Lofexidine Food Effect Study in Healthy Volunteers

NCT01437306 | Completed Phase 1

• 2 other identifiers: USWM-LX1-10041R01DA030916-01
• Study Type: interventional
• Target: 13
• Locations: 1 country
• Sites: 1

Brief Summary

The objective of this single-dose, open-label, randomized, two-period, two-way crossover, food-effect study is to evaluate the effect of food on the rate of absorption and oral bioavailability of a test formulation of lofexidine 400 μg (2 x 200 μg tablet) manufactured by US WorldMeds, LLC.

Conditions

Healthy

Keywords

lofexidine; food effect; pharmacokinetics; healthy volunteer

Outcome Measures

Primary Outcomes (1)

• Comparative Profile Pharmacokinetics TimeFrame 0.5, 1, 2, 3, 4, 5, 7, 10, 16, 24, 30, 36 and 48 hours post dose for Cmax, Tmax, Area Under the Curve, Elimination Rate Constant and Elimination Half Life

  Samples will be analyzed for lofexidine concentration and calculations will be performed for the following: Cmax and Tmax will be taken directly from the data. The elimination rate constant, will be calculated as the negative of the slope of the terminal log-linear segment of the plasma concentration time curve. Elimination half-life (T½) as follows: T½ = ln(2) / λZ Area under the curve will be calculated using the linear trapezoidal method and extrapolated to infinity using: AUCinf = AUClast + Clast/ λZ where Clast is the final concentration LOQ.

  48 Hours Following Each Dose

Study Arms (2)

Lofexidine following overnight fast

EXPERIMENTAL

A single dose of lofexidine (400 mcg or 2 x 200 mcg tablets) will be given to subjects following a minimum 10 hour overnight fast.

Drug: Lofexidine HCl

Lofexidine Following a High Fat Meal

EXPERIMENTAL

A single dose of lofexidine 400 mcg (or 2 x 200 mcg tablets) will be administered to subjects following a standard high-fat meal.

Drug: Lofexidine HCl

Interventions

Lofexidine HCl DRUG

400 mcg (2 x 200 mcg tablets) administered orally as a single dose

Lofexidine Following a High Fat Meal; Lofexidine following overnight fast

Eligibility Criteria

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

You may qualify if:

• All subjects must satisfy the following criteria to be considered for study participation:
• Subject must be a male or non-pregnant, non-breastfeeding female.
• 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).
• Female subjects must agree to use one of the following forms of birth control from screening until 14 days after completion of the study:
• Vasectomized partner (at least 6 months prior to dosing)
• Post-menopausal (at least 2 years prior to dosing)
• Surgically sterile (bilateral tubal ligation, hysterectomy, bilateral oophorectomy) at least 6 months prior to dosing
• Double barrier (diaphragm with spermicide; condoms with spermicide)
• IUD (intrauterine device)
• Abstinence (must agree to use a double barrier method if they become sexually active during the study)
• Implanted or intrauterine hormonal contraceptives in use for at least 6 consecutive months prior to study dosing and throughout the study duration
• Oral, patch, and injected contraceptives or vaginal hormonal device (i.e. NuvaRing®) in use for at least 3 consecutive months prior to study dosing and throughout the study duration.
• 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.

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, electrocardiogram (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 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, except hormonal contraceptive or hormonal replacement therapy, within 14 days prior to the first dose of study medication.
• Subjects that have discontinued the use of implanted, intrauterine, or injected hormonal contraceptives must not have used any for 6 months prior to the first dose of study medication.
• Subjects that have discontinued the use of oral, patch, or vaginal hormonal contraceptives must not have used any for 1 month 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.

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

• Charles W Gorodetzky, MD, PhD

  US WorldMeds

  PRINCIPAL INVESTIGATOR

• James A Longstreth, PhD

  US WorldMeds

  PRINCIPAL INVESTIGATOR

Study Design

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

Study Record Dates

• First Submitted: September 13, 2011
• First Posted: September 20, 2011
• Study Start: October 1, 2011
• Primary Completion: October 1, 2011
• Study Completion: October 1, 2011
• Last Updated: February 23, 2018

Record last verified: 2018-02

Locations

US (1)