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Lemborexant

Lemborexant
Lemborexant.svg
Clinical data
Trade namesDayvigo
Other namesE-2006
ATC code
  • none
Legal status
Legal status
Pharmacokinetic data
Protein binding94%[1]
MetabolismLiver (major: CYP3A4, minor: CYP3A5)[1]
MetabolitesM10[1]
Elimination half-life17–19 hours[1]
ExcretionFeces: 57.4%[1]
Urine: 29.1%[1]
Identifiers
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
Chemical and physical data
FormulaC22H20F2N4O2
Molar mass410.425 g·mol−1
3D model (JSmol)

Lemborexant, sold under the brand name Dayvigo, is a medication for the treatment of insomnia characterized by difficulties with sleep onset and/or sleep maintenance in adults.[1][2] Lemborexant was approved in the United States for use by adults with insomnia in December 2019.[3][4][2]

Medical uses

Lemborexant is used in the treatment of insomnia.[1]

Pharmacology

Pharmacodynamics

Lemborexant is a dual antagonist of the orexin OX1 and OX2 receptors.[5][6][7]

Pharmacokinetics

The time to peak levels of lemborexant is 1 to 3 hours.[1] A high-fat and high-calorie meal has been found to delay the time to peak levels by 2 hours.[1] Its plasma protein binding in vitro is 94%.[1] Lemborexant is metabolized primarily by CYP3A4 and to a lesser extent by CYP3A5.[1] The elimination half-life of lemborexant is 17 to 19 hours.[1] The medication is excreted in feces (57%) and to a lesser extent urine (29%).[1]

History

In June 2016, Eisai initiated Phase III clinical trials in the United States, France, Germany, Italy, Japan, Poland, Spain and the UK.[8]

In December 2019, lemborexant was approved for use in the United States based on results from the SUNRISE 1 and SUNRISE 2 Phase III clinical trials.[2][9]

Society and culture

Generic names

Lemborexant is the generic name of the drug and its INN.

Brand names

Lemborexant is sold under the brand name Dayvigo.[1]

References

  1. ^ a b c d e f g h i j k l m n o [www.accessdata.fda.gov]
  2. ^ a b c "FDA Approves Dayvigo (lemborexant) for the Treatment of Insomnia in Adult Patients". Drugs.com. 23 December 2019. Retrieved 10 January 2020.
  3. ^ "Novel Drug Approvals for 2019". U.S. Food and Drug Administration (FDA). 2 January 2020. Retrieved 10 January 2020. This article incorporates text from this source, which is in the public domain.
  4. ^ "FDA-Approved Drugs: Lemborexant". U.S. Food and Drug Administration (FDA). Retrieved 10 January 2020.
  5. ^ Christopher, John A (2014). "Small-molecule antagonists of the orexin receptors". Pharmaceutical Patent Analyst. 3 (6): 625–638. doi:10.4155/ppa.14.46. ISSN 2046-8954. PMID 25489915.
  6. ^ Cristoph Boss, Catherine Ross (2015). "Recent Trends in Orexin Research – 2010 to 2015". Bioorganic & Medicinal Chemistry Letters. 25 (15): 2875–2887. doi:10.1016/j.bmcl.2015.05.012. PMID 26045032.
  7. ^ Boss, Christoph (2014). "Orexin receptor antagonists – a patent review (2010 to August 2014)". Expert Opinion on Therapeutic Patents. 24 (12): 1367–1381. doi:10.1517/13543776.2014.978859. ISSN 1354-3776. PMID 25407283.
  8. ^ "Lemborexant". Specialist Pharmacy Service. Retrieved 5 November 2017.[dead link]
  9. ^ "Drug Trials Snapshot: Dayvigo". U.S. Food and Drug Administration (FDA). 20 December 2019. Retrieved 24 January 2020. This article incorporates text from this source, which is in the public domain.

Further reading

External links

  • "Lemborexant". Drug Information Portal. U.S. National Library of Medicine.