SUVOREXANT HYDROCHLORIDE

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C23H23ClN6O2.ClH
Molecular Weight	487.382
Optical Activity	( - )
Defined Stereocenters	1 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

Cl.C[C@@H]1CCN(CCN1C(=O)C2=C(C=CC(C)=C2)N3N=CC=N3)C4=NC5=C(O4)C=CC(Cl)=C5

InChI

InChIKey=BIIYCWIUJHUUAO-PKLMIRHRSA-N

InChI=1S/C23H23ClN6O2.ClH/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;1H/t16-;/m1./s1

HIDE SMILES / InChI

Molecular Formula	C23H23ClN6O2
Molecular Weight	450.921
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	1 / 1
E/Z Centers	0
Optical Activity	UNSPECIFIED

Molecular Formula	ClH
Molecular Weight	36.461
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: http://www.ncbi.nlm.nih.gov/pubmed/?term=PMC4419247
Curator's Comment: description was created based on several sources, including http://www.accessdata.fda.gov/drugsatfda_docs/label/2014/204569s001lbl.pdf; http://www.ncbi.nlm.nih.gov/pubmed/?term=24102345

Suvorexant is a selective dual antagonist of orexin receptors OX1R and OX2R. It has been approved for the treatment of insomnia. The mechanism by which suvorexant exerts its therapeutic effect in insomnia is presumed to be 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 OX1R and OX2R is thought to suppress wake drive.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Orexin receptor type 2 2 Target ID: O43614 Gene ID: 3062.0 Gene Symbol: HCRTR2 Target Organism: Homo sapiens (Human) Sources: http://www.ncbi.nlm.nih.gov/pubmed/?term=21473737	Antagonist 2778		0.55 nM [Ki]
Orexin receptor type 1 2 Target ID: O43613 Gene ID: 3061.0 Gene Symbol: HCRTR1 Target Organism: Homo sapiens (Human) Sources: http://www.ncbi.nlm.nih.gov/pubmed/?term=21473737	Antagonist 2778		0.35 nM [Ki]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Sleep-onset insomnia 2 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2014/204569s001lbl.pdf	Palliative		Approved 8429	BELSOMRA Approved Use Indicated for the treatment of insomnia characterized by difficulties with sleep onset and/or sleep maintenance. Launch Date 1.407888E12

C_max

Value	Dose	Analyte	Population
1.08 μM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29705869	40 mg 1 times / day steady-state, oral dose: 40 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	SUVOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1.329 μM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29705869	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	SUVOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1.425 μM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29705869	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	SUVOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1.488 μM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29705869	80 mg 1 times / day steady-state, oral dose: 80 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	SUVOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
2.085 μM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29705869	100 mg 1 times / day steady-state, oral dose: 100 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	SUVOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
0.356 μM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29705869	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	SUVOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
0.414 μM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29705869	10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	SUVOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
0.572 μM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29705869	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	SUVOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
0.574 μM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29705869	20 mg 1 times / day steady-state, oral dose: 20 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	SUVOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
0.802 μM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29705869	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	SUVOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
0.854 uM Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01043926	20 mg single, oral dose: 20 mg route of administration: oral experiment type: single co-administered:	SUVOREXANT plasma	Homo sapiens population: healthy age: sex: food status: Fasted

AUC

Value	Dose	Analyte	Population
10.64 μM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29705869	40 mg 1 times / day steady-state, oral dose: 40 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	SUVOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
11.48 μM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29705869	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	SUVOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
18.1 μM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29705869	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	SUVOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
18.32 μM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29705869	80 mg 1 times / day steady-state, oral dose: 80 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	SUVOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
27.62 μM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29705869	100 mg 1 times / day steady-state, oral dose: 100 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	SUVOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
3.43 μM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29705869	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	SUVOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
4.36 μM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29705869	10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	SUVOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
5.03 μM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29705869	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	SUVOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
6.08 μM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29705869	20 mg 1 times / day steady-state, oral dose: 20 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	SUVOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
8.53 μM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29705869	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	SUVOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED

T_1/2

Value	Dose	Analyte	Population
9.4 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29705869	40 mg 1 times / day steady-state, oral dose: 40 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	SUVOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
10 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29705869	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	SUVOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
12.6 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29705869	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	SUVOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
11.2 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29705869	80 mg 1 times / day steady-state, oral dose: 80 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	SUVOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
14.5 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29705869	100 mg 1 times / day steady-state, oral dose: 100 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	SUVOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
7.7 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29705869	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	SUVOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
8.1 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29705869	10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	SUVOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
8.4 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29705869	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	SUVOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
9.2 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29705869	20 mg 1 times / day steady-state, oral dose: 20 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	SUVOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
8.6 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29705869	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	SUVOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
12 h DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/204569Orig1s007lbl.pdf		SUVOREXANT plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
1% DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/204569Orig1s007lbl.pdf			SUVOREXANT plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN

Doses

Dose	Population	Adverse events
100 mg 1 times / day steady, oral Highest studied dose Dose: 100 mg, 1 times / day Route: oral Route: steady Dose: 100 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/29705869	healthy, 34.3 years(range: 19–45 years) n = 6 Health Status: healthy Age Group: 34.3 years(range: 19–45 years) Sex: M+F Population Size: 6 Sources: https://pubmed.ncbi.nlm.nih.gov/29705869	Other AEs: Somnolence, Fatigue... Other AEs: Somnolence (67%) Fatigue (83%) Insomnia (17%) Dizziness (33%) Phlebitis (33%) Sources: https://pubmed.ncbi.nlm.nih.gov/29705869

AEs

AE	Significance	Dose	Population
Insomnia	17%	100 mg 1 times / day steady, oral Highest studied dose Dose: 100 mg, 1 times / day Route: oral Route: steady Dose: 100 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/29705869	healthy, 34.3 years(range: 19–45 years) n = 6 Health Status: healthy Age Group: 34.3 years(range: 19–45 years) Sex: M+F Population Size: 6 Sources: https://pubmed.ncbi.nlm.nih.gov/29705869
Dizziness	33%	100 mg 1 times / day steady, oral Highest studied dose Dose: 100 mg, 1 times / day Route: oral Route: steady Dose: 100 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/29705869	healthy, 34.3 years(range: 19–45 years) n = 6 Health Status: healthy Age Group: 34.3 years(range: 19–45 years) Sex: M+F Population Size: 6 Sources: https://pubmed.ncbi.nlm.nih.gov/29705869
Phlebitis	33%	100 mg 1 times / day steady, oral Highest studied dose Dose: 100 mg, 1 times / day Route: oral Route: steady Dose: 100 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/29705869	healthy, 34.3 years(range: 19–45 years) n = 6 Health Status: healthy Age Group: 34.3 years(range: 19–45 years) Sex: M+F Population Size: 6 Sources: https://pubmed.ncbi.nlm.nih.gov/29705869
Somnolence	67%	100 mg 1 times / day steady, oral Highest studied dose Dose: 100 mg, 1 times / day Route: oral Route: steady Dose: 100 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/29705869	healthy, 34.3 years(range: 19–45 years) n = 6 Health Status: healthy Age Group: 34.3 years(range: 19–45 years) Sex: M+F Population Size: 6 Sources: https://pubmed.ncbi.nlm.nih.gov/29705869
Fatigue	83%	100 mg 1 times / day steady, oral Highest studied dose Dose: 100 mg, 1 times / day Route: oral Route: steady Dose: 100 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/29705869	healthy, 34.3 years(range: 19–45 years) n = 6 Health Status: healthy Age Group: 34.3 years(range: 19–45 years) Sex: M+F Population Size: 6 Sources: https://pubmed.ncbi.nlm.nih.gov/29705869

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
inducer 781 substrate 1737 inhibitor 1587	inducer 389 inhibitor 1767	inhibitor 1852

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP3A 214 P-gp 1461 CYP1A2 1524 CYP2B6 810 CYP2C8 911 CYP2C19 1478 OATP1B1 788 BCRP 699 OCT2 647	CYP2C19 991 P-gp 1537 CYP3A 191	CYP1A2 701

Drug as perpetrator

Target	Modality	Activity	Metabolite
CYP2C19 1553	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/204569Orig1s007lbl.pdf#page=13 Page: 13.0	no [IC50 5.3 uM]
CYP1A2 1692	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/204569Orig1s007lbl.pdf#page=203 Page: 203.0	no [IC50 >100 uM]	L-002015883 2
CYP3A 298	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/204569Orig1s007lbl.pdf#page=247 Page: 247.0	no	L-002015883 2
CYP3A4 1925	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/204569Orig1s007lbl.pdf#page=203 Page: 203.0	weak [IC50 11 uM]	L-002015883 2
CYP2C8 965	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/204569Orig1s007lbl.pdf#page=13 Page: 13.0	weak [IC50 15 uM]
CYP2C9 1819	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/204569Orig1s007lbl.pdf#page=13 Page: 13.0	weak [IC50 15 uM]
CYP2D6 1891	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/204569Orig1s007lbl.pdf#page=13 Page: 13.0	weak [IC50 17 uM]
CYP2C19 1553	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/204569Orig1s007lbl.pdf#page=203 Page: 203.0	weak [IC50 35 uM]	L-002015883 2
CYP2C8 965	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/204569Orig1s007lbl.pdf#page=203 Page: 203.0	weak [IC50 37 uM]	L-002015883 2
CYP2D6 1891	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/204569Orig1s007lbl.pdf#page=203 Page: 203.0	weak [IC50 39 uM]	L-002015883 2
CYP2B6 1001	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/204569Orig1s007lbl.pdf#page=203 Page: 203.0	weak [IC50 44 uM]	L-002015883 2
CYP2C9 1819	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/204569Orig1s007lbl.pdf#page=203 Page: 203.0	weak [IC50 47 uM]	L-002015883 2
CYP2B6 1001	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/204569Orig1s007lbl.pdf#page=13 Page: 13.0	weak [IC50 64 uM]
CYP1A2 1692	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/204569Orig1s007lbl.pdf#page=13 Page: 13.0	weak [IC50 74 uM]
CYP2C9 1819	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/204569Orig1s007lbl.pdf#page=135 Page: 135.0	weak
OCT2 648	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/204569Orig1s007lbl.pdf#page=13 Page: 13.0	yes [IC50 1.3 uM]
OATP1B1 803	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/204569Orig1s007lbl.pdf#page=13 Page: 13.0	yes [IC50 10 uM]
CYP3A4 1925	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/204569Orig1s007lbl.pdf#page=203 Page: 203.0	yes [IC50 4 uM]
P-gp 1650	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/204569Orig1s007lbl.pdf#page=13 Page: 13.0	yes [IC50 73 uM]
BCRP 773	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/204569Orig1s007lbl.pdf#page=13 Page: 13.0	yes [Inhibition 15 uM]
BCRP 773	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/204569Orig1s007lbl.pdf#page=217 Page: 217.0	yes [Inhibition 15 uM]	L-002015883 2
CYP1A2 1692	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/204569Orig1s007lbl.pdf#page=135 Page: 135.0	yes
CYP3A 298	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/204569Orig1s007lbl.pdf#page=13 Page: 13.0	yes
CYP3A4 1925	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/204569Orig1s007lbl.pdf#page=135 Page: 135.0	yes

Drug as victim

Target	Modality	Activity	Metabolite
CYP2C19 991	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/204569Orig1s007lbl.pdf#page=12 Page: 12.0	minor
CYP3A 191	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/204569Orig1s007lbl.pdf#page=12 Page: 12.0	yes
CYP3A4 1737	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/204569Orig1s007lbl.pdf#page=200 Page: 200.0	yes
P-gp 1537	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/204569Orig1s007lbl.pdf#page=219 Page: 219.0	yes	L-002015883 2

Sourcing

Vendor/Aggregator	ID	URL
ChEBI	CHEBI:82698	https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:82698
ChemicalBook	CB62589660	https://www.chemicalbook.com/ChemicalProductProperty_EN_CB62589660
ChemicalBook	CB92599932	https://www.chemicalbook.com/ChemicalProductProperty_EN_CB92599932
ZINC	ZINC000049036447	http://zinc15.docking.org/substances/ZINC000049036447

PubMed

Title	Date	PubMed
Discovery of the dual orexin receptor antagonist [(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 (MK-4305) for the treatment of insomnia.	2010 Jul 22	20565075
The hypocretins/orexins: integrators of multiple physiological functions.	2014 Jan	24102345
Dual orexin receptor antagonists - promising agents in the treatment of sleep disorders.	2014 Jan	23702225
Safety and efficacy of suvorexant during 1-year treatment of insomnia with subsequent abrupt treatment discontinuation: a phase 3 randomised, double-blind, placebo-controlled trial.	2014 May	24680372
Suvorexant: a novel therapy for the treatment of insomnia.	2014 Oct	25291725
Suvorexant: a dual orexin receptor antagonist for the treatment of sleep onset and sleep maintenance insomnia.	2015 Apr	25667197
Suvorexant: something new for sleep?	2015 Feb	25397996

Patents

Sample Use Guides

In Vivo Use Guide

The recommended dose for BELSOMRA (suvorexant) is 10 mg, taken no more than once per night and within 30 minutes of going to bed, with at least 7 hours remaining before the planned time of awakening. If the 10 mg dose is well-tolerated but not effective, the dose can be increased. The maximum recommended dose of BELSOMRA is 20 mg once daily

Route of Administration: Oral

In Vitro Use Guide

Examination of Suvorexant in radioligand binding assays using tissue from transgenic rats expressing the human OX2R found nearly full receptor occupancy (>90%) at plasma exposures of 1.1 μM.

Substance Class	Chemical Created by `admin` on `Sat Dec 16 18:37:41 UTC 2023` Edited by `admin` on `Sat Dec 16 18:37:41 UTC 2023`
Record UNII	5D3S2VQZ54
Record Status	`Validated (UNII)`
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Name

Type

Language

SUVOREXANT HYDROCHLORIDE

Common Name

English

METHANONE, ((7R)-4-(5-CHLORO-2-BENZOXAZOLYL)HEXAHYDRO-7-METHYL-1H-1,4-DIAZEPIN-1-YL)(5-METHYL-2-(2H-1,2,3-TRIAZOL-2-YL)PHENYL)-, HYDROCHLORIDE (1:1)

Systematic Name

English

Code System Code Type Description

FDA UNII

5D3S2VQZ54

Created by admin on Sat Dec 16 18:37:41 UTC 2023 , Edited by admin on Sat Dec 16 18:37:41 UTC 2023

PRIMARY

PUBCHEM

102004303

Created by admin on Sat Dec 16 18:37:41 UTC 2023 , Edited by admin on Sat Dec 16 18:37:41 UTC 2023

PRIMARY

CAS

1818333-03-7

Created by admin on Sat Dec 16 18:37:41 UTC 2023 , Edited by admin on Sat Dec 16 18:37:41 UTC 2023

PRIMARY

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					081L192FO9

SUVOREXANT

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Amount:

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					081L192FO9

SUVOREXANT

ACTIVE MOIETY

Amount:

Details

SMILES

InChI

DescriptionSources: http://www.ncbi.nlm.nih.gov/pubmed/?term=PMC4419247Curator's Comment: description was created based on several sources, including http://www.accessdata.fda.gov/drugsatfda_docs/label/2014/204569s001lbl.pdf; http://www.ncbi.nlm.nih.gov/pubmed/?term=24102345

CNS Activity

Originator

Approval Year

Targets

Conditions

Approved Use

Launch Date

Cmax

AUC

T1/2

Funbound

Doses

AEs

Overview

OverviewOther

Drug as perpetrator​

Drug as victim

Sourcing

PubMed

Patents

Sample Use Guides

Description
Sources: http://www.ncbi.nlm.nih.gov/pubmed/?term=PMC4419247
Curator's Comment: description was created based on several sources, including http://www.accessdata.fda.gov/drugsatfda_docs/label/2014/204569s001lbl.pdf; http://www.ncbi.nlm.nih.gov/pubmed/?term=24102345

C_max

T_1/2

F_unbound

Drug as perpetrator