NCT01707082

Brief Summary

Part A of the study will test the safety, the amount of drug in the body, and effects of the drug in the body after multiple doses. This will be conducted in healthy overweight adults. Part B of the study will test the effects of multiple doses of the investigational drug on the amount of midazolam, an approved drug, in healthy adults.

Trial Health

87
On Track

Trial Health Score

Automated assessment based on enrollment pace, timeline, and geographic reach

Enrollment
69

participants targeted

Target at P75+ for phase_1 healthy

Timeline
Completed

Started Oct 2012

Typical duration for phase_1 healthy

Geographic Reach
1 country

1 active site

Status
completed

Health score is calculated from publicly available data and should be used for screening purposes only.

Trial Relationships

Click on a node to explore related trials.

Study Timeline

Key milestones and dates

Study Start

First participant enrolled

October 1, 2012

Completed
2 days until next milestone

First Submitted

Initial submission to the registry

October 3, 2012

Completed
12 days until next milestone

First Posted

Study publicly available on registry

October 15, 2012

Completed
7 months until next milestone

Primary Completion

Last participant's last visit for primary outcome

May 1, 2013

Completed
Same day until next milestone

Study Completion

Last participant's last visit for all outcomes

May 1, 2013

Completed
Last Updated

July 31, 2013

Status Verified

July 1, 2013

Enrollment Period

7 months

First QC Date

October 3, 2012

Last Update Submit

July 29, 2013

Conditions

Healthy

Outcome Measures

Primary Outcomes (18)

  • Maximum Observed Plasma Concentration (Cmax)

    Pre-dose,0.5,1,2,3,4,5,6,7,8 and 16 hrs post morning dose Day 1 Part A

  • Time to Reach Maximum Observed Plasma Concentration (Tmax)

    Pre-dose,0.5,1,2,3,4,5,6,7,8 and 16 hrs post morning dose Day 1 Part A

  • Area Under the Curve from Time Zero to end of dosing interval (AUCtau)

    Pre-dose,0.5,1,2,3,4,5,6,7,8 and 16 hrs post morning dose Day 1 Part A

  • Apparent Oral Clearance (CL/F)

    Pre-dose,0.5,1,2,3,4,5,6,7,8 and 16 hrs post morning dose Day 1 Part A

  • Maximum Observed Plasma Concentration (Cmax)

    Pre-dose,0.5,1,2,3,4,5,6,7,8,10,12,16,24,36, and 48 hrs post morning dose Day 14 Part A

  • Time to Reach Maximum Observed Plasma Concentration (Tmax)

    Pre-dose,0.5,1,2,3,4,5,6,7,8,10,12,16,24,36, and 48 hrs post morning dose Day 14 Part A

  • Area Under the Curve from Time Zero to end of dosing interval (AUCtau)

    Pre-dose,0.5,1,2,3,4,5,6,7,8,10,12,16,24,36, and 48 hrs post morning dose Day 14 Part A

  • Minimum Observed Plasma Trough Concentration (Cmin)

    Pre-dose,0.5,1,2,3,4,5,6,7,8,10,12,16,24,36, and 48 hrs post morning dose Day 14 Part A

  • Apparent Oral Clearance (CL/F)

    Pre-dose,0.5,1,2,3,4,5,6,7,8,10,12,16,24,36, and 48 hrs post morning dose Day 14 Part A

  • Plasma Decay Half-Life (t1/2)

    Pre-dose,0.5,1,2,3,4,5,6,7,8,10,12,16,24,36, and 48 hrs post morning dose Day 14 Part A

  • Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast)

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

    Pre-dose,0.5,1,2,3,4,5,6,8,10,12 and 16 hrs post dose Day 1 Period 1 Part B

  • Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast)

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

    -2,-1.5,-1,Pre-dose,1,2,4,6,8,10,14 Day 14 Period 2 Part B

  • Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - 8)]

    AUC (0 - 8)= Area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time (0 - 8). It is obtained from AUC (0 - t) plus AUC (t - 8). Midazolam

    Pre-dose,0.5,1,2,3,4,5,6,8,10,12 and 16 hrs post dose Day 1 Period 1 Part B

  • Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - 8)]

    AUC (0 - 8)= Area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time (0 - 8). It is obtained from AUC (0 - t) plus AUC (t - 8). Midazolam

    -2,-1.5,-1,Pre-dose,1,2,4,6,8,10,14 Day 14 Period 2 Part B

  • Maximum Observed Plasma Concentration (Cmax)

    Pre-dose,0.5,1,2,3,4,5,6,8,10,12 and 16 hrs post dose Day 1 Period 1 Part B

  • Maximum Observed Plasma Concentration (Cmax)

    -2,-1.5,-1,Pre-dose,1,2,4,6,8,10,14 Day 14 Period 2 Part B

  • Average Concentration (Cav)

    Pre-dose,0.5,1,2,3,4,5,6,7,8,10,12,16,24,36, and 48 hrs post morning dose Day 14 Part A

  • Accumulation Ratio

    Pre-dose,0.5,1,2,3,4,5,6,7,8,10,12,16,24,36, and 48 hrs post morning dose Day 14 Part A

Secondary Outcomes (12)

  • Diastolic Blood Pressure

    Day 1 Pre-dose,1,2,4,8,12 and 16 hrs post dose Part A

  • Diastolic Blood Pressure

    Day 13 Pre-dose,1,2,4,8,12 and 16 hrs post dose Part A

  • Systolic Blood Pressure

    Day 1 Pre-dose,1,2,4,8,12 and 16 hrs post dose Part A

  • Systolic Blood Pressure

    Day 13 Pre-dose,1,2,4,8,12 and 16 hrs post dose Part A

  • interleukin-6

    Days 1 and 14 pre-dose Part A

  • +7 more secondary outcomes

Study Arms (7)

Part A Cohort 1

EXPERIMENTAL
Drug: PF-06282999Drug: Placebo

Part A Cohort 2

EXPERIMENTAL
Drug: PF-06282999Drug: Placebo

Part A Cohort 3

EXPERIMENTAL
Drug: PF-06282999Drug: Placebo

Part A Cohort 4

EXPERIMENTAL
Drug: PF-06282999Drug: Placebo

Part A Cohort 5

EXPERIMENTAL
Drug: PF-06282999Drug: Placebo

Part B Cohort 1

EXPERIMENTAL
Drug: midazolamDrug: PF-06282999

Part B Cohort 2

EXPERIMENTAL
Drug: midazolamDrug: PF-06282999

Interventions

PF-06282999DRUG

Tablet, 10 mg, every 8 hours, 14 days

Part A Cohort 1
PlaceboDRUG

Tablet, 0 mg, every 8 hours, 14 days

Part A Cohort 1
midazolamDRUG

Tablet, 7.5 mg, single dose on Period 1 Day 1 and Period 2 Day 14

Part B Cohort 1

Eligibility Criteria

Age18 Years - 55 Years
Sexall
Healthy VolunteersYes
Age GroupsAdult (18-64)

You may qualify if:

  • 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). Women must be of non childbearing potential.
  • Body Mass Index (BMI) of 27.0 to 35.0 kg/m2 (Part A) or 17.5 to 30.5 kg/m2 (Part B); and a total body weight \>50 kg (110 lbs).

You may not qualify if:

  • Evidence or history of clinically significant hematological, renal, endocrine, pulmonary, gastrointestinal, cardiovascular, hepatic, psychiatric, neurologic, or allergic disease (including clinically significant drug allergies, but excluding untreated, asymptomatic, seasonal allergies at time of dosing).
  • Subject with any contraindication to midazolam according to the country specific labeling or subject with previous intolerance or allergy to benzodiazepines (applicable to Part B of study only).
  • Subjects who were enrolled in Part A are excluded from participation in Part B of this study.
  • Subjects who have previously participated in a study with PF-06282999.

Contact the study team to confirm eligibility.

Sponsors & Collaborators

Study Sites (1)

Pfizer Investigational Site

Brussels, B-1070, Belgium

Location

Related Links

MeSH Terms

Interventions

2-(6-(5-chloro-2-methoxyphenyl)-4-oxo-2-thioxo-3,4-dihydropyrimidin-1(2H)-yl)acetamideMidazolam

Intervention Hierarchy (Ancestors)

BenzodiazepinesBenzazepinesHeterocyclic Compounds, 2-RingHeterocyclic Compounds, Fused-RingHeterocyclic Compounds

Study Officials

  • Pfizer CT.gov Call Center

    Pfizer

    STUDY DIRECTOR

Study Design

Study Type
interventional
Phase
phase 1
Allocation
RANDOMIZED
Masking
DOUBLE
Who Masked
PARTICIPANT, INVESTIGATOR
Purpose
BASIC SCIENCE
Intervention Model
PARALLEL
Sponsor Type
INDUSTRY
Responsible Party
SPONSOR

Study Record Dates

First Submitted

October 3, 2012

First Posted

October 15, 2012

Study Start

October 1, 2012

Primary Completion

May 1, 2013

Study Completion

May 1, 2013

Last Updated

July 31, 2013

Record last verified: 2013-07

Locations

BE(1)