nalmefene
Trade name: revex
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
Earliest trial started Aug 1, 2005 (NCT00132119)
Timeline
1990s
- Apr 17, 1995
Eurohlth Intl Sarl — Earliest FDA Approval
- Apr 17, 1995
Eurohlth Intl Sarl — NDA Organization
- Apr 17, 1995
Hikma — Marketing Organization
- Apr 17, 1995
Eurohlth Intl Sarl — NDA Secondary Org
- Apr 17, 1995
Hikma — NDA Secondary Org
2010s
- Jan 1, 2013
Earliest Phase 1 Sponsor(trial)
2020s
- Feb 8, 2022
Purdue Pharmaceuticals — Marketing Organization
- May 22, 2023
Indivior Inc. — Marketing Organization
- May 22, 2023
Indivior Inc. — NDA Secondary Org
- Nov 15, 2023
CHENGDU SHUODE — Marketing Organization
Indications
Approved for
Studied for
- Alcoholic Intoxication · Phase 1
- Alcohol-Induced Disorders · Phase 1/Phase 2
- Behavior, Addictive · Phase 3
- Disruptive, Impulse Control, and Conduct Disorders · Phase 2
- Drugs, Investigational · Phase 3
- Fibrosis · Phase 3
- Gambling · Phase 2/Phase 3
- Healthy Volunteers · Phase 1
- HIV Infections · Phase 1/Phase 2
- Kidney Failure, Chronic · Phase 1
- Liver Cirrhosis, Biliary · Phase 2
- Opiate Overdose · Phase 4
- Opioid-Related Disorders · Phase 2
- Pain · Phase 1/Phase 2
- Parkinson Disease · Phase 2
- Pharmacokinetics · Phase 1
- Pruritus · Phase 2
- Resuscitation · Phase 4
- Smoking Cessation · Phase 2
Mechanism of action
- Opioid receptors; mu/kappa/deltaANTAGONIST
Opioid receptors; mu/kappa/delta antagonist
Approval history
- approvedApr 17, 1995
Chemistry & pharmacology
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
- ChEMBLCHEMBL982 ↗
- WikipediaNalmefene ↗
- NCATSTOV02TDP9I ↗
- ChEMBLCHEMBL1201152 ↗
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 ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT06733519 | Phase 2 | Mar 1, 2025 | Tharimmune Inc |
| NCT06408714 | Phase 3 | Aug 26, 2024 | University of New Mexico |
| NCT06198686 | Phase 1 | Jan 26, 2024 | Tharimmune Inc |
| NCT05808881 | Phase 4 | Jun 30, 2023 | Purdue Pharmaceuticals |
| NCT05724797 | Phase 1 | Apr 17, 2023 | National Institute on Drug Abuse (NIDA), Nirsum Labs |
| NCT05540288 | Phase 3 | Nov 30, 2022 | University of Nantes |
| NCT06719986 | Phase 1 | Oct 3, 2022 | Purdue Pharmaceuticals |
| NCT04713358 | Phase 4 | Sep 24, 2021 | Hacettepe University, Jiao Tong University, Zhengzhou University |
| NCT05219669 | Phase 1 | Sep 1, 2021 | Opiant, Worldwide Clinical Trials |
| NCT04828005 | Phase 1 | Mar 30, 2021 | Opiant, Pharmaceutical Research Associates, Inc. (PRA) |
| NCT04759768 | Phase 1 | Feb 8, 2021 | Opiant, Worldwide Clinical Trials |
| NCT03278886 | Phase 1/Phase 2 (Phase 2) | Jul 3, 2018 | Boston University, National Institute on Alcohol Abuse and Alcoholism (NIAAA) |
| NCT03279562 | Phase 2 | Sep 1, 2017 | Pavlov First Saint Petersburg State Medical University, Yale University |
| NCT03129347 | Phase 1 | Jun 1, 2017 | National Institute on Drug Abuse (NIDA), Vince & Associates |
| NCT03096730 | N/A | Feb 6, 2017 | Nanjing Medical University, Tianjin Medical University |
| NCT02934919 | Phase 2 | Dec 1, 2016 | University Clermont Auvergne |
| NCT02824354 | Phase 3 | Jul 1, 2016 | University of Picardie Jules Verne |
| NCT03034408 | Phase 2 | Jul 1, 2016 | University of Geneva |
| NCT02679469 | Phase 1 | Feb 1, 2016 | Lundbeck, Otsuka |
| NCT02639273 | Phase 1 | Dec 18, 2015 | National Institute on Alcohol Abuse and Alcoholism (NIAAA) |
Organizations
Research & Development (29)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Lundbeck | For profit | 11 | 7 | 3 | 2008 |
| Opiant | For profit | 3 | 3 | 1 | 2021 |
| Otsuka | For profit | 3 | 3 | 2 | 2014 |
| National Institute on Alcohol Abuse and Alcoholism (NIAAA) | Government | 2 | 1 | 2 | 2015 |
| National Institute on Drug Abuse (NIDA) | Government | 2 | 1 | 1 | 2017 |
| Purdue Pharmaceuticals | For profit | 2 | 2 | 2 | 2022 |
| Somaxon Pharmaceuticals | For profit | 2 | 2 | 2 | 2005 |
| Tharimmune Inc | For profit | 2 | 2 | 2 | 2024 |
| Worldwide Clinical Trials | For profit | 2 | 0 | 1 | 2021 |
| Boston University | Academic/Hospital | 1 | 1 | 1 | 2018 |
| Hacettepe University | Academic/Hospital | 1 | 0 | 1 | 2021 |
| Hospital Universitari General de Catalunya | Academic/Hospital | 1 | 0 | 1 | 2015 |
| Jiao Tong University | Academic/Hospital | 1 | 1 | 1 | 2021 |
| Nanjing Medical University | Academic/Hospital | 1 | 1 | 1 | 2017 |
| Nirsum Labs | For profit | 1 | 1 | 1 | 2023 |
| Pavlov First Saint Petersburg State Medical University | Academic/Hospital | 1 | 0 | 1 | 2017 |
| Pharmaceutical Research Associates, Inc. (PRA) | For profit | 1 | 0 | 1 | 2021 |
| Serentis Ltd. | For profit | 1 | 1 | 1 | 2009 |
| Tianjin Medical University | Academic/Hospital | 1 | 0 | 1 | 2017 |
| University Clermont Auvergne | Academic/Hospital | 1 | 1 | 1 | 2016 |
Marketing (8)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| CHENGDU SHUODE | For profit | MKTG | Nov 15, 2023 |
| Eurohlth Intl Sarl | For profit | NDA | Apr 17, 1995 |
| Eurohlth Intl Sarl | For profit | NDA2 | Apr 17, 1995 |
| Hikma | For profit | MKTG | Apr 17, 1995 |
| Hikma | For profit | NDA2 | Apr 17, 1995 |
| Indivior Inc. | For profit | MKTG | May 22, 2023 |
| Indivior Inc. | For profit | NDA2 | May 22, 2023 |
| Purdue Pharmaceuticals | For profit | MKTG | Feb 8, 2022 |