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
Choosing to participate in a study is an important personal decision. Talk with your doctor and family members or friends about deciding to join a study. To learn more about this study, you or your doctor may contact the study research staff using the Contacts provided below. For general information, see Learn About Clinical Studies.

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 August 28, 2014