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| Other names | EBS-101; PSYRX-101; SCH-39166 |
| Routes of administration | By mouth |
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| Elimination half-life | 10 hours |
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| Formula | C19H20ClNO |
| Molar mass | 313.83 g·mol−1 |
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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.[1] It is taken by mouth.[2]
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]
- ^ a b c d e Cite error: The named reference
AdisInsightwas invoked but never defined (see the help page). - ^ a b c d Khasnavis T, Torres RJ, Sommerfeld B, Puig JG, Chipkin R, Jinnah HA (July 2016). "A double-blind, placebo-controlled, crossover trial of the selective dopamine D1 receptor antagonist ecopipam in patients with Lesch-Nyhan disease". Molecular Genetics and Metabolism. 118 (3): 160–166. doi:10.1016/j.ymgme.2016.04.012. PMID 27179999.
- ^ Karlsson P, Sedvall G, Halldin C, Swahn CG, Farde L (October 1995). "Evaluation of SCH 39166 as PET ligand for central D1 dopamine receptor binding and occupancy in man". Psychopharmacology. 121 (3): 300–308. doi:10.1007/BF02246067. PMID 8584610. S2CID 12659381.
- ^ Nathan PJ, O'Neill BV, Napolitano A, Bullmore ET (October 2011). "Neuropsychiatric adverse effects of centrally acting antiobesity drugs". CNS Neuroscience & Therapeutics. 17 (5): 490–505. doi:10.1111/j.1755-5949.2010.00172.x. PMC 6493804. PMID 21951371.
Recently a study reported findings from human phase 2 and phase 3 clinical trials examining the potential of the D1/D5 receptor antagonist, ecopipam, to enhance and maintain weight loss in obese patients [61]. While these studies showed promising weight loss in both phase 2 and phase 3, there were unexpected treatment related neuropsychiatric adverse events (ecopipam 31% vs. placebo 15%) in the phase 3 clinical trials (that were not observed in the phase 2 studies) and as a consequence phase 3 studies were discontinued. The neuropsychiatric adverse events included depression (ecopipam 16% vs. placebo 6%), anxiety (ecopipam 15% vs. placebo 6%), suicidal ideation (ecopipam 2% vs. placebo 1%), insomnia (ecopipam 17% vs. placebo 7%), fatigue (ecopipam 15% vs. placebo 6%), and somnolence (ecopipam 15% vs. placebo 4%). Psychiatric adverse events also accounted for more than half of the discontinuations because of treatment related adverse effects in the ecopipam group.
- ^ Gilbert DL, Budman CL, Singer HS, Kurlan R, Chipkin RE (2014). "A D1 receptor antagonist, ecopipam, for treatment of tics in Tourette syndrome". Clinical Neuropharmacology. 37 (1): 26–30. doi:10.1097/WNF.0000000000000017. PMID 24434529. S2CID 24829565.