Lemborexant, sold under the brand nameDayvigo, is anorexin antagonist medication which is used in the treatment ofinsomnia.[3][8] It is indicated specifically for the treatment of insomnia characterized by difficulties withsleep onset and/ormaintenance in adults.[3][8] The medication is takenby mouth.[3][8]
Lemborexant is used in the treatment ofinsomnia in adults.[3]
A majorsystematic review andnetwork meta-analysis of medications for the treatment of insomnia published in 2022 found that lemborexant had aneffect size (standardized mean difference (SMD)) againstplacebo for treatment of insomnia at 4weeks of 0.36 (95%CITooltip confidence interval 0.08 to 0.63) and at 3months of 0.41 (95%CI 0.04 to 0.78).[14] Lemborexant had similar effect sizes at 4weeks as the other evaluated and marketed orexin receptor antagonistssuvorexant (SMD 0.31, 95% CI 0.01 to 0.62) anddaridorexant (SMD 0.23, 95% CI –0.01 to 0.48), whereasbenzodiazepines andZ-drugs generally showed larger effect sizes (e.g., SMDs of 0.45 to 0.83) than lemborexant and the other orexin receptor antagonists.[14] However, the review concluded that lemborexant andeszopiclone among all of the insomnia medications assessed had the best profiles overall in terms ofefficacy,tolerability, andacceptability.[14]
Peak-normalized concentrations (% ofCmax) of the orexin receptor antagonists suvorexant (SUV; 20mg) and lemborexant (LEM; 10mg) with administration atsteady state in humans.[21]
Although lemborexant has a longerterminal elimination half-life than suvorexant, it appears to be more rapidlycleared than suvorexant in the earlier phases ofelimination.[21][7] In addition, lemborexant dissociates from the orexin receptors more rapidly than does suvorexant.[21] These differences may allow for comparatively reduced next-day effects such as daytime somnolence with lemborexant.[21][7]
In June 2016,Eisai initiated Phase IIIclinical trials in the United States, France, Germany, Italy, Japan, Poland, Spain and the UK.[22]
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.[11][23]
Lemborexant is thegeneric name of the drug and itsINNTooltip International Nonproprietary Name whileE-2006 was its developmental code name. Lemborexant is sold under the brand name Dayvigo.[3]
^abcdMuehlan C, Vaillant C, Zenklusen I, Kraehenbuehl S, Dingemanse J (November 2020). "Clinical pharmacology, efficacy, and safety of orexin receptor antagonists for the treatment of insomnia disorders".Expert Opinion on Drug Metabolism & Toxicology.16 (11):1063–1078.doi:10.1080/17425255.2020.1817380.PMID32901578.S2CID221572078.
^abcdefghijWaters K (February 2022). "Review of the Efficacy and Safety of Lemborexant, a Dual Receptor Orexin Antagonist (DORA), in the Treatment of Adults With Insomnia Disorder".The Annals of Pharmacotherapy.56 (2):213–221.doi:10.1177/10600280211008492.PMID34078141.S2CID235321467.
^abJacobson LH, Hoyer D, de Lecea L (May 2022). "Hypocretins (orexins): The ultimate translational neuropeptides".Journal of Internal Medicine.291 (5):533–556.doi:10.1111/joim.13406.PMID35043499.S2CID248119793.
^Christopher JA (2014). "Small-molecule antagonists of the orexin receptors".Pharmaceutical Patent Analyst.3 (6):625–638.doi:10.4155/ppa.14.46.PMID25489915.
^Boss C, Roch C (August 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.PMID26045032.
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