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Lemborexant

Lemborexant Struktur
1369764-02-2
CAS-Nr.
1369764-02-2
Englisch Name:
Lemborexant
Synonyma:
(1R,2S)-2-[[(2,4-Dimethyl-5-pyrimidinyl)oxy]methyl]-2-(3-fluorophenyl)-N-(5-fluoro-2-pyridinyl)cyclopropanecarboxamide;Lemborexan;E 2006;CS-2189;Dayvigo.;labradon;Lemborexant;Lemborexant API;lemborexant,E2006;E-2006 Lemborexant
CBNumber:
CB72744022
Summenformel:
C22H20F2N4O2
Molgewicht:
410.42
MOL-Datei:
1369764-02-2.mol

Lemborexant Eigenschaften

Schmelzpunkt:
173 - 175°C
Siedepunkt:
596.1±50.0 °C(Predicted)
Dichte
1.347±0.06 g/cm3(Predicted)
storage temp. 
-20°C, Inert atmosphere
L?slichkeit
DMSO (Slightly), Methanol (Slightly)
pka
12.30±0.40(Predicted)
Aggregatzustand
Solid
Farbe
White to Off-White
InChIKey
MUGXRYIUWFITCP-PGRDOPGGSA-N
SMILES
[C@@H]1(C(NC2=NC=C(F)C=C2)=O)C[C@@]1(COC1=CN=C(C)N=C1C)C1=CC=CC(F)=C1

Sicherheit

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

Lemborexant Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung

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).

Chemische Eigenschaften

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

Verwenden

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.

Pharmakokinetik

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%)

Synthese

Synthesis route of Lemborexant
Lemborexant

Arzneimittelwechselwirkung

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.

Einzelnachweise

https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212028s000lbl.pdf
https://www.smchealth.org/sites/main/files/file-attachments/dayvigo_for_publish.pdf1592332002
https://www.superiorhealthplan.com/content/dam/centene/Superior/policies/pharmacy-policies/Lemborexant%20(Dayvigo)%20(CP.PMN.233)%20(PDF).pdf

Lemborexant Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte


Lemborexant Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.

Global( 172)Lieferanten
Firmenname Telefon E-Mail Land Produktkatalog Edge Rate
Shaanxi Dideu Medichem Co. Ltd
+86-29-81139210 +86-18192627656
1059@dideu.com China 3703 58
Henan Bao Enluo International TradeCo.,LTD
+86-17331933971
deasea125996@gmail.com China 2472 58
BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD.
+86-18600796368
sales@sjar-tech.com China 529 58
Xi an Biohorlden Industry Trade Co Ltd
+86-18829283179 +86-13636819721
sales@horlden.com China 334 58
ATK CHEMICAL COMPANY LIMITED
+undefined-21-51877795
ivan@atkchemical.com China 33024 60
Shochem(Shanghai) Co.,Ltd
86-21-50800795
info@shochem.com CHINA 288 58
career henan chemical co
+86-0371-86658258 +8613203830695
factory@coreychem.com China 29792 58
HANGZHOU CLAP TECHNOLOGY CO.,LTD
86-571-88216897,88216896 13588875226
sales@hzclap.com CHINA 6312 58
ANHUI WITOP BIOTECH CO., LTD
+8615255079626
eric@witopchemical.com China 23541 58
AFINE CHEMICALS LIMITED
+86-571-85134551
info@afinechem.com China 15083 58

  • E 2006
  • Lemborexant
  • lemborexant,E2006
  • (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
  • E-2006 Lemborexant
  • 2-((1S,2S)-2-(((2,4-dimethylpyrimidin-5-yl)oxy)methyl)-2-(3-fluorophenyl)cyclopropyl)-N-(5-fluoropyridin-2-yl)acetamide
  • CS-2189
  • Dayvigo.
  • E-2006; E 2006; E2006; LEMBOREXANT; DAYVIGO.
  • Cyclopropanecarboxamide, 2-[[(2,4-dimethyl-5-pyrimidinyl)oxy]methyl]-2-(3-fluorophenyl)-N-(5-fluoro-2-pyridinyl)-, (1R,2S)-
  • Lemborexant USP/EP/BP
  • Lemborexant API
  • labradon
  • (1S,2R)-2-(((2,4-dimethylpyrimidin-5-yl)oxy)methyl)-1-(3-fluorophenyl)-N-(5-fluoropyridin-2-yl)cyclopropanecarboxamide
  • Lemborexant Impurity 1
  • (1R,2S)-2-[[(2,4-dimethyl-5-pyrimidine)oxy]methyl]-2-(3-fluorophenyl)-N-(5-fluoro-2-pyridyl)cyclopropaneformamide (Leborethen)
  • (1R,2S)-2-[[(2,4-Dimethyl-5-pyrimidinyl)oxy]methyl]-2-(3-fluorophenyl)-N-(5-fluoro-2-pyridinyl)cyclopropanecarboxamide
  • Lemborexan
  • 1369764-02-2
  • API
  • 1369764-02-2
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