Lemborexant

Lemborexant Basic information
Product Name:Lemborexant
Synonyms:(1R,2S)-2-[[(2,4-Dimethyl-5-pyrimidinyl)oxy]methyl]-2-(3-fluorophenyl)-N-(5-fluoro-2-pyridinyl)cyclopropanecarboxamide;E 2006;(1R,2S)-2-[(2,4-DIMETHYLPYRIMIDIN-5-YL)OXYMETHYL]-2-(3-FLUOROPHENYL)-N-(5-FLUOROPYRIDIN-2-YL)CYCLOPROPANE-1-CARBOXAMIDE;lemborexant / E-2006, CID 56944144;Lemborexant;lemborexant,E2006;E-2006 Lemborexant;2-((1S,2S)-2-(((2,4-dimethylpyrimidin-5-yl)oxy)methyl)-2-(3-fluorophenyl)cyclopropyl)-N-(5-fluoropyridin-2-yl)acetamide
CAS:1369764-02-2
MF:C22H20F2N4O2
MW:410.42
EINECS:
Product Categories:API;1369764-02-2
Mol File:1369764-02-2.mol
Lemborexant Structure
Lemborexant Chemical Properties
Melting point 173 - 175°C
Boiling point 596.1±50.0 °C(Predicted)
density 1.347±0.06 g/cm3(Predicted)
storage temp. -20°C, Inert atmosphere
solubility DMSO (Slightly), Methanol (Slightly)
pka12.30±0.40(Predicted)
form Solid
color White to Off-White
Safety Information
DEA Controlled SubstancesCSCN: 2245
CAS SCH: IV
NARC: N

MSDS Information
Lemborexant Usage And Synthesis
DescriptionLemborexant 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).
Chemical PropertiesLemborexant is a white to off-white powder that is practically insoluble in water.
UsesLemborexant 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 interactionsLemborexant 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 actionThe 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.
Referenceshttps://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 Preparation Products And Raw materials
Raw materials1369769-35-6-->2-Amino-5-fluoropyridine
15-BROMOPENTADECANOIC ACID 15-BROMO-1-PENTADECANOL

Email:[email protected] [email protected]
Copyright © 2024 Mywellwork.com All rights reserved.