Pharmacokinetics, Pharmacodynamics, and Safety of the Dual Orexin Receptor Antagonist Lemborexant: Findings From Single‐Dose and Multiple‐Ascending‐Dose Phase 1 Studies in Healthy Adults

• Published in: Clinical pharmacology in drug development Vol. 10; no. 2; pp. 153 - 165
• Main Authors: Landry, Ishani, Nakai, Kenya, Ferry, Jim, Aluri, Jagadeesh, Hall, Nancy, Lalovic, Bojan, Moline, Margaret L.
• Format: Journal Article
• Language: English
• Published: United States Wiley Subscription Services, Inc 01.02.2021; John Wiley and Sons Inc
• Subjects: Adult; Age Factors; Aged; Asians; Dose-Response Relationship, Drug; Double-Blind Method; Female; Half-Life; Humans; Insomnia; lemborexant; Male; Middle Aged; orexin receptor antagonists; Orexin Receptor Antagonists - administration & dosage; Orexin Receptor Antagonists - adverse effects; Orexin Receptor Antagonists - pharmacokinetics; Original Manuscript; Pharmacodynamics; Pharmacokinetics; Pyridines - administration & dosage; Pyridines - adverse effects; Pyridines - pharmacokinetics; Pyrimidines - administration & dosage; Pyrimidines - adverse effects; Pyrimidines - pharmacokinetics; safety; Sex Factors; Whites; pharmacokinetics; orexin receptor antagonists; lemborexant; pharmacodynamics; safety; insomnia

Lemborexant, a dual orexin receptor antagonist, is approved for the treatment of insomnia and is under investigation for treating other sleep disorders. Here we summarize pharmacokinetic, pharmacodynamic, and safety data from 3 randomized, double‐blind, placebo‐controlled phase 1 studies: single asc...