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lofexidine

Trade name: lucemyra

Small moleculeapprovedFast Track FDA

Approved

May 16, 2018

Lofexidine is newly FDA approved in the United States under the brand name LUCEMYRA for the treatment of opioid withdrawal symptoms in adults. Lofexidine acts as an agonist to α2 adrenergic receptors. These receptors inhibit adenylyl cyclase activity, leading to the inhibition of the second messenger, cyclic adenosine monophosphate (cAMP). The inhibition of cAMP leads to potassium efflux through calcium-activated channels, blocking calcium ions from entering the nerve terminal, resulting in suppression of neural firing, inhibition of norepinephrine release. Lofexidine replaces the opioid-driven inhibition of cAMP production and moderating the symptoms of opioid withdrawal. — NCATS

Clinical trial activity

39 trials · 22 clinical orgs · 2 marketing orgs

Phase 1
18
Phase 2
15
Phase 3
6
Phase 4
3

Earliest trial started Apr 1, 1996 (NCT00000345)

Timeline

1990s

  1. Jan 1, 1996

    Earliest Phase 1 Sponsor(trial)

2000s

  1. Jan 1, 2001

    Earliest Phase 3 Sponsor(trial)

  2. Jan 1, 2005

    Earliest Phase 2 Sponsor(trial)

2010s

  1. May 16, 2018

    US WorldMeds — Earliest FDA Approval

  2. May 16, 2018

    US WorldMeds — NDA Secondary Org

  3. May 16, 2018

    US WorldMeds — NDA Organization

  4. May 16, 2018

    US WorldMeds — Marketing Organization

2020s

  1. Aug 20, 2024

    Indoco Remedies — Marketing Organization

Indications

Approved for

Studied for

Mechanism of action

Approval history

  • approvedPriority reviewFast trackMay 16, 2018

Chemistry & pharmacology

Loading structure…

SMILES

CC(Oc1c(Cl)cccc1Cl)C1=NCCN1
Mol. weight
259.14 g/mol
Lipinski Ro5
Pass
Rule of 3
Yes
Chirality
Racemic Mixture
Inorganic
No
Polymer
No
Delivery
Oral
Availability
Prescription Only

Oral

Yes

Parenteral

No

Topical

No

First in class

Sources

Also known as

  • 1h-imidazole, 2-(1-(2,6-dichlorophenoxy)ethyl)-4,5-dihydro-
  • 2-(alpha-(2,6-dichlorophenoxy)ethyl)2-imidazoline
  • 2-(alpha-(2,6-dichlorophenoxy)ethyl)2-imidazoline
  • 2-(alpha-(2,6-dichlorophenoxy)ethyl) delta-2-imidazoline
  • britlofex
  • britlofex
  • britlofex
  • lofexadine
  • lofexidina
  • lofexidina
  • lofexidine
  • lofexidine
  • lofexidine
  • lofexidine
  • lofexidine
  • lofexidine
  • lofexidine
  • lofexidine
  • (+/-)-lofexidine
  • lofexidine hcl
  • lofexidine hcl
  • lofexidine hcl
  • lofexidine hydrochloride
  • lofexidine hydrochloride
  • lofexidine hydrochloride
  • lofexidine hydrochloride
  • lofexidine hydrochloride
  • lofexidine hydrochloride
  • lofexidine hydrochloride
  • lofexidine, (+-)-isomer
  • lofexidine monohydrochloride
  • lofexidine mono-hydrochloride
  • lofexidinum
  • lofexidinum
  • mdl-14042
  • mdl-14042

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT06711640Phase 1Jan 31, 2025National Institute on Drug Abuse (NIDA), US WorldMeds
NCT05995535Phase 2Jan 1, 2024University of Pennsylvania
NCT06047834Phase 2Oct 2, 2023National Institute on Drug Abuse (NIDA), US WorldMeds
NCT05511909Phase 2Dec 15, 2022Johns Hopkins University
NCT05053503N/ANov 1, 2021Spark Therapeutics
NCT05027919Phase 2Oct 1, 2021Johns Hopkins University, National Institute on Drug Abuse (NIDA)
NCT04360681Phase 2Aug 28, 2020Baylor University, Department of Defense, Department of Veteran Affairs, Pharmacotherapies for Alcohol and Substance Abuse Consortium, RTI International, US WorldMeds
NCT04325659Phase 2/Phase 3 (Phase 3)Jun 1, 2020Johns Hopkins University, National Institute on Drug Abuse (NIDA)
NCT04218240Phase 2Feb 29, 2020University of Pennsylvania
NCT04188730Phase 1Jan 31, 2020National Institute on Drug Abuse (NIDA), US WorldMeds
NCT04056182Phase 2Sep 1, 2019Columbia University, US WorldMeds
NCT04126083Phase 4Sep 1, 2019Mayo Clinic, US WorldMeds
NCT04070157Phase 2Aug 2, 2019US WorldMeds
NCT03718065Phase 2Jun 26, 2019Medical University of South Carolina, National Institute on Drug Abuse (NIDA), National Institutes of Health (NIH)
NCT05569031Phase 4Jan 1, 2019Zagazig University
NCT02801357Phase 1Jun 1, 2016US WorldMeds
NCT02681198Phase 1Feb 1, 2016National Institute on Drug Abuse (NIDA), US WorldMeds, Worldwide Clinical Trials
NCT02446002Phase 1May 1, 2015National Institute on Drug Abuse (NIDA), US WorldMeds, Worldwide Clinical Trials
NCT02363998Phase 3Feb 1, 2015National Institute on Drug Abuse (NIDA), US WorldMeds
NCT02313103Phase 1Nov 1, 2014National Institute on Drug Abuse (NIDA), US WorldMeds
Showing 20 of 39 trials
Page 1 / 2

Organizations

Research & Development (22)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
National Institute on Drug Abuse (NIDA)Government28631996
US WorldMedsFor profit211742006
University of PennsylvaniaAcademic/Hospital4221996
Worldwide Clinical TrialsFor profit4012011
Columbia UniversityAcademic/Hospital3322005
Johns Hopkins UniversityAcademic/Hospital3322020
Department of Veteran AffairsGovernment2122006
Yale UniversityAcademic/Hospital2122003
Baylor UniversityAcademic/Hospital1012020
Britannia Pharmaceuticals Ltd.For profit1012001
Department of DefenseGovernment1012020
Friends Research Institute, Inc.Academic/Hospital1011996
Government of SingaporeGovernment1112012
Mayo ClinicAcademic/Hospital1112019
Medical University of South CarolinaAcademic/Hospital1112019
National Institutes of Health (NIH)Government1012019
Orlando Clinical Research CenterFor profit1012014
Pharmacotherapies for Alcohol and Substance Abuse ConsortiumAcademic/Hospital1112020
RTI InternationalAcademic/Hospital1012020
Singapore Clinical Research InstituteAcademic/Hospital1012012
22 organizations
Page 1 / 2

Marketing (4)

OrganizationOrg typeRelationshipDate
Indoco RemediesFor profitMKTGAug 20, 2024
US WorldMedsFor profitNDA2May 16, 2018
US WorldMedsFor profitNDAMay 16, 2018
US WorldMedsFor profitMKTGMay 16, 2018