LLC

🇺🇸

Orlando, Florida, United States

Profil Institute for Clinical Research, Inc.

🇺🇸

Chula Vista, California, United States

Rainier Clinical Research Center, Inc.

🇺🇸

Renton, Washington, United States

MRA Clinical Research

🇺🇸

South Miami, Florida, United States

Miami Research Associates, Inc.

🇺🇸

South Miami, Florida, United States

Anaheim Clinical Trials, LLC

🇺🇸

Anaheim, California, United States

SeaView Research, Inc.

🇺🇸

Miami, Florida, United States

Avail Clinical Research, LLC

🇺🇸

DeLand, Florida, United States

MRA Clinical Research, LLC

🇺🇸

South Miami, Florida, United States

Louisville Metabolic and Atherosclerosis Research Center

🇺🇸

Louisville, Kentucky, United States

Clinical Trials of Texas, Inc.

🇺🇸

San Antonio, Texas, United States

Buffalo Clinical Research Center, LLC

🇺🇸

Buffalo, New York, United States

Clinilabs, Inc.

🇺🇸

Eatontown, New Jersey, United States

Community Research

🇺🇸

Cincinnati, Ohio, United States

DaVita Clinical Research

🇺🇸

Minneapolis, Minnesota, United States

Diablo Clinical Research, Inc.

🇺🇸

Walnut Creek, California, United States

PRA International

🇺🇸

Marlton, New Jersey, United States

High Point Clinical Trials Center, LLC

🇺🇸

High Point, North Carolina, United States

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