NCT01629446

Lofexidine Mass Balance in Volunteers

A Single-Center, Open-Label, Single-Period, Single-Treatment Study to Determine the Mass Balance of a Single Oral Dose of 14C Labeled Lofexidine

• Status: Completed
• Phase: Phase 1
• Study type: Interventional
• Enrollment: 6 (actual)
• Sponsor: USWM, LLC (dba US WorldMeds) · Industry
• Sex: Male
• Age: 18 Years – 50 Years
• Healthy volunteers: Accepted

Summary

The purpose of this study is to see how lofexidine (investigational study formulation drug) is absorbed, broken down, and removed from the body. To do this, a special form of the study drug will be used that has a radioactive carbon atom attached. Blood, urine, and feces samples will be collected at different times to measure the amount of the study drug and radioactivity they contain. The amount of radioactivity you will be exposed to is less than the amount of radiation from a regular X-ray.

Detailed description

The purpose of this study is to determine the mass balance of a single oral dose of 14C labeled lofexidine. Study US WorldMeds Reference Number USWM-LX1-1003, conducted in July and August of 2011, was a single-center, open-label, two-period, two-treatment, randomized sequence study to determine the mass balance and absolute bioavailability of a single oral dose of 14C-labeled lofexidine compared to a single intravenous dose of lofexidine. During the conduct of the study, deficiencies occurred in the collection and processing of urine samples from subjects administered the oral dose of 14C-labeled lofexidine. In study USWM-LX1-1003-1, six male subjects will be dosed with 14C labeled lofexidine oral solution in order to provide accurate data for the mass balance portion of the study. Male subjects who successfully participated in and completed study USWM-LX1-1003 will be enrolled first. Additional male subjects will be enrolled as needed to provide a cohort of 6 subjects. Additional provisions to ensure adequate urine collections have now been implemented at the site and will be utilized in USWM-LX1-1003-1. All blood draws for pharmacokinetic analysis and radioanalysis, and all urine and fecal collection intervals, will occur at the same time points in USWM-LX1-1003-1 as they did in USWM-LX1-1003. To study the absorption, distribution, metabolism, and elimination (ADME), trace amounts of 14C compounds are quantified using accelerator mass spectrometry (AMS). As a form of an isotope ratio atom counter that achieves the lowest detection limits of any type of mass spectrometry, AMS provides quantitative sensitivity towards 14C labeled compounds to low attomole (10-18) levels. This high degree of sensitivity enables the detection of compounds in very small specimens and/or tissues after administration of doses that can be both chemically and radiochemically small (microdose levels). At the radioactive dose to be given (approximately 280 nCi; 10.36 kBq) the total radiation exposure to the participant is within the level of background radiation exposure that occurs naturally and orders of magnitude (1000 fold reduction on average) below the levels typical for human metabolism studies using 14C tracers.

Conditions

• Normal Healthy Volunteers

Interventions

Type	Name	Description
DRUG	Lofexidine hydrochloride	Single Dose = Solution containing 400 μg lofexidine HCl and a tracer amount of 14C lofexidine

Timeline

• Start date: 2012-05-01
• Primary completion: 2012-06-01
• Completion: 2012-06-01
• First posted: 2012-06-27
• Last updated: 2017-10-26

Locations

1 site across 1 country: United States