Investigational Drug Details
| Drug ID: | D192 |
| Drug Name: | JKB-121 |
| Synonyms: | Nalmefene |
| Type: | Chemical drug |
| DrugBank ID: | DB06230 |
| DrugBank Description: | Nalmefene is a 6-methylene analogue of naltrexone and opioid system modulator but with no opioid activity . It mediates a partial agonist effect on kappa receptors . It is primarily used in the management of alcohol dependence in adult patients in conjunction with continuous psychosocial support focused on treatment adherence and reducing alcohol consumption when it is exists as the hydrochloride dihydrate form under the trade name Selincro. Selincro is orally administered as tablets. Nalmefene works to reduce alcohol consumption in individuals by positive reward effect of alcohol which involves the opioid system, as well as the sedative and dysphoric properties of alcohol . It is also indicated to prevent or reverse the effects of opioids, including respiratory depression, sedation, and hypotension by acting on the opioid receptor as an antagonist under the trade name Revex for intramuscular, intravenous and subcutaneous injection, where nalmefene hydrochloride is an active ingredient. |
| PubChem ID: | 5284594 |
| CasNo: | 55096-26-9 |
| Repositioning for NAFLD: | No |
| SMILES: | O[C@@]12[C@@]34c5c(O[C@H]3C(=C)CC2)c(O)ccc5C[C@H]1N(CC4)CC1CC1 |
| Structure: |
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| InChiKey: | WJBLNOPPDWQMCH-MBPVOVBZSA-N |
| Molecular Weight: | 339.435 |
| DrugBank Targets: | Mu-type opioid receptor antagonist; Kappa-type opioid receptor partial agonist; Delta-type opioid receptor antagonist |
| DrugBank MoA: | Nalmefene is an opioid system modulator with a distinct μ, δ, and κ receptor profile. It acts as a selective opioid receptor ligand with antagonist activity at the μ and δ receptors and partial agonist activity at the κ receptor . Animal studies suggest that the kappa receptor signalling responses lead to antagonism of acute reward and positive reinforcement effects of drugs by decreasing dopamine in the nucleus accumbens . Thus it is suggested that nalmefene may be more effective treatment for alcohol dependence than , which is a pure mu and delta receptor antagonist . In vivo studies and rat studies have demonstrated that nalmefene reduces self-administration of alcohol, possibly by modulating cortico-mesolimbic functions . Nalmefene, a 6-methylene analogue of naltrexone, is a competitive opioid antagonist which binds with high affinity to the mu opioid receptor. Nalmefene itself does not induce any opioid activity, but prevents or reverses the effects of opioids such as respiratory depression and sedation when injected. Some pharmacodynamic studies showed that nalmefene has a longer duration of action than naloxone at fully reversing doses however the relative potency of these two antagonists are reported to be similar . |
| DrugBank Pharmacology: | Nalmefene has not been shown to produce tolerance, physical dependence, or abuse potential . When adminsitered as an antidote for opioid overdose, nalmefene is not known to produce any respiratory depression, psychomimetic effects, or pupillary constriction . In the absence of opioid agonists, there was no observable pharmacological activity. Nalmefene injection can produce acute withdrawal symptoms in individuals who are opioid-dependent. |
| DrugBank Indication: | Indicated for the reduction of alcohol consumption in adult patients with alcohol dependence who have a high drinking risk level (DRL), without physical withdrawal symptoms and who do not require immediate detoxification . Indicated for the complete or partial reversal of opioid drug effects, including respiratory depression - induced by either natural or synthetic opioids - or in the management of known or suspected opioid overdose . |
| Targets: | TLR4 antagonist |
| Therapeutic Category: | Anti-inflammatory |
| Clinical Trial Progress: | Phase 2 completed (NCT02442687) |
| Latest Progress: | Under clinical trials |
| Trial ID | Source ID | Phases | Status | Study Results | Start Date | Last Update Posted | |
|---|---|---|---|---|---|---|---|
| L0220 | NCT02442687 | Phase 2 | Completed | Has Results | August 1, 2015 | January 7, 2019 | Details |
| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs | |
|---|---|---|---|---|---|
| S05 | Anti-inflammatory | inflammatory | Bile acid; TNF-a inhibitor; Dual PPAR-α and -δ agonists; Toll-Like Receptor; (TLR)-4 antagonist; Caspase inhibitor; ASK-1 inhibitor | Ursodeoxycholic Acid; Pentoxifylline; Elafibranor; JKB-121; Emricasan; Selonsertib; | Details |
| Article ID | PMID | Source | Title |
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