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Revision as of 02:55, 11 May 2022

ACT-539313
Clinical data
Routes of
administration
Oral
Drug classOrexin receptor antagonist
Pharmacokinetic data
Elimination half-life3.3–6.5 hours[1][2]
Identifiers
  • 4-methyl-2-[1,2,3]triazol-2-yl-phenyl)-[(R)-3-(3-[1,2,3]triazol-2-yl-benzyl)morpholin-4-yl]methanone

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.[3][4][5][6][1][2] 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).[3][1][2] As of May 2022, the drug is in phase 2 clinical trials for binge eating disorder.[3] ACT-539313 was originated by Idorsia Pharmaceuticals and is under development by Actelion Pharmaceuticals.[3]

References

  1. ^ a b c Kaufmann P, Ort M, Golor G, Kornberger R, Dingemanse J (July 2020). "First-in-human study with ACT-539313, a novel selective orexin-1 receptor antagonist". Br J Clin Pharmacol. 86 (7): 1377–1386. doi:10.1111/bcp.14251. PMC 7319015. PMID 32067262.
  2. ^ a b c Kaufmann P, Ort M, Golor G, Kornberger R, Dingemanse J (June 2021). "Multiple-dose clinical pharmacology of the selective orexin-1 receptor antagonist ACT-539313". Prog Neuropsychopharmacol Biol Psychiatry. 108: 110166. doi:10.1016/j.pnpbp.2020.110166. PMID 33159976.
  3. ^ a b c d https://adisinsight.springer.com/drugs/800049623
  4. ^ Jacobson LH, Hoyer D, de Lecea L (May 2022). "Hypocretins (orexins): The ultimate translational neuropeptides". J Intern Med. 291 (5): 533–556. doi:10.1111/joim.13406. PMID 35043499.
  5. ^ Yaeger, Jazmine D.W.; Krupp, Kevin T.; Gale, Jason J.; Summers, Cliff H. (December 2020). "Counterbalanced microcircuits for Orx1 and Orx2 regulation of stress reactivity". Medicine in Drug Discovery. 8: 100059. doi:10.1016/j.medidd.2020.100059. ISSN 2590-0986.
  6. ^ Caldirola D, Alciati A, Cuniberti F, Perna G (2021). "Experimental Drugs for Panic Disorder: An Updated Systematic Review". J Exp Pharmacol. 13: 441–459. doi:10.2147/JEP.S261403. PMC 8055642. PMID 33889031.{{cite journal}}: CS1 maint: unflagged free DOI (link)