Estimate The Effect Of Lersivirine On The Pharmacokinetics Of S- And R-Methadone

Open Label, Single-Sequence Study To Estimate The Effect Of Lersivirine (UK-453,061) On S- And R-Methadone In Subjects Receiving Chronic Methadone Treatment

Status

Completed

Phases

Phase 1

Study type

Interventional

Source

ClinicalTrials.gov

Registry ID

NCT01099748

Enrollment

Registered

2010-04-07

Start date

2010-05-31

Completion date

2010-06-30

Last updated

2010-08-30

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

Conditions

Healthy Volunteers

Keywords

Drug interaction, pharmacokinetics, lersivirine, methadone

Brief summary

The objective of this study is to estimate the effect of lersivirine on the pharmacokinetics of R-methadone and S-methadone and to investigate the safety and tolerability of lersivirine when co-administered with methadone. Symptoms of methadone withdrawal will also be assessed.

Interventions

DRUGMethadone

Methadone 50 - 150 mg QD (Day 1)

DRUGLersivirine + Methadone

Lersivirine 1000 mg QD + Methadone 50 - 150 mg QD (Days 2-11)

Study design

Allocation

NON_RANDOMIZED

Intervention model

CROSSOVER

Primary purpose

TREATMENT

Masking

NONE

Eligibility

Sex/Gender

ALL

Age

18 Years to 55 Years

Healthy volunteers

Yes

Inclusion criteria

* Healthy male and/or female subjects (Healthy is defined as no clinically relevant abnormalities identified by a detailed medical history except drug abuse), full physical examination, including blood pressure and pulse rate measurement, 12-lead ECG and clinical laboratory tests). * Body Mass Index (BMI) of 17.5 to 35.5 kg/m2; and a total body weight \>50 kg (110 lbs). * Receiving stable methadone maintenance treatment for at least 3 months (dose range 50-150 mg QD).

Exclusion criteria

* Subjects on therapy for Hepatitis B and/or Hepatitis C; Evidence of impaired liver function (ie, AST and/or ALT greater than 3 times the upper limit of normal, total bilirubin \>1.5 times the upper limit of normal, albumin \<3.5 g/dL). * 12-lead ECG demonstrating QTc \>450 msec for males and QTc \>470 msec for females or any other clinically significant abnormalities at screening.

Design outcomes

Primary

Measure	Time frame
R-methadone and S-methadone plasma pharmacokinetic parameters: AUC24, Cmax, Tmax, and C24h on Days 1 and 11	Day 12

Secondary

Measure	Time frame
Symptoms of methadone withdrawal as assessed by the Short Opiate Withdrawal Scale (SOWS), Desires for Drug Questionnaire (DDQ) and Pupillary Diameter measurement performed on Days 0 -12.	Day 12
Safety and toleration assessed by spontaneous reporting of adverse events, vital signs, 12-lead ECG and laboratory safety assessments	Day 12

Countries

United States

Outcome results

None listed

Source: ClinicalTrials.gov · Data processed: Feb 4, 2026