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

Phase 1

Completed

• Conditions: Healthy Volunteer
• Interventions: 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)

• Registration Number: NCT01603485
• Lead Sponsor: Pfizer

Brief Summary

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.

Detailed Description

Not available

Study Timeline

• Study First Submitted: 2012-05-10
• Study First Submitted QC: 2012-05-21
• Study First Posted: 2012-05-22
• Study Start: 2012-06
• Primary Completion: 2012-08
• Study Completion: 2012-08
• Status Verified: 2012-09
• Last Update Submitted: 2012-09-18
• Last Update Posted: 2012-09-19

Recruitment & Eligibility

• Status: COMPLETED
• Sex: All
• Target Recruitment: 16

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.

Study & Design

• Study Type: INTERVENTIONAL
• Study Design: SINGLE_GROUP

Arm && Interventions

Group	Intervention	Description
Lersivirine	Lersivirine Modified-Release #3 (fasted)	-
Lersivirine	Lersivirine Immediate-Release (fasted)	-
Lersivirine	Lersivirine Modified-Release #1 (fasted)	-
Lersivirine	Lersivirine Modified-Release #2 (fasted)	-
Lersivirine	Lersivirine Modified-Release (fed)	-

Primary Outcome Measures

Name	Time	Method
Lersivirine Maximum Observed Plasma Concentration (Cmax)	T = 0 (predose), 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 24, 36 and 48 hours post dose
Lersivirine Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - ∞)]	T = 0 (predose), 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 24, 36 and 48 hours post dose
Lersivirine Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast)	T = 0 (predose), 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 24, 36 and 48 hours post dose

Secondary Outcome Measures

Name	Time	Method
Lersivirine Plasma Decay Half-Life (t1/2)	T = 0 (predose), 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 24, 36 and 48 hours post dose
Lersivirine Time to Reach Maximum Observed Plasma Concentration (Tmax)	T = 0 (predose), 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 24, 36 and 48 hours post dose
Lersivirine Observed Plasma Concentration at time 24hr (C24)	T = 24 hours post dose
Lersivirine Last Observed Plasma Concentration (Clast)	T = 0 (predose), 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 24, 36 and 48 hours post dose

Trial Locations

Locations (1)

Pfizer Investigational Site; 🇧🇪 Bruxelles, Belgium