Study to Estimate the Pharmacokinetics, Bioavailability and Effect of Food on Single Dose Modified-release Lersivirine 500 mg in Healthy Subjects

This study has been completed.
Sponsor:
Collaborator:
ViiV Healthcare
Information provided by (Responsible Party):
Pfizer
ClinicalTrials.gov Identifier:
NCT01603485
First received: May 10, 2012
Last updated: September 18, 2012
Last verified: September 2012
  Purpose

The purpose of this study is to estimate the pharmacokinetics (PK) of 3 different modified-release formulations of lersivirine and compare it to the PK of the immediate-release tablet. The effect of food on the PK of one of the modified-release tablets will also be assess along with the safety and tolerability of each treatment.


Condition Intervention Phase
Healthy Volunteer
Drug: Lersivirine Immediate-Release (fasted)
Drug: Lersivirine Modified-Release #1 (fasted)
Drug: Lersivirine Modified-Release #2 (fasted)
Drug: Lersivirine Modified-Release #3 (fasted)
Drug: Lersivirine Modified-Release (fed)
Phase 1

Study Type: Interventional
Study Design: Endpoint Classification: Bio-availability Study
Intervention Model: Single Group Assignment
Masking: Open Label
Primary Purpose: Basic Science
Official Title: Open-Label, Randomized, Crossover Study to Estimate the Pharmacokinetics, Bioavailability and Effect of Food on Single Dose Modified-Release Lersivirine (UK-453,061) 500 mg in Healthy Subjects

Further study details as provided by Pfizer:

Primary Outcome Measures:
  • Lersivirine Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - ∞)] [ Time Frame: T = 0 (predose), 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 24, 36 and 48 hours post dose ] [ Designated as safety issue: No ]
  • Lersivirine Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast) [ Time Frame: T = 0 (predose), 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 24, 36 and 48 hours post dose ] [ Designated as safety issue: No ]
  • Lersivirine Maximum Observed Plasma Concentration (Cmax) [ Time Frame: T = 0 (predose), 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 24, 36 and 48 hours post dose ] [ Designated as safety issue: No ]

Secondary Outcome Measures:
  • Lersivirine Plasma Decay Half-Life (t1/2) [ Time Frame: T = 0 (predose), 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 24, 36 and 48 hours post dose ] [ Designated as safety issue: No ]
  • Lersivirine Time to Reach Maximum Observed Plasma Concentration (Tmax) [ Time Frame: T = 0 (predose), 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 24, 36 and 48 hours post dose ] [ Designated as safety issue: No ]
  • Lersivirine Observed Plasma Concentration at time 24hr (C24) [ Time Frame: T = 24 hours post dose ] [ Designated as safety issue: No ]
  • Lersivirine Last Observed Plasma Concentration (Clast) [ Time Frame: T = 0 (predose), 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 24, 36 and 48 hours post dose ] [ Designated as safety issue: No ]

Enrollment: 16
Study Start Date: June 2012
Study Completion Date: August 2012
Primary Completion Date: August 2012 (Final data collection date for primary outcome measure)
Arms Assigned Interventions
Experimental: Lersivirine Drug: Lersivirine Immediate-Release (fasted)
Single 500 mg dose of Lersivirine Immediate-Release Tablets (2 x 250 mg)
Drug: Lersivirine Modified-Release #1 (fasted)
Single 500 mg dose of Lersivirine Modified-Release Tablet #1
Drug: Lersivirine Modified-Release #2 (fasted)
Single 500 mg dose of Lersivirine Modified-Release Tablet #2
Drug: Lersivirine Modified-Release #3 (fasted)
Single 500 mg dose of Lersivirine Modified-Release Tablet #3
Drug: Lersivirine Modified-Release (fed)
Single 500 mg dose of Lersivirine Modified-Release Tablet dosed with food.

  Eligibility

Ages Eligible for Study:   18 Years to 55 Years
Genders Eligible for Study:   Both
Accepts Healthy Volunteers:   Yes
Criteria

Inclusion Criteria:

  • Body Mass Index (BMI) of 17.5 to 30.5 kg/m2; and a total body weight >50 kg (110 lbs).
  • Subjects who are willing and able to comply with scheduled visits, treatment plan, laboratory tests, and other study procedures.

Exclusion Criteria:

  • History of regular alcohol consumption exceeding 14 drinks/week for females or 21 drinks/week for males (1 drink = 5 ounces (150 mL) of wine or 12 ounces (360 mL) of beer or 1.5 ounces (45 mL) of hard liquor) within 6 months of Screening;
  • Treatment with an investigational drug within 60 days (or as determined by the local requirement, whichever is longer) or 5 half-lives preceding the first dose of study medication;
  • Use of prescription or nonprescription drugs and dietary supplements within 7 days or 5 half-lives (whichever is longer) prior to the first dose of study medication.
  Contacts and Locations
Please refer to this study by its ClinicalTrials.gov identifier: NCT01603485

Locations
Belgium
Pfizer Investigational Site
Bruxelles, Belgium, B-1070
Sponsors and Collaborators
Pfizer
ViiV Healthcare
Investigators
Study Director: Pfizer CT.gov Call Center Pfizer
  More Information

Additional Information:
No publications provided

Responsible Party: Pfizer
ClinicalTrials.gov Identifier: NCT01603485     History of Changes
Other Study ID Numbers: A5271050
Study First Received: May 10, 2012
Last Updated: September 18, 2012
Health Authority: United States: Food and Drug Administration

Keywords provided by Pfizer:
Bioavailability
Pharmacokinetics
Lersivirine
Modified-release

ClinicalTrials.gov processed this record on April 20, 2014