Lemborexant (E2006) is an oral active diorexin receptor antagonist (DORA) and has been approved by the US Food and Drug Administration for the treatment of insomnia[1-2].
Lemborexant(1-25mg;15days) had a positive effect on Sleep Efficiency (SE) by improving both sleep onset (decreasing LPS) and sleep maintenance (decreasing WASO) in a dose-related manner[2]. In 62 subjects, according to circadian rhythm, day and night parameters (placebo, n = 12; lemborexant 2.5 mg [LEM2.5], n = 12; lemborexant 5 mg [LEM5], n = 13, lemborexant 10 mg [LEM10], n = 13 and lemborexant 15 mg [LEM15], n = 12). Mean least active 5 hours (L5) showed a decrease from baseline to week 4 for LEM2.5, LEM5 and LEM15 that was significantly greater than with placebo, suggesting a reduction in restlessness[3].
References:
[1]. Dayvigo [prescribing information] (lemborexant), Woodcliff Lake, NJ: Eisai Inc. US. https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212028s000lbl.pdf. Accessed January 08, 2020.
[2]. Murphy P, Moline M, et,al. 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. 2017 Nov 15;13(11):1289-1299. doi: 10.5664/jcsm.6800. PMID: 29065953; PMCID: PMC5656478.
[3]. Moline M, Thein S, et,al. Safety and Efficacy of Lemborexant in Patients With Irregular Sleep-Wake Rhythm Disorder and Alzheimer's Disease Dementia: Results From a Phase 2 Randomized Clinical Trial. J Prev Alzheimers Dis. 2021;8(1):7-18. doi: 10.14283/jpad.2020.69. PMID: 33336219.
Lemborexant (E2006) 是一种口服活性双食欲素受体拮抗剂 (DORA)，已获得美国食品和药物管理局批准用于治疗失眠[1-2]。
Lemborexant(1- 25 毫克；15 天）通过以剂量相关的方式改善入睡（降低 LPS）和睡眠维持（降低 WASO），对睡眠效率 (SE) 产生积极影响 [2]。在 62 名受试者中，根据昼夜节律、昼夜参数（安慰剂，n = 12；lemborexant 2.5 mg [LEM2.5]，n = 12；lemborexant 5 mg [LEM5]，n = 13，lemborexant 10 mg [LEM10] , n = 13 和 lemborexant 15 mg [LEM15], n = 12)。 LEM2.5、LEM5 和 LEM15 的平均最少活动 5 小时 (L5) 显示从基线到第 4 周的减少明显大于安慰剂，表明躁动减少[3]。