Loading AI tools
Investigational dopamine antagonist From Wikipedia, the free encyclopedia
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.[1] It is taken by mouth.[2]
Clinical data | |
---|---|
Other names | EBS-101; PSYRX-101; SCH-39166 |
Routes of administration | By mouth |
ATC code |
|
Legal status | |
Legal status |
|
Pharmacokinetic data | |
Elimination half-life | 10 hours |
Identifiers | |
| |
CAS Number | |
PubChem CID | |
IUPHAR/BPS | |
ChemSpider | |
UNII | |
CompTox Dashboard (EPA) | |
Chemical and physical data | |
Formula | C19H20ClNO |
Molar mass | 313.83 g·mol−1 |
3D model (JSmol) | |
| |
| |
(verify) |
Ecopipam acts as a selective dopamine D1 and D5 receptor antagonist.[1] It is orally active, has an elimination half-life of 10 hours, crosses the blood–brain barrier, and substantially occupies brain dopamine receptors.[2][3] Side effects of ecopipam may include depression, anxiety, fatigue, sedation, somnolence, insomnia, headaches, muscle twitching, and suicidal ideation, among others.[4][5][2] It appears to lack the typical extrapyramidal effects like tardive dyskinesia that occur with D2 receptor antagonists.[2]
Ecopipam is an experimental drug and has not been approved for medical use.[1] As of April 2022, it is in phase 3 trials for Lesch-Nyhan syndrome, phase 2 trials for Tourette syndrome and speech disorders, and phase 2/phase 1 trials for restless legs syndrome.[1] The drug was also under development for the treatment of cocaine-related disorders, obesity, and schizophrenia, but development for these indications was discontinued.[1]
Ecopipam is a selective dopamine D1 and D5 receptor antagonist.[6] It shows little affinity for either dopamine D2-like or 5-HT2 receptors.[6]
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 2/3 clinical trial for the treatment of Tourette syndrome in children ages 7 to 17.[18]
Ecopipam is additionally under development for the treatment of Lesch–Nyhan syndrome (phase 3) and restless legs syndrome (phase 1/2).[1]
Ecopipam is an investigational first-in-class drug being evaluated for the treatment of childhood-onset fluency disorder (stuttering) in adults. It is under development for the treatment of stuttering (phase 2).[19] There are currently no U.S. Food and Drug Administration (FDA) approved medications for the treatment of stuttering.[19]
Chemically, ecopipam is a synthetic benzazepine derivative. It can be synthesized from a simple tetralin derivative:[20]
Seamless Wikipedia browsing. On steroids.
Every time you click a link to Wikipedia, Wiktionary or Wikiquote in your browser's search results, it will show the modern Wikiwand interface.
Wikiwand extension is a five stars, simple, with minimum permission required to keep your browsing private, safe and transparent.