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Nonbenzodiazepine Sedative Hypnotics and Risk of Fall-Related Injury

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The Neurobiology of Sleep

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Suvorexant for Primary Insomnia: A Systematic Review and Meta-Analysis of Randomized Placebo-Controlled Trials

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On-the-Road Driving Performance the Morning after Bedtime Use of Suvorexant 20 and 40 mg: A Study in Non-Elderly Healthy Volunteers

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Suvorexant in Elderly Patients with Insomnia: Pooled Analyses of Data from Phase III Randomized Controlled Clinical Trials

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Orexin and Alzheimer’s Disease

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Suvorexant

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Suvorexant: First Global Approval

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Increased plasma orexin-A levels in patients with insomnia disorder are not associated with prepro-orexin or orexin receptor gene polymorphisms

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Pilot prospective study of post-surgery sleep and EEG predictors of post-operative delirium

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Suvorexant for the treatment of insomnia

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Intact learning and memory in rats following treatment with the dual orexin receptor antagonist almorexant

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On-the-road driving performance the morning after bedtime use of suvorexant 15 and 30 mg in healthy elderly

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Orexin/Hypocretin and Organizing Principles for a Diversity of Wake-Promoting Neurons in the Brain

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Inhibition of Orexin Signaling Promotes Sleep Yet Preserves Salient Arousability in Monkeys

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Novel class of medications, orexin receptor antagonists, in the treatment of insomnia – critical appraisal of suvorexant

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Differential Effects of the Dual Orexin Receptor Antagonist Almorexant and the GABAA-α1 Receptor Modulator Zolpidem, Alone or Combined with Ethanol, on Motor Performance in the Rat

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CSF-hypocretin-1 levels in patients with major depressive disorder compared to healthy controls

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Electroencephalographic Power Spectral Density Profile of the Orexin Receptor Antagonist Suvorexant in Patients with Primary Insomnia and Healthy Subjects

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Profile of suvorexant in the management of insomnia

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Efficacy and safety of almorexant in adult chronic insomnia: a randomized placebo-controlled trial with an active reference

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A Phase II Dose-Ranging Study Evaluating the Efficacy and Safety of the Orexin Receptor Antagonist Filorexant (MK-6096) in Patients with Primary Insomnia

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Dual orexin receptor antagonists show distinct effects on locomotor performance, ethanol interaction and sleep architecture relative to gamma-aminobutyric acid-A receptor modulators

Ramirez, A. D., Gotter, A. L., Fox, S. V., Tannenbaum, P. L., Yao, L., Tye, S. J., McDonald, T. P., Brunner, J., Garson, S. L., Reiss, D. R., et al. (2013) · Frontiers in Neuroscience · doi:10.3389/fnins.2013.00254 · Cited by 40 · see citing works

Orexin OX2 Receptor Antagonists as Sleep Aids

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In vitro and in vivo characterisation of the metabolism and disposition of suvorexant in humans

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The hypocretin/orexin antagonist almorexant promotes sleep without impairment of performance in rats

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Orexin receptor antagonist-induced sleep does not impair the ability to wake in response to emotionally salient acoustic stimuli in dogs

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Design and Synthesis of Potent and Highly Selective Orexin 1 Receptor Antagonists with a Morphinan Skeleton and Their Pharmacologies

Nagase, H., Yamamoto, N., Yata, M., Ohrui, S., Okada, T., Saitoh, T., Kutsumura, N., Nagumo, Y., Irukayama‐Tomobe, Y., Ishikawa, Y., et al. (2017) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.6b01418 · Cited by 35 · see citing works

Concentration–Response Modeling of ECG Data From Early‐Phase Clinical Studies as an Alternative Clinical and Regulatory Approach to Assessing QT Risk — Experience From the Development Program of Lemborexant

Murphy, P., Yasuda, S., Nakai, K., Yoshinaga, T., Hall, N., Zhou, M., Aluri, J., Rege, B., Moline, M. L., Ferry, J., et al. (2016) · The Journal of Clinical Pharmacology · doi:10.1002/jcph.785 · Cited by 33 · see citing works

Insight Into Reduction of Wakefulness by Suvorexant in Patients With Insomnia: Analysis of Wake Bouts

Svetnik, V., Snyder, E., Tao, P., Scammell, T. E., Roth, T. G., Lines, C., & Herring, W. J. (2017) · SLEEP · doi:10.1093/sleep/zsx178 · Cited by 33 · see citing works

Suvorexant in Elderly Patients with Insomnia: Pooled Analyses of Data from Phase III Randomized Controlled Clinical Trials

Christensen, M., & Riordan, P. A. (2022) · Springer eBooks · doi:10.1007/978-3-030-94960-0_67 · Cited by 32 · see citing works

Suvorexant: a promising, novel treatment for insomnia

Parish, J. M., & Lee‐Iannotti, J. K. (2016) · Neuropsychiatric Disease and Treatment · doi:10.2147/ndt.s31495 · Cited by 30 · see citing works

Dual Orexin Receptor Antagonist, Almorexant, in Elderly Patients With Primary Insomnia: A Randomized, Controlled Study

Roth, T. G., Black, J. E., Cluydts, R., Charef, P., Cavallaro, M., Kramer, F., Zammit, G. K., & Walsh, J. K. (2016) · SLEEP · doi:10.1093/sleep/zsw034 · Cited by 30 · see citing works

Entry‐into‐humans study with ACT‐462206, a novel dual orexin receptor antagonist, comparing its pharmacodynamics with almorexant

Hoch, M., van Gorsel, H. C., van Gerven, J., & Dingemanse, J. (2014) · The Journal of Clinical Pharmacology · doi:10.1002/jcph.297 · Cited by 27 · see citing works

Why Does Sleep Stop Migraine?

BIGAL, M. E., & Hargreaves, R. J. (2013) · Current Pain and Headache Reports · doi:10.1007/s11916-013-0369-0 · Cited by 27 · see citing works

Pharmacodynamic effects of suvorexant and zolpidem on EEG during sleep in healthy subjects

Struyk, A. F., Gargano, C., Drexel, M., Stoch, S. A., Svetnik, V., Ma, J., & Mayleben, D. W. (2016) · European Neuropsychopharmacology · doi:10.1016/j.euroneuro.2016.07.002 · Cited by 26 · see citing works

Minimum duration of actigraphy-defined nocturnal awakenings necessary for morning recall

Winser, M. A., McBean, A. L., & Montgomery‐Downs, H. E. (2013) · Sleep Medicine · doi:10.1016/j.sleep.2013.03.018 · Cited by 25 · see citing works

Discovery of piperidine ethers as selective orexin receptor antagonists (SORAs) inspired by filorexant

Raheem, I. T., Breslin, M. J., Bruno, J. G., Cabalu, T. D., Cooke, A., Cox, C. D., Cui, D., Garson, S. L., Gotter, A. L., Fox, S. V., et al. (2014) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2014.12.056 · Cited by 23 · see citing works

Discovery of highly potent and selective orexin 1 receptor antagonists (1-SORAs) suitable for in vivo interrogation of orexin 1 receptor pharmacology

Stump, C. A., Cooke, A., Bruno, J. G., Cabalu, T. D., Gotter, A. L., Harrell, C. M., Kuduk, S. D., McDonald, T. P., O'Brien, J. L., Renger, J. J., et al. (2016) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2016.10.019 · Cited by 20 · see citing works

Suvorexant: Efficacy and safety profile of a dual orexin receptor antagonist in treating insomnia

Owen, R. T. (2016) · Drugs of today · doi:10.1358/dot.2016.52.1.2439940 · Cited by 16 · see citing works

Orexin Receptor Antagonism in Painful Diabetic Neuropathy

Herring, W. J., Ge, J. Y., Jackson, S., Assaid, C. A., Connor, K. M., & Michelson, D. (2017) · Clinical Journal of Pain · doi:10.1097/ajp.0000000000000503 · Cited by 9 · see citing works

The dual orexin receptor antagonist, DORA‐22, lowers histamine levels in the lateral hypothalamus and prefrontal cortex without lowering hippocampal acetylcholine

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Clinical trials of new drugs for Alzheimer disease

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Insomnia disorder: State of the science and challenges for the future

Riemann, D. W., Benz, F., Dressle, R. J., Espie, C. A., Johann, A. F., Blanken, T. F., Leerssen, J., Wassing, R., Henry, A. L., Kyle, S. D., et al. (2022) · Journal of Sleep Research · doi:10.1111/jsr.13604 · Cited by 368 · see citing works

The Extraordinary Importance of Sleep: The Detrimental Effects of Inadequate Sleep on Health and Public Safety Drive an Explosion of Sleep Research.

Worley, S. L. (2018) · Europe PMC (PubMed Central) · Cited by 182 · see citing works

An update on the novel and approved drugs for Alzheimer disease

Alhazmi, H. A., & Albratty, M. (2022) · Saudi Pharmaceutical Journal · doi:10.1016/j.jsps.2022.10.004 · Cited by 122 · see citing works

Neuronal Networks in Hypertension

Guyenet, P. G., Stornetta, R. L., Souza, G. M. P. R., Abbott, S. B. G., & Brooks, V. L. (2020) · Hypertension · doi:10.1161/hypertensionaha.120.14521 · Cited by 110 · see citing works

Hypocretins (orexins): The ultimate translational neuropeptides

Jacobson, L. H., Hoyer, D., & de Lecea, L. (2022) · Journal of Internal Medicine · doi:10.1111/joim.13406 · Cited by 107 · see citing works

Effects of orexin receptor antagonism on human sleep architecture: A systematic review

Clark, J. W., Brian, M. L., Drummond, S. P. A., Hoyer, D., & Jacobson, L. H. (2020) · Sleep Medicine Reviews · doi:10.1016/j.smrv.2020.101332 · Cited by 86 · see citing works

Sleep Physiology, Circadian Rhythms, Waking Performance and the Development of Sleep-Wake Therapeutics

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Hypocretin/Orexin Receptor Pharmacology and Sleep Phases

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Involvement of orexinergic system in psychiatric and neurodegenerative disorders: A scoping review

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Pharmacogenomics of Cognitive Dysfunction and Neuropsychiatric Disorders in Dementia

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Targeting the orexin/hypocretin system for the treatment of neuropsychiatric and neurodegenerative diseases: From animal to clinical studies

Ten-Blanco, M., Flores, Á., Cristino, L., Pereda-Pérez, I., & Berrendero, F. (2023) · Frontiers in Neuroendocrinology · doi:10.1016/j.yfrne.2023.101066 · Cited by 47 · see citing works

Sleep therapeutics and neuropsychiatric illness

Krystal, A. D. (2019) · Neuropsychopharmacology · doi:10.1038/s41386-019-0474-9 · Cited by 43 · see citing works

Insomnia as a predictor of diagnosed memory problems: 2006–2016 Health and Retirement Study

Beydoun, H. A., Beydoun, M. A., Weiss, J., Hossain, S. A., Huang, S., Alemu, B. T., & Zonderman, A. B. (2021) · Sleep Medicine · doi:10.1016/j.sleep.2021.01.038 · Cited by 43 · see citing works

At the intersection of sleep deficiency and opioid use: mechanisms and therapeutic opportunities

Greenwald, M. K., Moses, T. E. H., & Roehrs, T. (2021) · Translational research · doi:10.1016/j.trsl.2021.03.006 · Cited by 29 · see citing works

Translational approaches to influence sleep and arousal

Brown, R. E., Spratt, T. J., & Kaplan, G. B. (2022) · Brain Research Bulletin · doi:10.1016/j.brainresbull.2022.05.002 · Cited by 29 · see citing works

Sleep–Wake Disorders in Alzheimer’s Disease: A Review

Sun, Y.-Y., Wang, Z., Zhou, H.-Y., & Huang, H. (2022) · ACS Chemical Neuroscience · doi:10.1021/acschemneuro.2c00097 · Cited by 27 · see citing works

Orexin receptor antagonists in the pathophysiology and treatment of sleep disorders and epilepsy

Sheibani, M., Shayan, M., Khalilzadeh, M., Ghasemi, M., & Dehpour, A. R. (2023) · Neuropeptides · doi:10.1016/j.npep.2023.102335 · Cited by 26 · see citing works

The Discovery of Suvorexant: Lessons Learned That Can Be Applied to Other CNS Drug Development Efforts

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Daridorexant for the Treatment of Insomnia

Robinson, C. L., Supra, R., Downs, E., Kataria, S., Parker, K., Kaye, A. D., Viswanath, O., & Urits, I. (2022) · Health Psychology Research · doi:10.52965/001c.37400 · Cited by 22 · see citing works

Impact of Daridorexant, a Dual Orexin Receptor Antagonist, on Cardiac Repolarization Following Bedtime Dosing: Results from a Thorough QT Study Using Concentration-QT Analysis

Schilling, U., Henrich, A., Muehlan, C., Krause, A., Dingemanse, J., & Ufer, M. (2021) · Clinical Drug Investigation · doi:10.1007/s40261-021-01062-1 · Cited by 20 · see citing works

Synthesis and clinical application of new drugs approved by FDA in 2022

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Oxadiazole Derivatives as Dual Orexin Receptor Antagonists: Synthesis, Structure–Activity Relationships, and Sleep‐Promoting Properties in Rats

Brotschi, C., Roch, C., Gatfield, J., Treiber, A., Williams, J. T., Sifferlen, T., Heidmann, B., Jenck, F., Bolli, M. H., & Boss, C. (2019) · ChemMedChem · doi:10.1002/cmdc.201900242 · Cited by 17 · see citing works

Dysregulation of striatal dopamine D2/D3 receptor-mediated by hypocretin induces depressive behaviors in rats

Chen, B., Xu, J., Chen, S., Mou, T., Wang, Y., Wang, H., Zhang, Z., Ren, F., Wang, Z., Jin, K., et al. (2023) · Journal of Affective Disorders · doi:10.1016/j.jad.2023.01.031 · Cited by 15 · see citing works

In vivo Evidence for Brain Region-Specific Molecular Interactions Between Cannabinoid and Orexin Receptors

Kim, H. J. J., Zagzoog, A., Smolyakova, A.-M., Ezeaka, U. C., Benko, M. J., Holt, T., & Laprairie, R. B. (2021) · Frontiers in Neuroscience · doi:10.3389/fnins.2021.790546 · Cited by 12 · see citing works

CYP450-Mediated metabolism of suvorexant and investigation of metabolites in forensic case specimens

Skillman, B. N., & Kerrigan, S. (2020) · Forensic Science International · doi:10.1016/j.forsciint.2020.110307 · Cited by 11 · see citing works

The putative effects of orexin receptor antagonists on pain and sleep in humans: A systematic review

Babiloni, A. H., Sangalli, L., Puertas, F. J., Morin, C. M., Lavigne, G. J., & Fabbro, C. D. (2025) · Sleep Medicine · doi:10.1016/j.sleep.2025.106633 · Cited by 9 · see citing works

KLF4 Exerts Sedative Effects in Pentobarbital-Treated Mice

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Dual orexin receptor antagonist ameliorates sleep deprivation-induced learning and memory impairment in APP/PS1 mice

Li, Y., Yan, Z., Shao, N., Tang, S. H., Zhang, X., Liu, X. M., & Tang, J. (2024) · Sleep Medicine · doi:10.1016/j.sleep.2024.07.023 · Cited by 7 · see citing works

Suvorexant in the Treatment of Difficulty Falling and Staying Asleep (Insomnia)

Berger, A. A., Sottosanti, E., Winnick, A. A., Keefe, J., Gilbert, E., Hasoon, J. J., Thase, M. E., Kaye, A. D., Viswanath, O., & Urits, I. (2025) · Psychopharmacology Bulletin · doi:10.64719/pb.4429 · Cited by 8 · see citing works

Sleep Pharmacogenetics: The Promise of Precision Medicine.

Krystal, A., & Prather, A. (2019) · Sleep Medicine Clinics · doi:10.1016/j.jsmc.2019.05.003 · Cited by 6 · see citing works

Cannabinoid and Orexigenic Systems Interplay as a New Focus of Research in Alzheimer’s Disease

Rebassa, J. B., Capó, T., Lillo, J., Raïch, I., Reyes‐Resina, I., & Navarro, G. (2024) · International Journal of Molecular Sciences · doi:10.3390/ijms25105378 · Cited by 5 · see citing works

Insomnia medications: History, characteristics, and guidelines for optimal use in clinical practice

Krystal, A. D. (2023) · Journal of Sleep Research · doi:10.1111/jsr.14084 · Cited by 4 · see citing works

Integrating serum pharmacochemistry with network pharmacology and pharmacological validation to elucidate the mechanism of KaiXinSan in treating insomnia

Zhang, S., Guo, D., Zhao, C., Shi, Y., Zou, J., Shi, H., Cheng, J., Sun, J., & Zhang, X. (2025) · BMC Complementary Medicine and Therapies · doi:10.1186/s12906-025-05196-z · Cited by 2 · see citing works

Effect of ramelteon coadministered with antidepressant in patients with insomnia and major depressive disorder: an exploratory study

Uchimura, N., Nakatome, K., Miyata, K., & Uchiyama, M. (2019) · Sleep and Biological Rhythms · doi:10.1007/s41105-019-00230-3 · Cited by 2 · see citing works

Synthesis and biological activity evaluation of azacycloheptane sulfonamide derivatives as potential orexin receptor antagonists

Guo, B., Xiu, J., Shen, Y., & Li, Q. (2020) · RSC Advances · doi:10.1039/d0ra05068g · Cited by 1 · see citing works

Old and new methods in sleep research/sleep medicine and insomnia

Riemann, D. W. (2019) · Journal of Sleep Research · doi:10.1111/jsr.12840 · Cited by 1 · see citing works

Orexin and Psychoneurobiology: A Hidden Treasure

Al-Kuraishy, H. M., Al-Gareeb, A. I., & Al-Harchan, N. A. (2020) · IntechOpen eBooks · doi:10.5772/intechopen.91852

Assessing and treating insomnia with specific comorbidities

Atkinson, R., Singh, M., & Drake, C. L. (2021) · Elsevier eBooks · doi:10.1016/b978-0-12-822963-7.00053-0

Somnologics

Herberger, S., Rüther, E., & Hajak, G. (2021) · Springer eBooks · doi:10.1007/978-3-319-56015-1_421-1

Orexin

Nakamachi, T. (2021) · Elsevier eBooks · doi:10.1016/b978-0-12-820649-2.00036-x

Las orexinas como biomarcadores para demencia tipo Alzheimer y relación con síntomas neuropsiquiátricos

Lozano-Tovar, S., Monroy‐Jaramillo, N., & Rodríguez‐Agudelo, Y. (2022) · Revista chilena de neuro-psiquiatría · doi:10.4067/s0717-92272022000300313

Somnologics

Herberger, S., Rüther, E., & Hajak, G. (2022) · Springer eBooks · doi:10.1007/978-3-030-62059-2_421

Modified Investigation Tools and Techniques Useful in Alzheimer’s Disease Research

Deore, S. L., Baviskar, B. A., Kide, A. A., Khadabadi, S. S., & Shende, B. A. (2023) · Springer eBooks · doi:10.1007/978-981-99-2657-2_3

Daridorexant: A drug to treat insomnia

Tyagi, H., Sharma, A. K., Khera, N., Sharma, B., Bajaj, M., & Kaur, M. (2023) · Pharmaspire · doi:10.56933/pharmaspire.2023.15114

Orexin Receptor System: Molecular Insights and Therapeutic Implications

Sharma, P., Choudhary, G., Sachdeva, M., Mehta, G., & Tripathi, R. (2024) · Current Drug Therapy · doi:10.2174/0115748855312643241004111641

Biochemical Substrates, Mechanisms, and Pathways Involved in Normal Sleep and Sleep Disorders: A Review

Shrivastava, D., & Pandey, R. (2026) · Sleep and Vigilance · doi:10.1007/s41782-025-00331-9

Unveiling the binding mechanism of orexin 2 receptor antagonists with computational chemistry

Sena, C. P. D. S., de Albuquerque, P. C., Fulco, U. L., de Oliveira, J. I. N., & Vieira, D. S. (2026) · Physical Chemistry Chemical Physics · doi:10.1039/d5cp03790e

Shenling Jiangzhi formula alleviates atherosclerosis in ApoE−/− mice by inhibiting vascular inflammation via the NF-κB/NLRP3 pathway

Kong, Q., Niu, Y., Yao, J., Hou, X., 王岳林, Wang, Y., Jia, R., & Zhou, H. (2026) · Journal of Ethnopharmacology · doi:10.1016/j.jep.2026.121878

Association between hypnotic medication use and in-hospital falls among older adults: A multicenter landmark analysis

Nishino, T., Kubota, Y., Miyagi, Y., Tanabe, N., YAMAGUCHI, F., Ito, H., Soh, S., Yano, A., Mizuno, M., Kim, C., et al. (2026) · PLoS ONE · doi:10.1371/journal.pone.0351299

FDA-approved imidazole- and benzimidazole-based drugs: An update

Du, J., Wei, Q., Chen, X., Chen, X., Zhang, T., Zhang, D., Li, X., Yang, Y., & Wang, Y. (2026) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2026.119281

Interprofessional and interdisciplinary management of nonwithdrawal delirium in a geriatric trauma center—A practical guide

Stenmanns, C., Frohnhofen, H., Möllmann, H. L., Vogt, R., Lakomek, F., Latz, D., Neuerburg, C., & Beyersdorf, C. (2026) · Zeitschrift für Gerontologie und Geriatrie · doi:10.1007/s00391-026-02652-4

Effects of lemborexant vs placebo on total daytime sleep in shift workers: a randomized controlled trial

Prather, A. A., Mitgang, D., Coggins, T., Ovais, T., & Krystal, A. D. (2026) · Journal of Clinical Sleep Medicine · doi:10.1007/s44470-026-00199-0 · Cited by 1 · see citing works

Suvorexant: The first orexin receptor antagonist to treat insomnia

Dubey, A. K., Handu, S. S., & Mediratta, P. K. (2015) · Journal of Pharmacology and Pharmacotherapeutics · doi:10.4103/0976-500x.155496 · Cited by 71 · see citing works

Orexin receptor antagonism for treatment of insomnia

Herring, W. J., Snyder, E., Budd, K., Hutzelmann, J., Snavely, D. B., Liu, K., Lines, C., Roth, T. G., & Michelson, D. (2012) · Neurology · doi:10.1212/wnl.0b013e31827688ee · Cited by 321 · see citing works

Orexin receptor antagonists: a new treatment for insomnia?

Riemann, D. W., & Spiegelhalder, K. (2014) · The Lancet Neurology · doi:10.1016/s1474-4422(13)70311-9 · Cited by 25 · see citing works

Suvorexant: Efficacy and safety profile of a dual orexin receptor antagonist in treating insomnia

Owen, R. T. (2016) · Drugs of today · doi:10.1358/dot.2016.52.1.2439940 · Cited by 16 · see citing works

Novel class of medications, orexin receptor antagonists, in the treatment of insomnia – critical appraisal of suvorexant

Anderson, S. L., & Norman, J. (2016) · Nature and Science of Sleep · doi:10.2147/nss.s76910 · Cited by 49 · see citing works