Lofexidine

Generic Name: Lofexidine

Brand Names: Lucemyra

Drug Type: Small Molecule

Chemical Formula: C_₁₁H_₁₂Cl_₂N_₂O

CAS Number: 31036-80-3

Unique Ingredient Identifier: UI82K0T627

Background: Lofexidine is a non-opioid centrally acting alpha2-adrenergic receptor agonist that was first approved for the treatment of opioid withdrawal in the United Kingdom in 1992. It was first studied for use as an antihypertensive in 1980, but its researched was stopped as it was found less effective for the treatment of hypertension than clonidine. Lofexidine was then repurposed for the treatment of opioid withdrawal, as it was seen to be more economical and have fewer side effects than clonidine. Lofexidine was developed by US Woldmeds LLC and it was approved by the FDA on May 16, 2018.

Indication: Lofexidine is indicated for mitigation of symptoms associated with acute withdrawal from opioids and for facilitation of the completion of opioid discontinuation treatment. It is the first non-opioid medication for the symptomatic management of opioid discontinuation.

Opioid withdrawal syndrome is a debilitating manifestation of opioid dependence. This condition is extremely unpleasant lasting several days with some of the main features being abdominal pain, nausea, diarrhea, mydriasis, lacrimation, and piloerection. These symptoms are often observed after abrupt reductions in the opioid dose and can be resolved by re-administration of the opioid.

Associated Conditions: Abrupt opioid withdrawal

Clinical Trials

A Pharmacokinetic, Safety, and Tolerability Study of LUCEMYRA in the Treatment of Opioid Withdrawal Management in Adolescent Subjects

Phase 1

Not yet recruiting

Conditions: Opioid Withdrawal (Disorder)
Opioid Use Disorder

Interventions: Drug: LUCEMYRA (lofexidine) tablets

First Posted Date: 2024-12-02

Last Posted Date: 2025-05-14

Lead Sponsor: USWM, LLC (dba US WorldMeds)

Target Recruit Count: 16

Registration Number: NCT06711640

Locations: 🇺🇸
Mountain Manor Treatment Center, Baltimore, Maryland, United States

Treatment of Withdrawal Symptoms and Prevention of Relapse in Patients With Tramadol Abuse

Phase 4

Completed

Conditions: Opiate Withdrawal Syndrome

Interventions: Drug: Venlafaxine
Drug: Lofexidine

First Posted Date: 2022-10-06

Last Posted Date: 2022-10-06

Lead Sponsor: Zagazig University

Target Recruit Count: 52

Registration Number: NCT05569031

Locations: 🇪🇬
Faculty of medicine, Zagazig, Sharkia, Egypt

Evaluating Buspirone to Treat Opioid Withdrawal

Phase 2

Recruiting

Conditions: Anxiety
Opioid Withdrawal
Opioid Craving
Opioid Use Disorder

Interventions: Drug: Buspirone
Drug: Placebo
Drug: Lofexidine

First Posted Date: 2022-08-23

Last Posted Date: 2025-01-03

Lead Sponsor: Johns Hopkins University

Target Recruit Count: 100

Registration Number: NCT05511909

Locations: 🇺🇸
Behavioral Pharmacology Research Unit, Baltimore, Maryland, United States

Delivering Transcutaneous Auricular Neurostimulation to Improve Relapse Prevention in Opioid Use Disorder

Not Applicable

Completed

Conditions: Opioid-use Disorder
Opioid Withdrawal

Interventions: Drug: Lofexidine
Device: Sparrow Ascent Therapy System
Drug: Extended-release injectable naltrexone

First Posted Date: 2021-09-22

Last Posted Date: 2025-04-10

Lead Sponsor: Spark Biomedical, Inc.

Target Recruit Count: 108

Registration Number: NCT05053503

Locations: 🇺🇸
Hazelden Betty Ford Foundation, Plymouth, Minnesota, United States
🇺🇸
Gaudenzia, Inc., Crownsville, Maryland, United States

Assessing a Clinically-meaningful Opioid Withdrawal Phenotype

Phase 2

Recruiting

Conditions: Opioid Withdrawal
Opioid Use Disorder
Opioid Craving

Interventions: Drug: Morphine
Drug: Naloxone + lofexidine pretreatment
Drug: Naloxone + placebo pretreatment
Drug: Lofexidine

First Posted Date: 2021-08-31

Last Posted Date: 2025-05-01

Lead Sponsor: University of Maryland, Baltimore

Target Recruit Count: 60

Registration Number: NCT05027919

Locations: 🇺🇸
Johns Hopkins University Bayview Medical Campus, Baltimore, Maryland, United States

Lofexidine Combined With Buprenorphine for Reducing Symptoms of PTSD and OU Relapse in Veterans

Phase 2

Recruiting

Conditions: Post Traumatic Stress Disorder
Opioid-use Disorder

Interventions: Drug: Lofexidine
Drug: Placebo oral tablet

First Posted Date: 2020-04-24

Last Posted Date: 2024-11-06

Lead Sponsor: Pharmacotherapies for Alcohol and Substance Use Disorders Alliance

Target Recruit Count: 120

Registration Number: NCT04360681

Locations: 🇺🇸
South Texas Veterans Health Care System, San Antonio, Texas, United States
🇺🇸
Michael E. DeBakey Veterans Affairs Medical Center, Houston, Texas, United States

An Innovative Intervention for OUD Treatment

Phase 2

Recruiting

Conditions: Opioid-Related Disorders
Opioid Dependence
Opioid Addiction
Opioid Withdrawal

Interventions: Drug: Lofexidine
Drug: Placebo
Device: Bridge Device
Device: Sham Bridge Device

First Posted Date: 2020-03-27

Last Posted Date: 2024-10-09

Lead Sponsor: Johns Hopkins University

Target Recruit Count: 75

Registration Number: NCT04325659

Locations: 🇺🇸
Behavioral Pharmacology Research Unit, Baltimore, Maryland, United States

Combining Pregabalin (LYRICA®) With Lofexidine (LUCEMYRATM) to Treat OPIOID Withdrawal

Phase 2

Completed

Conditions: Opioid Withdrawal

Interventions: Drug: Pregabalin 200 MG capsules
Drug: Placebo oral tablet
Drug: Lofexidine 0.18Mg Tab

First Posted Date: 2020-01-06

Last Posted Date: 2024-08-28

Lead Sponsor: University of Pennsylvania

Target Recruit Count: 90

Registration Number: NCT04218240

Locations: 🇺🇸
Mountain Manor Treatment Center, Baltimore, Maryland, United States
🇺🇸
Treatment Research Center, Philadelphia, Pennsylvania, United States
🇺🇸
John Mariani, New York, New York, United States