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A Study of PF-05175157 in Healthy Volunteers and Type 2 Diabetic Patients

Phase 1
Completed
Conditions
Diabetes Mellitus, Type 2
Interventions
Registration Number
NCT01396161
Lead Sponsor
Pfizer
Brief Summary

The primary purpose of this study is to evaluate the safety, tolerability, pharmacokinetics and pharmacodynamics of multiple ascending doses of PF-05175157 in healthy volunteers and patients with type 2 diabetes mellitus.

Detailed Description

Not available

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
64
Inclusion Criteria
  • Healthy male and/or female subjects between the ages of 18 and 55 years, inclusive. Healthy is defined as no clinically relevant abnormalities identified by a detailed medical history, full physical examination, including blood pressure and pulse rate measurement, 12 lead ECG and clinical laboratory tests.
  • In addition, subjects must have normal pulmonary function tests and normal ocular examination.
  • Body Mass Index (BMI) of 25.5 - 35.5 kg/m2; and a total body weight >50 kg (110 lbs).
  • Women must be of non-childbearing potential.
  • Subjects with type 2 diabetes: HbA1c ≥7.0% and ≤10.0% if on metformin only, and ≥6.5% and ≤9.0% if patient requires to be washed-off an SU or DPP-4i.
  • For subjects with type 2 diabetes, due to possible effects on disposition, CYP P450 3A4/5 and 2D6 substrates should not be co-administered with study medications.
Exclusion Criteria
  • Evidence or history of clinically significant hematological, renal, endocrine, gastrointestinal, cardiovascular, hepatic, psychiatric, neurologic, or allergic disease (including drug allergies, but excluding untreated, asymptomatic seasonal allergies at time of dosing).
  • Evidence or history of any chronic ongoing or current pulmonary disease.
  • History of smoking in the past 5 years and a history of smoking more than 10 pack years, or history or evidence of habitual use of other (non smoked) tobacco or nicotine containing products within 3 months of Screening, or positive cotinine test at Screening or Day -3.
  • Active ocular disease including infection, glaucoma, seasonal allergies, dry eye symptoms or retinal/optic nerve disease.

Study & Design

Study Type
INTERVENTIONAL
Study Design
Not specified
Arm && Interventions
GroupInterventionDescription
30 mg PF-05175157 or Placebo QDPF-05175157 or Placebo-
100 mg PF-05175157 or Placebo BIDPF-05175157 or PlaceboPlanned dose might be modified based on emerging safety and PK data.
200 mg PF-05175157 or Placebo QDPF-05175157 or PlaceboPlanned dose might be modified based on emerging safety and PK data.
100 mg PF-05175157 or Placebo QDPF-05175157 or PlaceboPlanned dose might be modified based on emerging safety and PK data.
xxx mg PF-05175157PF-05175157 or PlaceboDose will be determined based on results obtained from Arms 1 to 4.
Primary Outcome Measures
NameTimeMethod
Number of Participants With Adverse Events (AEs) and Serious Adverse Events (SAEs)2 weeks

Counts of participants who had treatment-emergent adverse events (TEAEs), defined as newly occurring or worsening after first dose. Relatedness to PF-05175157 was assessed by the investigator (Yes/No). Participants with multiple occurrences of an AE within a category were counted once within the category.

Secondary Outcome Measures
NameTimeMethod
Maximum Observed Plasma Concentration (Cmax)Hour 0 (pre-dose), 0.5, 1, 2, 3, 4, 6, 8, 12, 24 hours post-dose on Day 1 and 14; at Hour 0 (pre-dose), 3.5, 12 hours post-dose for Day 4, 7 and 11
Time to Reach Maximum Observed Plasma Concentration (Tmax)Hour 0 (pre-dose), 0.5, 1, 2, 3, 4, 6, 8, 12, 24 hours post-dose on Day 1 and 14; at Hour 0 (pre-dose), 3.5, 12 hours post-dose for Day 4, 7 and 11
Area Under the Curve From Time Zero to End of Dosing Interval (AUCtau)Hour 0 (pre-dose), 0.5, 1, 2, 3, 4, 6, 8, 12, 24 hours post-dose on Day 1 and 14; at Hour 0 (pre-dose), 3.5, 12 hours post-dose for Day 4, 7 and 11
Accumulation Ratio for Area Under the Concentration-Time Curve (Rˇac, AUC)Hour 0 (pre-dose), 0.5, 1, 2, 3, 4, 6, 8, 12, 24 hours post-dose on Day 1 and 14; at Hour 0 (pre-dose), 3.5, 12 hours post-dose for Day 4, 7 and 11

Rˇac for the AUC is defined as AUC (τ, single dose \[ss\]) / AUC (τ, multiple dose \[sd\]).

Renal Clearance (CLr)Hour 0 (pre-dose), 0.5, 1, 2, 3, 4, 6, 8, 12, 24 hours post-dose on Day 1 and 14; at Hour 0 (pre-dose), 3.5, 12 hours post-dose for Day 4, 7 and 11

CLr is the amount of unchanged drug excreted in the participants urine from time zero to end of dosing interval.

Plasma Decay Half-Life (t1/2)Hour 0 (pre-dose), 0.5, 1, 2, 3, 4, 6, 8, 12, 24 hours post-dose on Day 1 and 14; at Hour 0 (pre-dose), 3.5, 12 hours post-dose for Day 4, 7 and 11

Plasma decay half-life is the time measured for the plasma concentration to decrease by one half.

Urinary RecoveryHour 0 (pre-dose), 0.5, 1, 2, 3, 4, 6, 8, 12, 24 hours post-dose on Day 1 and 14; at Hour 0 (pre-dose), 3.5, 12 hours post-dose for Day 4, 7 and 11

Percentage of PF-05175157 excreted unchanged in urine over the dosing interval.

Trial Locations

Locations (3)

MRA Clinical Research

🇺🇸

South Miami, Florida, United States

Miami Research Associates

🇺🇸

South Miami, Florida, United States

Pulmonary Physicians of South Florida

🇺🇸

South Miami, Florida, United States

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