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Ecopipam
Investigational dopamine antagonist From Wikipedia, the free encyclopedia
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Ecopipam (development codes SCH-39166, EBS-101, and PSYRX-101) is a dopamine antagonist which is under development for the treatment of Lesch–Nyhan syndrome, Tourette syndrome, speech disorders, and restless legs syndrome.[2] It is taken by mouth.[3]
Ecopipam acts as a selective dopamine D1 and D5 receptor antagonist.[2] It is orally active, has an elimination half-life of 10 hours, crosses the blood–brain barrier, and substantially occupies brain dopamine receptors.[3][4] Side effects of ecopipam may include depression, anxiety, fatigue, sedation, somnolence, insomnia, headaches, muscle twitching, and suicidal ideation, among others.[5][6][3] It appears to lack the typical extrapyramidal effects like tardive dyskinesia that occur with D2 receptor antagonists.[3]
Ecopipam is an experimental drug and has not been approved for medical use.[2] It was discovered in the CNS preclinical labs at Schering-Plough Corporation (now Merck) under the direction of Richard Chipkin, PhD.[1] As of April 2024, it is in Phase 3 trials for Tourette Syndrome, Phase 2 trials for Tourette syndrome and speech disorders, and phase 2/Phase 1 trials for restless legs syndrome.[2] The drug was also under development for the treatment of cocaine-related disorders, obesity, and schizophrenia, but development for these indications was discontinued.[2]
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Pharmacology
Pharmacodynamics
Ecopipam is a selective dopamine D1 and D5 receptor antagonist.[1] It shows little affinity for either dopamine D2-like or 5-HT2 receptors.[1]
Clinical trials
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Perspective
Based on its profile in animal models, ecopipam was first studied as a treatment for schizophrenia but showed no efficacy.[7][8] Side effects including sedation, restlessness, vomiting, and anxiety were generally rated mild. There were no reports of Parkinsonian-like extrapyramidal symptoms typically seen with D2 antagonists.
Human clinical studies also showed that ecopipam was an effective antagonist of the acute euphoric effects of cocaine.[9] However, the effect did not persist following repeated administration.[10]
Researchers have postulated that dopamine via D1 receptors in the mesolimbic system is involved with rewarded behaviors and pleasure.[11] One such behavior is eating, and ecopipam has been shown in a large clinical study to be an effective treatment for obesity.[12] However, reports of mild-to-moderate, reversible anxiety and depression made it unsuitable for commercialization as an anti-obesity drug, and its development was stopped for that indication.[13]
As of 2021, Emalex Biosciences is investigating its potential use for central nervous system disorders.[14] Open-label studies have found ecopipam to reduce gambling behaviors in subjects with pathological gambling[15] and to decrease the motor and vocal tics in adults with Tourette syndrome.[16] A subsequent double-blind placebo-controlled study in pediatric subjects confirmed ecopipam's ability to ameliorate the motor and vocal symptoms seen in patients with Tourette syndrome.[17] Ecopipam is currently in a Phase 3 clinical trial for the treatment of Tourette syndrome in children ages 7 to 17[18] and for the treatment of restless syndrome augmentation (Phase 1/2)[2]
Ecopipam is an investigational first-in-class drug also being evaluated for the treatment of childhood-onset fluency disorder (stuttering) in adults.[19] There are currently no U.S. Food and Drug Administration (FDA) approved medications for this disorder.[19]
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Chemistry
Chemically, ecopipam is a synthetic benzazepine derivative. It can be synthesized from a simple tetralin derivative:[20]
See also
- Berupipam (NNC 22-0010)
- NNC 01-0687 (ADX-10061)
- Odapipam (NNC 01-0756)
- SCH-23390
References
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