Suvorexant

Suvorexant
Clinical data
ATC code	None;
Legal status
Legal status	In general: ℞ (Prescription only);
Identifiers
	IUPAC name [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone;
CAS Number	1030377-33-3 ;
PubChem CID	24965990;
ChemSpider	24662178 ;
CompTox Dashboard (EPA)	DTXSID90145616 ;
ECHA InfoCard	100.210.546
Chemical and physical data
Formula	C23H23ClN6O2
Molar mass	450.920 g/mol (free base) g·mol−1
3D model (JSmol)	Interactive image;
	SMILES C[C@@H]1CCN(CCN1C(=O)C2=C(C=CC(=C2)C)N3N=CC=N3)C4=NC5=C(O4)C=CC(=C5)Cl;
	InChI InChI=1S/C23H23ClN6O2/c1-15-3-5-20(30-25-8-9-26-30)18(13-15)22(31)29-12-11-28(10-7-16(29)2)23-27-19-14-17(24)4-6-21(19)32-23/h3-6,8-9,13-14,16H,7,10-12H2,1-2H3/t16-/m1/s1 ; Key:JYTNQNCOQXFQPK-MRXNPFEDSA-N ;
	(what is this?) (verify)

Suvorexant (Belsomra) is a non-selective orexin receptor antagonist marketed by Merck & Co. for the treatment of insomnia.^[1]^[2]^[3] The drug (originally known as MK-4305) completed three phase III trials^[4] and was approved for sale by the U.S. Food & Drug Administration on August 13, 2014.^[5] In the United States, the DEA has approved suvorexant on August 27, 2014. ^[6] Suvorexant has been placed on the list of schedule IV controlled substances.^[7] Merck has said that it expects the drug to be available in late 2014 or early 2015.

Medical uses

Suvorexant is used for the treatment of insomnia, characterized by difficulties with [sleep onse]t and/or sleep maintenance.^[8]

Mechanism of action

Suvorexant exerts its therapeutic effect in insomnia through antagonism of orexin receptors. The orexin neuropeptide signaling system is a central promoter of wakefulness. Blocking the binding of wake-promoting neuropeptides orexin A and orexin B to receptors Orexin receptor type 1 and Orexin receptor type 2 is thought to suppress wake drive.^[9]

References

^ Attention: This template ({{cite doi}}) is deprecated. To cite the publication identified by doi:10.1021/jm100541c, please use {{cite journal}} (if it was published in a bona fide academic journal, otherwise {{cite report}} with |doi=10.1021/jm100541c instead.
^ Attention: This template ({{cite doi}}) is deprecated. To cite the publication identified by doi:10.1021/op1002853, please use {{cite journal}} (if it was published in a bona fide academic journal, otherwise {{cite report}} with |doi=10.1021/op1002853 instead.
^ Attention: This template ({{cite doi}}) is deprecated. To cite the publication identified by doi:10.3109/01677063.2011.566953, please use {{cite journal}} (if it was published in a bona fide academic journal, otherwise {{cite report}} with |doi=10.3109/01677063.2011.566953 instead.
^
Three completed trials:
- Clinical trial number NCT01097629 for "Safety and Efficacy Study in Primary Insomnia Patients-Study B (4305-029)" at ClinicalTrials.gov
- Clinical trial number NCT01021813 for "A Long Term Safety Study of MK4305 in Patients With Primary Insomnia (4305-009 AM3)" at ClinicalTrials.gov
- Clinical trial number NCT01097616 for "Safety and Efficacy Study in Primary Insomnia Patients- Study A (4305-028)" at ClinicalTrials.gov
^ http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm409950.htm
^ {{cite web}}: Empty citation (help)
^ https://www.federalregister.gov/articles/2014/02/13/2014-03124/schedules-of-controlled-substances-placement-of-suvorexant-into-schedule-iv
^ http://www.merck.com/product/usa/pi_circulars/b/belsomra/belsomra_pi.pdf. {{cite web}}: Missing or empty |title= (help)
^ http://www.merck.com/product/usa/pi_circulars/b/belsomra/belsomra_pi.pdf. {{cite web}}: Missing or empty |title= (help)

Template:Neuropeptide agonists and antagonists

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[1] Attention: This template ({{cite doi}}) is deprecated. To cite the publication identified by doi:10.1021/jm100541c, please use {{cite journal}} (if it was published in a bona fide academic journal, otherwise {{cite report}} with |doi=10.1021/jm100541c instead.

[2] Attention: This template ({{cite doi}}) is deprecated. To cite the publication identified by doi:10.1021/op1002853, please use {{cite journal}} (if it was published in a bona fide academic journal, otherwise {{cite report}} with |doi=10.1021/op1002853 instead.

[3] Attention: This template ({{cite doi}}) is deprecated. To cite the publication identified by doi:10.3109/01677063.2011.566953, please use {{cite journal}} (if it was published in a bona fide academic journal, otherwise {{cite report}} with |doi=10.3109/01677063.2011.566953 instead.

[4] Three completed trials:
Clinical trial number NCT01097629 for "Safety and Efficacy Study in Primary Insomnia Patients-Study B (4305-029)" at ClinicalTrials.gov

Clinical trial number NCT01021813 for "A Long Term Safety Study of MK4305 in Patients With Primary Insomnia (4305-009 AM3)" at ClinicalTrials.gov

Clinical trial number NCT01097616 for "Safety and Efficacy Study in Primary Insomnia Patients- Study A (4305-028)" at ClinicalTrials.gov

[5] Clinical trial number NCT01097629 for "Safety and Efficacy Study in Primary Insomnia Patients-Study B (4305-029)" at ClinicalTrials.gov

[6] Clinical trial number NCT01021813 for "A Long Term Safety Study of MK4305 in Patients With Primary Insomnia (4305-009 AM3)" at ClinicalTrials.gov

[7] Clinical trial number NCT01097616 for "Safety and Efficacy Study in Primary Insomnia Patients- Study A (4305-028)" at ClinicalTrials.gov

[5] ttps://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm409950.htm

[6] {{cite web}}: Empty citation (help)

[7] ttps://www.federalregister.gov/articles/2014/02/13/2014-03124/schedules-of-controlled-substances-placement-of-suvorexant-into-schedule-iv

[8] ttps://www.merck.com/product/usa/pi_circulars/b/belsomra/belsomra_pi.pdf. {{cite web}}: Missing or empty |title= (help)

[9] ttps://www.merck.com/product/usa/pi_circulars/b/belsomra/belsomra_pi.pdf. {{cite web}}: Missing or empty |title= (help)

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