レンボレキサント

化学名:レンボレキサント

英語名:Lemborexant

CBNumberCB72744022

MFC22H20F2N4O2

MW410.42

别名

レンボレキサント

レンボレキサント (JAN)

(1R,2S)-2-{[(2,4-ジメチルピリミジン-5-イル)オキシ]メチル}-2-(3-フルオロフェニル)-N-(5-フルオロピリジン-2-イル)シクロプロパン-1-カルボキサミド

レンボレキサント物理性質

安全性情報

DEA Controlled Substances

CSCN: 2245
CAS SCH: IV
NARC: N

レンボレキサント化学特性,用途語,生産方法

効能
催眠薬, オレキシン受容体拮抗薬
説明
Lemborexant is a newer orexin receptor antagonist which is submitted to US FDA for review as new drug application for the treatment of insomnia after completing two key Phase 3 studies of lemborexant – SUNRISE 1 (Study 304) and SUNRISE 2 (Study 303).
化学的特性
Lemborexant is a white to off-white powder that is practically insoluble in water.
使用
Lemborexant is a novel orexin receptor antagonist and is used in the treatment of insomnia, characterised by difficulties with sleep onset or sleep maintenance. Orexins are neuropeptides involved in regulating sleep and arousal by promoting wakefulness. Lemborexant blocks the binding of orexins A and B to their receptors 1 and 2 thereby reducing wakefulness and promoting sleep. Suvorexant is the other orexin receptor antagonist marketed in Australia for insomnia.

薬物動態学

Effect of food	High-fat & high-calorie meal delay Tmax & reduce Cmax
Tmax	1 to 3 hours
Half-life	17 hours (5 mg) and 19 hours (10 mg)
Metabolism	primarily metabolized by CYP3A4
Excretion	Urine (29%); feces (57%)

薬物相互作用
Lemborexant is metabolized by CYP3A4 and is susceptible to interactions with medications such as amiodarone, amlodipine, carbamazepine, clarithromycin, diltiazem, fluoxetine and phenytoin. Lemborexant may affect other medications metabolised by CYP2B6, such as bupropion and methadone. Alcohol should be avoided: a single dose of alcohol can increase lemborexant concentrations up to 70%.
Mode of action
The mechanism of action of lemborexant in the treatment of insomnia is Blocks the binding of wake-promoting neuropeptides orexin A and orexin B to receptors OX1R and OX2R, presumed to suppress wake drive.
参考文献
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212028s000lbl.pdf
https://www.smchealth.org/sites/main/files/file-attachments/dayvigo_for_publish.pdf?1592332002
https://www.superiorhealthplan.com/content/dam/centene/Superior/policies/pharmacy-policies/Lemborexant%20(Dayvigo)%20(CP.PMN.233)%20(PDF).pdf