ArticleSleep2019
Preclinical in vivo characterization of lemborexant (E2006), a novel dual orexin receptor antagonist for sleep/wake regulation.
Article in Sleep, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 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.
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Who cites it
21 citing papers in PubMed, 47 citations in OpenAlex.
- Efficacy and safety of lemborexant in midlife women with insomnia disorder.Menopause (New York, N.Y.) · 2023Trial
- 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.Clinical pharmacology in drug development · 2021Trial
- REST-a deep learning tool for automated mouse sleep stage classification.Sleep advances : a journal of the Sleep Research Society · 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
- Lemborexant Reduces Infarct Volume and Improves Long-Term Functional Recovery in a Murine Model of Ischemic Stroke.bioRxiv : the preprint server for biology · 2025Article
- Sleep Architecture Alterations Following High-Dose Steroid Pulse Therapy: A Pilot Study Using a Portable Electroencephalogram-Based Device.Neuropsychopharmacology reports · 2025Article
- Lemborexant ameliorates tau-mediated sleep loss and neurodegeneration in males in a mouse model of tauopathy.Nature neuroscience · 2025Article
- Dual orexin receptor antagonists as promising therapeutics for Alzheimer's disease.Npj biological timing and sleep · 2025Review
- Sleep, inflammation, and hemodynamics in rodent models of traumatic brain injury.Frontiers in neuroscience · 2024Review
- Abuse potential assessment of the dual orexin receptor antagonist daridorexant in rats.Journal of psychopharmacology (Oxford, England) · 2023Article
- FDA-Approved Fluorinated Heterocyclic Drugs from 2016 to 2022.International journal of molecular sciences · 2023Review
- The abuse potential of lemborexant, a dual orexin receptor antagonist, according to the 8 factors of the Controlled Substances Act.Psychopharmacology · 2023Review
- Can Lemborexant for Insomnia Prevent Delirium in High-Risk Patients with Pancreato-Biliary Disease after Endoscopic Procedures under Deep Sedation?Journal of clinical medicine · 2022Article
- Efficacy and safety of lemborexant over 12 months in Asian adults with insomnia disorder.Sleep medicine: X · 2022Article
- Pilot Study of Lemborexant for Insomnia in Cancer Patients with Delirium.Journal of palliative medicine · 2022Observational
- Nonclinical pharmacology of daridorexant: a new dual orexin receptor antagonist for the treatment of insomnia.Psychopharmacology · 2021Review
- Orexin A Enhances Pro-Opiomelanocortin Transcription Regulated by BMP-4 in Mouse Corticotrope AtT20 Cells.International journal of molecular sciences · 2021Article
- Hypocretin/Orexin Receptor Pharmacology and Sleep Phases.Frontiers of neurology and neuroscience · 2021Review
- The effect of lemborexant for insomnia disorder.SAGE open medicine · 2021Article
- Evaluation of SAMP8 Mice as a Model for Sleep-Wake and Rhythm Disturbances Associated with Alzheimer's Disease: Impact of Treatment with the Dual Orexin (Hypocretin) Receptor Antagonist Lemborexant.Journal of Alzheimer's disease : JAD · 2021Article
Corrections and comments
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Authors and funding
5 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
STUDY
objectivesTo present results from in vivo studies underlying the preclinical development of lemborexant (E2006), a novel dual orexin (hypocretin) receptor antagonist for sleep/wake regulation.
methodsRodent (wild-type rats and wild-type and orexin neuron-deficient [orexin/ataxin-3 Tg/+] mice) studies were performed to evaluate the effects of single-dose oral lemborexant (1-300 mg/kg) on orexin-induced increases in plasma adrenocorticotropic hormone (ACTH), locomotor activity, vigilance state measures (wakefulness, nonrapid eye movement [non-REM] sleep, rapid eye movement [REM] sleep), ethanol-induced anesthesia, and motor coordination, and the effects of multiple-dose oral lemborexant (30 mg/kg) on vigilance state measures. Active comparators were almorexant and zolpidem. Pharmacokinetics were assessed after single-dose lemborexant in mice and rats.
resultsLemborexant prevented the orexin-promoted increase in ACTH in rats, therefore demonstrating inhibition of the orexin signaling pathway. Furthermore, lemborexant promoted sleep in wild-type mice and rats. Lemborexant promoted REM and non-REM sleep at an equal rate (there was no change in the REM sleep ratio). In contrast, zolpidem reduced REM sleep. The sleep-promoting effect of lemborexant was mediated via the orexin-peptide signaling pathway as demonstrated by a lack of sleep promotion in orexin neuron-deficient mice. Chronic dosing was not associated with a change in effect size or sleep architecture immediately postdosing. Lemborexant did not increase the sedative effects of ethanol or impair motor coordination, showing good safety margin in animals. Pharmacokinetic/pharmacodynamic data for mice and rats were well aligned.
conclusionsThese findings supported further clinical evaluation (ongoing at this time) of lemborexant as a potential candidate for treating insomnia and other sleep disorders.
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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.