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The abuse potential of lemborexant, a dual orexin receptor antagonist, according to the 8 factors of the Controlled Substances Act.
Moline, Margaret; Asakura, Shoji; Beuckman, Carsten; Landry, Ishani; Setnik, Beatrice; Ashworth, Judy; Henningfield, Jack E.
Affiliation
  • Moline M; Eisai Inc., 200 Metro Boulevard, Nutley, Jersey, NJ, 07110, USA. Margaret_Moline@eisai.com.
  • Asakura S; Eisai Co., Ltd., Tsukuba, Japan.
  • Beuckman C; Formerly Eisai Co., Ltd., Tsukuba, Japan.
  • Landry I; Formerly Eisai, Nutley, Jersey, NJ, USA.
  • Setnik B; Altasciences, Laval, Quebec, Canada and the Department of Pharmacology and Toxicology, University of Toronto, Toronto, Ontario, Canada.
  • Ashworth J; Pinney Associates, Inc., Bethesda, MD, USA.
  • Henningfield JE; Pinney Associates, Inc., Bethesda, MD, USA.
Psychopharmacology (Berl) ; 240(4): 699-711, 2023 Apr.
Article in En | MEDLINE | ID: mdl-36749354
RATIONALE: Lemborexant (LEM) is a dual orexin receptor antagonist (DORA) approved in multiple countries including the USA, Japan, Canada, Australia, and several Asian countries for the treatment of insomnia in adults. As a compound with central nervous system activity, it is important to understand the abuse potential of LEM with respect to public health. OBJECTIVES: This review discusses data for LEM relevant to each of the 8 factors of the United States Controlled Substances Act. RESULTS: LEM did not demonstrate abuse potential in nonclinical testing and was associated with a low incidence of abuse-related adverse events in clinical study participants with insomnia disorder. Similar to other DORAs that have been evaluated (eg., almorexant, suvorexant (SUV), and daridorexant), LEM and the positive controls (zolpidem and SUV) also showed drug liking in a phase 1 abuse potential study that enrolled subjects who used sedatives recreationally. However, internet surveillance of SUV and the FDA Adverse Events Reporting System suggests that drugs in the DORA class display very low abuse-related risks in the community. Additionally, as described in FDA-approved labeling, it does not carry physical dependence and withdrawal risks. CONCLUSIONS: LEM, similar to most other prescription insomnia medications, was placed into Schedule IV. However, LEM and other drugs in the DORA class may have a lower potential for abuse as suggested by real-world postmarketing data from federal surveys and internet surveillance, and thus may have lower risks to public health than Schedule IV benzodiazepines and nonbenzodiazepine hypnotics that potentiate GABA signaling.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Orexin Receptor Antagonists / Sleep Initiation and Maintenance Disorders Limits: Adult / Humans Language: En Journal: Psychopharmacology (Berl) Year: 2023 Document type: Article Affiliation country: United States Country of publication: Germany

Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Orexin Receptor Antagonists / Sleep Initiation and Maintenance Disorders Limits: Adult / Humans Language: En Journal: Psychopharmacology (Berl) Year: 2023 Document type: Article Affiliation country: United States Country of publication: Germany