Trial reportClinical pharmacology in drug development2021
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.
Trial report in Clinical pharmacology in drug development, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 32 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
32 citing papers in PubMed, 64 citations in OpenAlex.
- Clinical Trial: Lemborexant Efficacy and Safety in Liver Cirrhosis-Randomized, Double-Blind, Crossover Clinical Trial.Alimentary pharmacology & therapeutics · 2026Trial
- Effect of alcohol coadministration on the pharmacodynamics, pharmacokinetics, and safety of lemborexant: A randomized, placebo-controlled crossover study.Journal of psychopharmacology (Oxford, England) · 2022Trial
- Effect of gastric acid-reducing agents on the pharmacokinetics and efficacy of lemborexant.Pharmacology research & perspectives · 2020Trial
- Effects of lemborexant on sleep quality and its association with morning alertness: Post hoc analysis of two phase 3 trials.Sleep medicine: X · 2026Article
- Therapeutic potential of targeting the orexin (hypocretin) system in sleep disorders.Nature reviews. Endocrinology · 2026Review
- Quantitative determination of suvorexant, lemborexant, and daridorexant in human plasma using a MonoTip C18 and gas chromatography-mass spectrometry.Forensic toxicology · 2026Article
- The determination of the novel insomnia medication lemborexant using a validated liquid chromatography-tandem mass spectrometry method, and its quantitation in clinical and forensic samples.Forensic toxicology · 2026Article
- Beyond traditional sleeping pills: safety, efficacy and multidisease potential of three approved orexin receptor antagonists.Frontiers in psychiatry · 2026Review
- Lemborexant overdose presenting with mild sedation despite high plasma levels: A case report.Toxicology reports · 2025Article
- Current and novel dual orexin receptor antagonists for the treatment of insomnia: the emergence of vornorexant.The international journal of neuropsychopharmacology · 2025Review
- Targeting the Orexin System in the Pharmacological Management of Insomnia and Other Diseases: Suvorexant, Lemborexant, Daridorexant, and Novel Experimental Agents.International journal of molecular sciences · 2025Review
- Incorporation of suvorexant and lemborexant into hair and their distributions after a single intake.Forensic toxicology · 2025Article
- Efficacy of Lemborexant in Adults ≥ 65 Years of Age with Insomnia Disorder.Neurology and therapy · 2024Article
- G protein-coupled receptors (GPCRs): advances in structures, mechanisms, and drug discovery.Signal transduction and targeted therapy · 2024Review
- A retrospective clinical practice study comparing the usefulness of dual-orexin receptor antagonists and a melatonin receptor agonist in patients switching from long-term benzodiazepine receptor agonists.Journal of clinical sleep medicine : JCSM : official publication of the American Academy of Sleep Medicine · 2024Article
- Preclinical metabolism and the disposition of vornorexant/TS-142, a novel dual orexin 1/2 receptor antagonist for the treatment of insomnia.Pharmacology research & perspectives · 2024Article
- Emerging and upcoming therapies in insomnia.Translational and clinical pharmacology · 2024Article
- Article
- Projection of Target Drug Particle Size in Oral Formulations Using the Refined Developability Classification System (rDCS).Pharmaceutics · 2023Article
- The abuse potential of lemborexant, a dual orexin receptor antagonist, according to the 8 factors of the Controlled Substances Act.Psychopharmacology · 2023Review
Corrections and comments
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Authors and funding
7 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
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 ascending doses in healthy adults (Study 001; 1-200 mg; N = 64), multiple ascending doses in healthy and elderly adults (Study 002; 2.5-75 mg; N = 55), and multiple doses in healthy white and Japanese adults (Study 003; 2.5-25 mg; N = 32). Lemborexant exposure increased with increasing dose. The time to maximum concentration ranged from approximately 1 to 3 hours for the 5- and 10-mg doses. The mean effective half-life was 17 hours for lemborexant 5 mg and 19 hours for lemborexant 10 mg. The plasma concentration at 9 hours postdose was 27% of the maximum concentration following multiple dosing with lemborexant 10 mg. There were no clinically relevant effects on next-morning residual sleepiness (Karolinska Sleepiness Scale, Digital Symbol Substitution Test, Psychomotor Vigilance Test) for doses through 10 mg/day, indicating no effect of residual plasma concentrations on next-day residual effects. Lemborexant was well tolerated across the doses tested. There were no clinically relevant effects of age, sex, or race on lemborexant pharmacokinetics, pharmacodynamics, or safety. These results suggest that lemborexant at doses through 25 mg provides an overall pharmacokinetic, pharmacodynamic, and safety profile suitable for obtaining the target pharmacologic effect supporting treatment of insomnia while minimizing residual effects during wake time.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.