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Nivasorexant

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Nivasorexant (INNTooltip International Nonproprietary Name; developmental code name ACT-539313) is an orexin receptor antagonist which is under development for the treatment of binge eating disorder and was previously under development for the treatment of anxiety disorders.[4][5][6][7][1][2]

Other namesACT-539313; ACT539313
Routes of
administrationOral
Drug classOrexin receptor antagonist
Elimination half-life3.3–6.5 hours[1][2]
Quick facts Clinical data, Other names ...
Nivasorexant
Clinical data
Other namesACT-539313; ACT539313
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[3][1]
CAS Number
PubChem CID
UNII
Chemical and physical data
FormulaC23H23N7O2
Molar mass429.484 g·mol−1
3D model (JSmol)
  • CC1=CC(=C(C=C1)C(=O)N2CCOC[C@H]2CC3=CC(=CC=C3)N4N=CC=N4)N5N=CC=N5
  • InChI=1S/C23H23N7O2/c1-17-5-6-21(22(13-17)30-26-9-10-27-30)23(31)28-11-12-32-16-20(28)15-18-3-2-4-19(14-18)29-24-7-8-25-29/h2-10,13-14,20H,11-12,15-16H2,1H3/t20-/m1/s1
  • Key:GKPHAIOJCHBZCT-HXUWFJFHSA-N
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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 or SO1RA).[4][1][2][8] It was the first SO1RA drug to enter clinical development.[8]

As of May 2022, the drug was in phase 2 clinical trials for binge eating disorder.[4] The phase 2 trial found that Nivasorexant did not improve binge-eating compared to the placebo,[9] after which Idorsia (the developer of nivasorexant) signaled in May 2022 that it would not pursue further development of the drug.[10]

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