nalmefene

Trade name: revex

Small moleculeapproved

Approved

Apr 17, 1995

Nalmefene is the first medication approved for alcoholism with the primary goal of reducing alcohol intake in an as needed approach. Nalmefene received a marketing authorization valid throughout the European Union on February 25, 2013 and is under development in Asia. Nalmefene is an opioid system modulator with a distinct μ, δ, and κ receptor profile. In vitro studies have demonstrated that Nalmefene is a selective opioid receptor ligand with antagonist activity at the μ and δ receptors and partial agonist activity at the κ receptor. In vivo studies have demonstrated that nalmefene reduces alcohol consumption, possibly by modulating cortico-mesolimbic functions. In the US, immediate-release injectable nalmefene was approved in 1995 as an antidote for opioid overdose. It was sold under the trade name Revex. The product was discontinued by its manufacturer around 2008. Currently Nalmefene is sold under the trade name Selincro. Selincro is indicated for the reduction of alcohol consumption in adult patients with alcohol dependence who have a high drinking-risk level, without physical withdrawal symptoms and who do not require immediate detoxification. — NCATS

Clinical trial activity

34 trials · 29 clinical orgs · 5 marketing orgs

Phase 1
13
Phase 2
15
Phase 3
9
Phase 4
4

Earliest trial started Aug 1, 2005 (NCT00132119)

Timeline

1990s

  1. Apr 17, 1995

    Eurohlth Intl Sarl — Earliest FDA Approval

  2. Apr 17, 1995

    Eurohlth Intl Sarl — NDA Organization

  3. Apr 17, 1995

    Hikma — Marketing Organization

  4. Apr 17, 1995

    Eurohlth Intl Sarl — NDA Secondary Org

  5. Apr 17, 1995

    Hikma — NDA Secondary Org

2000s

  1. Jan 1, 2005

    Earliest Phase 2 Sponsor(trial)

  2. Jan 1, 2008

    Earliest Phase 3 Sponsor(trial)

2010s

  1. Jan 1, 2013

    Earliest Phase 1 Sponsor(trial)

2020s

  1. Feb 8, 2022

    Purdue Pharmaceuticals — Marketing Organization

  2. May 22, 2023

    Indivior Inc. — Marketing Organization

  3. May 22, 2023

    Indivior Inc. — NDA Secondary Org

  4. Nov 15, 2023

    CHENGDU SHUODE — Marketing Organization

Indications

Mechanism of action

Approval history

  • approvedApr 17, 1995

Chemistry & pharmacology

Loading structure…

SMILES

C=C1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5
Mol. weight
339.44 g/mol
Lipinski Ro5
Pass
Rule of 3
No
Chirality
Single Stereoisomer
Inorganic
No
Polymer
No
Delivery
Parenteral, Topical
Availability
Prescription Only

Oral

No

Parenteral

Yes

Topical

Yes

Sources

Also known as

  • 6-desoxy-6-methylenenaltrexone
  • 6-desoxy-6-methylenenaltrexone
  • jf-1
  • jf-1
  • nalmefene
  • nalmefene
  • nalmefene
  • nalmefene
  • nalmefene
  • nalmefene
  • nalmefene
  • nalmefene
  • nalmefene
  • nalmefene hcl
  • nalmefene hcl
  • nalmefene hcl
  • nalmefene hydrochloride
  • nalmefene hydrochloride
  • nalmefene hydrochloride
  • nalmefene hydrochloride
  • nalmefene hydrochloride
  • nalmefene hydrochloride dihydrate
  • nalmefene hydrochloride dihydrate
  • nalmetrene
  • nalmetrene
  • nalmetrene
  • orf-11676
  • orf-11676
  • orf-11676
  • revex
  • revex
  • revex
  • revex
  • selincro
  • selincro
  • selincro
  • selincro

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT06733519Phase 2Mar 1, 2025Tharimmune Inc
NCT06408714Phase 3Aug 26, 2024University of New Mexico
NCT06198686Phase 1Jan 26, 2024Tharimmune Inc
NCT05808881Phase 4Jun 30, 2023Purdue Pharmaceuticals
NCT05724797Phase 1Apr 17, 2023National Institute on Drug Abuse (NIDA), Nirsum Labs
NCT05540288Phase 3Nov 30, 2022University of Nantes
NCT06719986Phase 1Oct 3, 2022Purdue Pharmaceuticals
NCT04713358Phase 4Sep 24, 2021Hacettepe University, Jiao Tong University, Zhengzhou University
NCT05219669Phase 1Sep 1, 2021Opiant, Worldwide Clinical Trials
NCT04828005Phase 1Mar 30, 2021Opiant, Pharmaceutical Research Associates, Inc. (PRA)
NCT04759768Phase 1Feb 8, 2021Opiant, Worldwide Clinical Trials
NCT03278886Phase 1/Phase 2 (Phase 2)Jul 3, 2018Boston University, National Institute on Alcohol Abuse and Alcoholism (NIAAA)
NCT03279562Phase 2Sep 1, 2017Pavlov First Saint Petersburg State Medical University, Yale University
NCT03129347Phase 1Jun 1, 2017National Institute on Drug Abuse (NIDA), Vince & Associates
NCT03096730N/AFeb 6, 2017Nanjing Medical University, Tianjin Medical University
NCT02934919Phase 2Dec 1, 2016University Clermont Auvergne
NCT02824354Phase 3Jul 1, 2016University of Picardie Jules Verne
NCT03034408Phase 2Jul 1, 2016University of Geneva
NCT02679469Phase 1Feb 1, 2016Lundbeck, Otsuka
NCT02639273Phase 1Dec 18, 2015National Institute on Alcohol Abuse and Alcoholism (NIAAA)
Showing 20 of 34 trials
Page 1 / 2

Organizations

Research & Development (29)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
LundbeckFor profit11732008
OpiantFor profit3312021
OtsukaFor profit3322014
National Institute on Alcohol Abuse and Alcoholism (NIAAA)Government2122015
National Institute on Drug Abuse (NIDA)Government2112017
Purdue PharmaceuticalsFor profit2222022
Somaxon PharmaceuticalsFor profit2222005
Tharimmune IncFor profit2222024
Worldwide Clinical TrialsFor profit2012021
Boston UniversityAcademic/Hospital1112018
Hacettepe UniversityAcademic/Hospital1012021
Hospital Universitari General de CatalunyaAcademic/Hospital1012015
Jiao Tong UniversityAcademic/Hospital1112021
Nanjing Medical UniversityAcademic/Hospital1112017
Nirsum LabsFor profit1112023
Pavlov First Saint Petersburg State Medical UniversityAcademic/Hospital1012017
Pharmaceutical Research Associates, Inc. (PRA)For profit1012021
Serentis Ltd.For profit1112009
Tianjin Medical UniversityAcademic/Hospital1012017
University Clermont AuvergneAcademic/Hospital1112016
29 organizations
Page 1 / 2

Marketing (8)

OrganizationOrg typeRelationshipDate
CHENGDU SHUODEFor profitMKTGNov 15, 2023
Eurohlth Intl SarlFor profitNDAApr 17, 1995
Eurohlth Intl SarlFor profitNDA2Apr 17, 1995
HikmaFor profitMKTGApr 17, 1995
HikmaFor profitNDA2Apr 17, 1995
Indivior Inc.For profitMKTGMay 22, 2023
Indivior Inc.For profitNDA2May 22, 2023
Purdue PharmaceuticalsFor profitMKTGFeb 8, 2022