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A Single Dose Study Of PF-06678552 In Healthy Subjects

Phase 1
Completed
Conditions
Healthy
Interventions
Drug: PF-06678552 or Placebo
Registration Number
NCT01992614
Lead Sponsor
Pfizer
Brief Summary

PF-06678552 is a new compound proposed for the treatment of hypercholesteremia. The primary purpose of this study is to evaluate the safety and tolerability, pharmacokinetics, and pharmacodynamics of single oral doses of PF-06678552 in healthy subjects.

Detailed Description

Not available

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
24
Inclusion Criteria
  • Healthy male and/or female subjects of non childbearing potential.
  • Body Mass Index (BMI) of 18 to 30.5 kg/m2; and a total body weight >50 kg
  • Low density lipoprotein cholesterol between 115 mg/dL and 190 mg/dL
Exclusion Criteria
  • Evidence or history of clinically significant hematological, renal, endocrine, pulmonary, gastrointestinal, cardiovascular, hepatic, psychiatric, neurologic, or allergic disease (including drug allergies, but excluding untreated, asymptomatic, seasonal allergies at time of dosing)

Study & Design

Study Type
INTERVENTIONAL
Study Design
CROSSOVER
Arm && Interventions
GroupInterventionDescription
Cohort 1PF-06678552 or PlaceboSingle ascending doses of PF-06678552 or placebo to investigate the safety, tolerability, PK, and PD.
Cohort 2PF-06678552 or PlaceboSingle ascending doses of PF-06678552 or placebo to investigate the safety, tolerability, PK, and PD.
Cohort 3PF-06678552 or PlaceboSingle ascending doses of PF-06678552 or placebo to investigate the safety, tolerability, PK, and PD.
Primary Outcome Measures
NameTimeMethod
Assessment of adverse events (AEs), clinical laboratory tests, vital signs (including blood pressure and pulse rate) and cardiac conduction intervals as assessed via 12-lead electrocardiogram (ECG).0 to 72 hours post dose
Secondary Outcome Measures
NameTimeMethod
Time to Reach Maximum Observed Plasma Concentration (Tmax) for PF-066785520, 0.5, 1, 2, 2.5, 3, 4, 6, 8, 12, 16, 24, 36, 48 hours post dose

Time to Reach Maximum Observed Plasma Concentration (Tmax)

Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast) for PF-066449270, 0.5, 1, 2, 2.5, 3, 4, 6, 8, 12, 16, 24, 36, 48 hours post dose

Area under the plasma concentration time-curve from zero to the last measured concentration (AUClast)

Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - infinity)] for PF-066449270, 0.5, 1, 2, 2.5, 3, 4, 6, 8, 12, 16, 24, 36, 48 hours post dose

AUC (0 - infinity)= Area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time (0 - infinity). It is obtained from AUC (0 - t) plus AUC (t - infinity).

Maximum Observed Plasma Concentration (Cmax) for PF-066449270, 0.5, 1, 2, 2.5, 3, 4, 6, 8, 12, 16, 24, 36, 48 hours post dose

Maximum Observed Plasma Concentration (Cmax)

Time to Reach Maximum Observed Plasma Concentration (Tmax) for PF-066449270, 0.5, 1, 2, 2.5, 3, 4, 6, 8, 12, 16, 24, 36, 48 hours post dose

Time to Reach Maximum Observed Plasma Concentration (Tmax)

Plasma Decay Half-Life (t1/2) for PF-066449270, 0.5, 1, 2, 2.5, 3, 4, 6, 8, 12, 16, 24, 36, 48 hours post dose

Plasma Decay Half-Life (t1/2)

Amount of PF-06644927 excreted in the urine (Ae)0-4, 4-12, and 12-24 hours post dose

Amount of drug excreted in the urine is a measure of the degree that the kidneys filter drug from the blood to the urine.

Percent of PF-06678552 dose excreted in the urine as PF-06644927 (Ae%)0-4, 4-12, and 12-24 hours post dose

The percent of PF-06678552 dose excreted in the urine as PF-06644927 is calculated from the mass of dose excreted in the urine compared to the total dose of PF-06678552 and corrected for the relative weight of PF-06644927 to PF-06678552.

Renal Clearance (CLr) for PF-066449270-4, 4-12, and 12-24 hours post dose

Renal clearance is the measure of the rate of drug moving into the urine from blood

Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - infinity)] for PF-066785520, 0.5, 1, 2, 2.5, 3, 4, 6, 8, 12, 16, 24, 36, 48 hours post dose

AUC (0 - infinity)= Area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time (0 - infinity). It is obtained from AUC (0 - t) plus AUC (t - infinity).

Apparent Oral Clearance (CL/F) for PF-066785520, 0.5, 1, 2, 2.5, 3, 4, 6, 8, 12, 16, 24, 36, 48 hours post dose

Clearance of a drug is a measure of the rate at which a drug is metabolized or eliminated by normal biological processes. Clearance obtained after oral dose (apparent oral clearance) is influenced by the fraction of the dose absorbed. Drug clearance is a quantitative measure of the rate at which a drug substance is removed from the blood.

Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast) for PF-066785520, 0.5, 1, 2, 2.5, 3, 4, 6, 8, 12, 16, 24, 36, 48 hours post dose

Area under the plasma concentration time-curve from zero to the last measured concentration (AUClast)

Maximum Observed Plasma Concentration (Cmax) for for PF-066785520, 0.5, 1, 2, 2.5, 3, 4, 6, 8, 12, 16, 24, 36, 48 hours post dose

Maximum Observed Plasma Concentration (Cmax)

Plasma Decay Half-Life (t1/2) for PF-066785520, 0.5, 1, 2, 2.5, 3, 4, 6, 8, 12, 16, 24, 36, 48 hours post dose

Plasma Decay Half-Life (t1/2)

Apparent Volume of Distribution (Vz/F) for PF-066785520, 0.5, 1, 2, 2.5, 3, 4, 6, 8, 12, 16, 24, 36, 48 hours post dose

Volume of distribution is defined as the theoretical volume in which the total amount of drug would need to be uniformly distributed to produce the desired plasma concentration of a drug. Apparent volume of distribution after oral dose (Vz/F) is influenced by the fraction absorbed.

Trial Locations

Locations (1)

Pfizer Investigational Site

🇧🇪

Brussels, Belgium

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