| Identification | Back Directory | [Name]
Lemborexant | [CAS]
1369764-02-2 | [Synonyms]
E 2006
CS-2189
Dayvigo.
Lemborexant
lemborexant,E2006
E-2006 Lemborexant
Lemborexant USP/EP/BP
lemborexant / E-2006, CID 56944144
E-2006; E 2006; E2006; LEMBOREXANT; DAYVIGO.
(1R,2S)-2-[[(2,4-Dimethyl-5-pyrimidinyl)oxy]methyl]-2-(3-fluorophenyl)-N-(5-fluoro-2-pyridinyl)cyclopropanecarboxamide
(1R,2S)-2-[(2,4-DIMETHYLPYRIMIDIN-5-YL)OXYMETHYL]-2-(3-FLUOROPHENYL)-N-(5-FLUOROPYRIDIN-2-YL)CYCLOPROPANE-1-CARBOXAMIDE
2-((1S,2S)-2-(((2,4-dimethylpyrimidin-5-yl)oxy)methyl)-2-(3-fluorophenyl)cyclopropyl)-N-(5-fluoropyridin-2-yl)acetamide
Cyclopropanecarboxamide, 2-[[(2,4-dimethyl-5-pyrimidinyl)oxy]methyl]-2-(3-fluorophenyl)-N-(5-fluoro-2-pyridinyl)-, (1R,2S)- | [Molecular Formula]
C22H20F2N4O2 | [MDL Number]
MFCD28502271 | [MOL File]
1369764-02-2.mol | [Molecular Weight]
410.42 |
| Chemical Properties | Back Directory | [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) | [form ]
Solid | [pka]
12.30±0.40(Predicted) | [color ]
White to Off-White |
| Hazard Information | Back Directory | [Description]
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). | [Chemical Properties]
Lemborexant is a white to off-white powder that is practically insoluble in water. | [Uses]
Lemborexant is a novel orexin receptor antagonist and is used in the treatment of insomnia. | [Pharmacokinetics]
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Effect of food
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High-fat & high-calorie meal delay Tmax & reduce Cmax
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Tmax
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1 to 3 hours
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Half-life
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17 hours (5 mg) and 19 hours (10 mg)
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Metabolism
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primarily metabolized by CYP3A4
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Excretion
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Urine (29%); feces (57%)
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| [Synthesis]
Synthesis route of Lemborexant
 | [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. | [References]
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 |
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