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

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

Status

Completed

Phases

Phase 1

Study type

Interventional

Source

ClinicalTrials.gov

Registry ID

NCT01603485

Enrollment

Registered

2012-05-22

Start date

2012-06-30

Completion date

2012-08-31

Last updated

2012-09-19

For informational purposes only — not medical advice. Sourced from public registries and may not reflect the latest updates. Terms

Conditions

Healthy Volunteer

Keywords

Bioavailability, Pharmacokinetics, Lersivirine, Modified-release

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.

Interventions

DRUGLersivirine Immediate-Release (fasted)

Single 500 mg dose of Lersivirine Immediate-Release Tablets (2 x 250 mg)

DRUGLersivirine Modified-Release #1 (fasted)

Single 500 mg dose of Lersivirine Modified-Release Tablet #1

DRUGLersivirine Modified-Release #2 (fasted)

Single 500 mg dose of Lersivirine Modified-Release Tablet #2

DRUGLersivirine Modified-Release #3 (fasted)

Single 500 mg dose of Lersivirine Modified-Release Tablet #3

DRUGLersivirine Modified-Release (fed)

Single 500 mg dose of Lersivirine Modified-Release Tablet dosed with food.

Study design

Allocation

Intervention model

SINGLE_GROUP

Primary purpose

BASIC_SCIENCE

Masking

NONE

Eligibility

Sex/Gender

ALL

Age

18 Years to 55 Years

Healthy volunteers

Yes

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.

Design outcomes

Primary

Measure	Time frame
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
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

Secondary

Measure	Time frame
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 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
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

Countries

Belgium

Outcome results

None listed

Source: ClinicalTrials.gov · Data processed: Mar 8, 2026