Lemborexant

Lemborexant
Clinical data
Other names	E-2006
ATC code	None;
Legal status
Legal status	Experimental drug;
Identifiers
	IUPAC name (1R,2S)-2-[(2,4-Dimethylpyrimidin-5-yl)oxymethyl]-2-(3-fluorophenyl)-N-(5-fluoropyridin-2-yl)cyclopropane-1-carboxamide;
CAS Number	1369764-02-2;
PubChem CID	56944144;
ChemSpider	34500836;
KEGG	D11022;
Chemical and physical data
Formula	C22H20F2N4O2
Molar mass	410.417 g/mol g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CC1=NC(=NC=C1OCC2(CC2C(=O)NC3=NC=C(C=C3)F)C4=CC(=CC=C4)F)C;
	InChI InChI=1S/C22H20F2N4O2/c1-13-19(11-25-14(2)27-13)30-12-22(15-4-3-5-16(23)8-15)9-18(22)21(29)28-20-7-6-17(24)10-26-20/h3-8,10-11,18H,9,12H2,1-2H3,(H,26,28,29)/t18-,22+/m0/s1; Key:MUGXRYIUWFITCP-PGRDOPGGSA-N;

Lemborexant (INN) (code name E-2006) is a dual antagonist of the orexin OX₁ and OX₂ receptors which is under development by Eisai for the treatment of insomnia.[1] [2][3] In June 2016, Eisai initiated phase 3 clinical trials which are currently underway in the US, France, Germany, Italy, Japan, Poland, Spain and the UK, and are expected to extend to Canada. [4]

References

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.
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.
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.
"Lemborexant – SPS - Specialist Pharmacy Service – The first stop for professional medicines advice". www.sps.nhs.uk. Retrieved 2017-11-05.

External links

Lemborexant — AdisInsight

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[Christopher2014-1] 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.

[Boss2015-2] 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.

[Boss2014-3] 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.

[4] "Lemborexant – SPS - Specialist Pharmacy Service – The first stop for professional medicines advice". www.sps.nhs.uk. Retrieved 2017-11-05.

Insomnia pharmacotherapies
GABA_AR PAMs	Benzodiazepines: Brotizolam Cinolazepam Climazolam Clorazepate Doxefazepam Estazolam Etizolam Flunitrazepam Flurazepam Flutoprazepam Haloxazolam Loprazolam Lormetazepam Midazolam Nimetazepam Nitrazepam Quazepam Temazepam Triazolam; Nonbenzodiazepines/Z-drugs: Eszopiclone Zaleplon Zolpidem Zopiclone; Others: Alcohols (e.g., ethchlorvynol, amylene hydrate, ethanol) Barbiturates (e.g., amobarbital, pentobarbital, phenobarbital, secobarbital) Bromides (e.g., potassium bromide, sodium bromide) Carbamates (e.g., meprobamate) Chloral hydrate Clomethiazole Kava Paraldehyde Piperidinediones (e.g., glutethimide) Quinazolinones (e.g., methaqualone) Sulfonmethane Valerian
Antihistamines (H₁R inverse agonists)	Alimemazine Captodiame Dimenhydrinate Diphenhydramine Doxylamine Etodroxizine Hydroxyzine Meclizine Methapyrilene Pheniramine Phenyltoloxamine Pimethixene Promethazine Propiomazine Pyrilamine TCAs (e.g., amitriptyline, doxepin, trimipramine) TeCAs (e.g., mirtazapine) Triprolidine
OXR antagonists	Almorexant^§ Filorexant^§ Lemborexant^§ Suvorexant
MTR agonists	Agomelatine Melatonin Ramelteon Tasimelteon
Miscellaneous	Antipsychotics (e.g., quetiapine, olanzapine, chlorpromazine) Ashwagandha Benzoctamine Cannabinoids (e.g., cannabis, dronabinol (THC), nabilone) Chamomile Fenadiazole Gabapentinoids (e.g., gabapentin, pregabalin, phenibut) Hops Lavender Menthyl isovalerate Niaprazine Opioids (e.g., hydrocodone, oxycodone, morphine) Passion flower Scopolamine Serotonin precursors (tryptophan, 5-HTP) Sodium oxybate (GHB) Sympatholytics (e.g., clonidine, guanfacine) TCAs (e.g., amitriptyline, doxepin, trimipramine) TeCAs (e.g., mirtazapine) Theanine Trazodone Valnoctamide

Lemborexant

See also

References

External links