Lofexidine Mass Balance in Volunteers

NCT01629446 | Completed Phase 1

• 2 other identifiers: USWM-LX1-1003-11R01DA030916-01
• Study Type: interventional
• Target: 6
• Locations: 1 country
• Sites: 1

Brief 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.

Conditions

Normal Healthy Volunteers

Keywords

Phase 1; Normal healthy volunteers; Mass Balance

Outcome Measures

Primary Outcomes (1)

• Mass Balance

  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).

  plasma, urine, and fecal samples up to 216 hours post dose

Secondary Outcomes (1)

• tolerability of lofexidine oral solution

  plasma samples over 144 hours post dose

Study Arms (1)

Lofexidine HCl with 14C tracer

EXPERIMENTAL

Drug: Lofexidine hydrochloride

Interventions

Lofexidine hydrochloride DRUG

Single Dose = Solution containing 400 μg lofexidine HCl and a tracer amount of 14C lofexidine

Lofexidine HCl with 14C tracer

Eligibility Criteria

• Age: 18 Years - 50 Years
• Sex: male
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Subject must be a male
• Subject must be between 18 and 50 years of age (inclusive).
• Subject's Body Mass Index (BMI) must be between 18 and 30 kg/m2 (inclusive), and subject must weigh a minimum of 50 kg (110 lbs).
• Subject must voluntarily consent to participate in this study and provide their written informed consent prior to start of any study-specific procedures.
• Subject is willing and able to remain in the study unit for the entire duration of each confinement period.
• Subject's vital signs must be within the following ranges to be included: Vital signs measured sitting after 3 minutes rest; heart rate: 50-90 bpm; systolic BP: 100-140 mmHg; and diastolic BP: 50-90 mmHg. Out-of-range vital signs may be repeated once. Predose vital signs will be assessed by the Principal Investigator or designee (e.g., a medically qualified sub-investigator) prior to study drug administration. The Principal Investigator or designee will verify the eligibility of each subject with out-of-range vital signs and document approval prior to dosing.
• Subject is willing to eat entire meals and snacks provided during confinement at the research facility; and understand that the diet will include foods with high fiber content and possibly prune juice.
• Subject is willing to remain in the clinical research center for a minimum of 7 consecutive days during pre-dose, dose, and post-dose evaluation periods.
• Subject is willing to collect all urine and fecal samples for the duration of the study period as required.
• Subject is willing to use a waterless commode located in a designated dry room for urine and feces collection for the duration of the study period as required.
• Subject is willing to abstain from showering for the first 72 to 96 hours following dose administration. After the restriction from showering is lifted, subject must be willing to provide a urine sample prior to showering for the remainder of the confinement period.

You may not qualify if:

• History or presence of clinically significant cardiovascular, pulmonary, hepatic, renal, hematologic, gastrointestinal, endocrine, immunologic, dermatologic, neurologic, oncologic, or psychiatric disease or any other condition that, in the opinion of the Investigator, would jeopardize the safety of the subject or the validity of the study results.
• Has a clinically significant abnormal finding on the physical exam, medical history, ECG, or clinical laboratory results at screening.
• History of any syncopal episode or seizures.
• Presence of acute disease state (eg, nausea, vomiting, fever, diarrhea) within 7 days prior to scheduled dose administration.
• History or presence of allergic or adverse response to lofexidine or related drugs.
• Has been on a significantly abnormal diet during the 4 weeks preceding the first dose of study medication.
• Has donated blood or plasma within 30 days prior to the first dose of study medication.
• Has participated in a standard radiolabeled clinical trial within the last 12 months prior to the first dose of study medication or a micro tracer clinical trial within the last 3 months prior to the first dose of study medication.
• Has participated in another clinical trial (randomized subjects only) within 30 days prior to the first dose of study medication.
• Has used any over-the-counter (OTC) medication, including nutritional supplements, within 7 days prior to the first dose of study medication.
• Has used any prescription medication within 14 days prior to the first dose of study medication.
• Has been treated with any known drugs that are moderate or strong inhibitors/inducers of CYP enzymes such as barbiturates, phenothiazines, cimetidine, carbamazepine, etc., within 30 days prior to the first dose of study medication and that in the Investigator's judgment may impact subject safety or the validity of the study results.
• Has smoked or used tobacco products within 60 days prior to the first dose of study medication.
• Has any prior history of substance abuse or treatment (including alcohol) within the past 2 years.
• Has a positive urine screen for drugs of abuse (amphetamines, barbiturates, benzodiazepines, cocaine, cannabinoids, opiates).

Sponsors & Collaborators

• USWM, LLC (dba US WorldMeds): lead
• National Institute on Drug Abuse (NIDA): collaborator

Study Sites (1)

Worldwide Clinical Trials

San Antonio, Texas, 78217, United States

Location

MeSH Terms

Interventions

lofexidine

Study Officials

• James A Longstreth, PhD

  US WorldMeds

  PRINCIPAL INVESTIGATOR

• Charles W Gorodetzky, MD, PhD

  US WorldMeds

  PRINCIPAL INVESTIGATOR

• Mark Leibowitz, MD

  Worldwide Clinical Trials

  PRINCIPAL INVESTIGATOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NA
• Masking: NONE
• Purpose: BASIC SCIENCE
• Intervention Model: SINGLE GROUP
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: June 14, 2012
• First Posted: June 27, 2012
• Study Start: May 1, 2012
• Primary Completion: June 1, 2012
• Study Completion: June 1, 2012
• Last Updated: October 26, 2017

Record last verified: 2017-10

Locations

US (1)