Lemborexant
Lemborexant, sold under the brand name Dayvigo, is a medication for the treatment of insomnia characterized by difficulties with sleep onset and/or sleep maintenance in adults.[1][2] Lemborexant was approved in the United States for use by adults with insomnia in December 2019.[3][4][2]
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Trade names | Dayvigo |
Other names | E-2006 |
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Protein binding | 94%[1] |
Metabolism | Liver (major: CYP3A4, minor: CYP3A5)[1] |
Metabolites | M10[1] |
Elimination half-life | 17–19 hours[1] |
Excretion | Feces: 57.4%[1] Urine: 29.1%[1] |
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Formula | C22H20F2N4O2 |
Molar mass | 410.425 g·mol−1 |
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Pharmacology
Pharmacokinetics
The time to peak levels of lemborexant is 1 to 3 hours.[1] A high-fat and high-calorie meal has been found to delay the time to peak levels by 2 hours.[1] Its plasma protein binding in vitro is 94%.[1] Lemborexant is metabolized primarily by CYP3A4 and to a lesser extent by CYP3A5.[1] The elimination half-life of lemborexant is 17 to 19 hours.[1] The medication is excreted in feces (57%) and to a lesser extent urine (29%).[1]
History
In June 2016, Eisai initiated Phase III clinical trials in the United States, France, Germany, Italy, Japan, Poland, Spain and the UK.[8]
In December 2019, lemborexant was approved for use in the United States based on results from the SUNRISE 1 and SUNRISE 2 Phase III clinical trials.[2][9]
Society and culture
Generic names
Lemborexant is the generic name of the drug and its INN.
Brand names
Lemborexant is sold under the brand name Dayvigo.[1]
References
- https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212028s000lbl.pdf
- "FDA Approves Dayvigo (lemborexant) for the Treatment of Insomnia in Adult Patients". Drugs.com. 23 December 2019. Retrieved 10 January 2020.
- "Novel Drug Approvals for 2019". U.S. Food and Drug Administration (FDA). 2 January 2020. Retrieved 10 January 2020. This article incorporates text from this source, which is in the public domain.
- "FDA-Approved Drugs: Lemborexant". U.S. Food and Drug Administration (FDA). Retrieved 10 January 2020.
- Christopher, John A (2014). "Small-molecule antagonists of the orexin receptors". Pharmaceutical Patent Analyst. 3 (6): 625–638. doi:10.4155/ppa.14.46. ISSN 2046-8954. PMID 25489915.
- Cristoph Boss, Catherine Ross (2015). "Recent Trends in Orexin Research – 2010 to 2015". Bioorganic & Medicinal Chemistry Letters. 25 (15): 2875–2887. doi:10.1016/j.bmcl.2015.05.012. PMID 26045032.
- Boss, Christoph (2014). "Orexin receptor antagonists – a patent review (2010 to August 2014)". Expert Opinion on Therapeutic Patents. 24 (12): 1367–1381. doi:10.1517/13543776.2014.978859. ISSN 1354-3776. PMID 25407283. S2CID 21106711.
- "Lemborexant". Specialist Pharmacy Service. Archived from the original on 7 November 2017. Retrieved 5 November 2017.
- "Drug Trials Snapshot: Dayvigo". U.S. Food and Drug Administration (FDA). 20 December 2019. Retrieved 24 January 2020. This article incorporates text from this source, which is in the public domain.
Further reading
- Abad VC, Guilleminault C (September 2018). "Insomnia in Elderly Patients: Recommendations for Pharmacological Management". Drugs Aging. 35 (9): 791–817. doi:10.1007/s40266-018-0569-8. PMID 30058034. S2CID 51866276.
- Murphy P, Moline M, Mayleben D, Rosenberg R, Zammit G, Pinner K, Dhadda S, Hong Q, Giorgi L, Satlin A (November 2017). "Lemborexant, A Dual Orexin Receptor Antagonist (DORA) for the Treatment of Insomnia Disorder: Results From a Bayesian, Adaptive, Randomized, Double-Blind, Placebo-Controlled Study". J Clin Sleep Med. 13 (11): 1289–1299. doi:10.5664/jcsm.6800. PMC 5656478. PMID 29065953.
- Murphy PJ, Yasuda S, Nakai K, Yoshinaga T, Hall N, Zhou M, Aluri J, Rege B, Moline M, Ferry J, Darpo B (January 2017). "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". J Clin Pharmacol. 57 (1): 96–104. doi:10.1002/jcph.785. PMID 27338807. S2CID 3711638.