Lemborexant

Lemborexant 구조식 이미지
카스 번호:
1369764-02-2
상품명:
Lemborexant
동의어(영문):
E 2006;CS-2189;Dayvigo.;labradon;Lemborexant;Lemborexant API;lemborexant,E2006;E-2006 Lemborexant;Lemborexant USP/EP/BP;Lemborexant Impurity 1
CBNumber:
CB72744022
분자식:
C22H20F2N4O2
포뮬러 무게:
410.42
MOL 파일:
1369764-02-2.mol

Lemborexant 속성

녹는점
173 - 175°C
끓는 점
596.1±50.0 °C(Predicted)
밀도
1.347±0.06 g/cm3(Predicted)
저장 조건
-20°C, Inert atmosphere
용해도
DMSO(약간 용해됨), 메탄올(약간 용해됨)
산도 계수 (pKa)
12.30±0.40(Predicted)
물리적 상태
고체
물리적 상태
단단한 모양
색상
흰색에서 황백색까지

안전

DEA Controlled Substances CSCN: 2245
CAS SCH: IV
NARC: N

Lemborexant C화학적 특성, 용도, 생산

개요

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).

화학적 성질

Lemborexant is a white to off-white powder that is practically insoluble in water.

용도

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.

Pharmacokinetics

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%)

Drug interactions

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.

참고 문헌

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

Lemborexant 준비 용품 및 원자재

원자재

준비 용품


Lemborexant 공급 업체

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BOC Sciences
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ANHUI WITOP BIOTECH CO., LTD
+8615255079626
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Dideu Industries Group Limited
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1026@dideu.com China 29220 58

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