Chemistry:Nivasorexant
Nivasorexant (INN; developmental code name ACT-539313) is an orexin antagonist medication which is under development for the treatment of binge eating disorder and was previously under development for the treatment of anxiety disorders.[1][2][3][4][5][6]
It is an orally active small-molecule compound with an elimination half-life of 3.3 to 6.5 hours and acts as a selective orexin OX1 receptor antagonist (1-SORA).[1][5][6]
As of May 2022, the drug is in phase 2 clinical trials for binge eating disorder.[1] Following negative efficacy results of a phase 2 trial of nivasorexant for binge eating disorder, Idorsia (the developer of nivasorexant) signaled in May 2022 that it would not pursue further development of the drug for this indication.[7]
References
- ↑ 1.0 1.1 1.2 "ACT 539313 - AdisInsight". https://adisinsight.springer.com/drugs/800049623.
- ↑ "Hypocretins (orexins): The ultimate translational neuropeptides". Journal of Internal Medicine 291 (5): 533–556. May 2022. doi:10.1111/joim.13406. PMID 35043499.
- ↑ "Counterbalanced microcircuits for Orx1 and Orx2 regulation of stress reactivity". Medicine in Drug Discovery 8. December 2020. doi:10.1016/j.medidd.2020.100059. ISSN 2590-0986.
- ↑ "Experimental Drugs for Panic Disorder: An Updated Systematic Review". Journal of Experimental Pharmacology 13: 441–459. 2021. doi:10.2147/JEP.S261403. PMID 33889031.
- ↑ 5.0 5.1 "First-in-human study with ACT-539313, a novel selective orexin-1 receptor antagonist". British Journal of Clinical Pharmacology 86 (7): 1377–1386. July 2020. doi:10.1111/bcp.14251. PMID 32067262. "ACT-539313 ((4-methyl-2-[1,2,3]triazol-2-yl-phenyl)-[(R)- 3-(3-[1,2,3]triazol-2-yl-benzyl)-morpholin-4-yl]-methanone) is an orally active, reversible, selective OX1 receptor antagonist (1-SORA) that readily crosses the blood–brain barrier.".
- ↑ 6.0 6.1 "Multiple-dose clinical pharmacology of the selective orexin-1 receptor antagonist ACT-539313". Progress in Neuro-Psychopharmacology & Biological Psychiatry 108. June 2021. doi:10.1016/j.pnpbp.2020.110166. PMID 33159976.
- ↑ "Just months after its first FDA approval, Idorsia dumps binge-eating drug candidate after PhII fail". https://endpts.com/just-months-after-its-first-fda-approval-idorsia-dumps-binge-eating-drug-candidate-after-phii-fail/.
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