suvorexant 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
orexin receptor antagonists	4881	1030377-33-3

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: MK 4305 suvorexant belsomra MK-4305	a highly selective antagonist for orexin receptors OX1R and OX2R, 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 Molecular weight: 450.93 Formula: C23H23ClN6O2 CLOGP: 5.10 LIPINSKI: 0 HAC: 8 HDO: 0 TPSA: 80.29 ALOGS: -3.58 ROTB: 3 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

MK 4305
suvorexant
belsomra
MK-4305

a highly selective antagonist for orexin receptors OX1R and OX2R, 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

Molecular weight: 450.93
Formula: C23H23ClN6O2
CLOGP: 5.10
LIPINSKI: 0
HAC: 8
HDO: 0
TPSA: 80.29
ALOGS: -3.58
ROTB: 3

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

None

ADMET properties:

Property	Value	Reference
Vd (Volume of distribution)	0.69 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	0.84 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.05 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	10.37 hours	Lombardo F, Berellini G, Obach RS
BA (Bioavailability)	0.62 %	Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K

Approvals:

Date	Agency	Company	Orphan
Aug. 13, 2014	FDA	MERCK SHARP DOHME

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Drug ineffective	503.28	20.54	536	5246	1044229	62439011
Nightmare	172.13	20.54	65	5717	19129	63464111
Abnormal dreams	156.90	20.54	52	5730	10464	63472776
Sleep paralysis	138.03	20.54	27	5755	633	63482607
Somnolence	128.97	20.54	116	5666	178569	63304671
Poor quality sleep	95.05	20.54	43	5739	19892	63463348
Wrong technique in product usage process	92.17	20.54	62	5720	62278	63420962
No adverse event	91.06	20.54	53	5729	41352	63441888
Feeling abnormal	72.61	20.54	78	5704	148314	63334926
Product dose omission issue	71.71	20.54	97	5685	234216	63249024
Product packaging quantity issue	61.94	20.54	16	5766	1343	63481897
Hallucination	61.29	20.54	46	5736	54771	63428469
Initial insomnia	59.33	20.54	22	5760	6135	63477105
Altered state of consciousness	46.89	20.54	29	5753	25201	63458039
Product blister packaging issue	45.75	20.54	9	5773	217	63483023
Middle insomnia	44.09	20.54	22	5760	12621	63470619
Inappropriate schedule of product administration	33.17	20.54	44	5738	103921	63379319
Therapeutic product effect incomplete	31.12	20.54	47	5735	125009	63358231
Product quality issue	29.19	20.54	25	5757	35840	63447400
Suicidal ideation	29.04	20.54	32	5750	62389	63420851
Sleep terror	27.38	20.54	10	5772	2670	63480570
Delirium	27.21	20.54	28	5754	50513	63432727
Anxiety	26.44	20.54	60	5722	217481	63265759
Circumstance or information capable of leading to medication error	23.82	20.54	10	5772	3860	63479380
Sleep disorder	23.70	20.54	33	5749	81533	63401707
Somnambulism	23.41	20.54	11	5771	5532	63477708
Restlessness	22.89	20.54	20	5762	29433	63453807
Overdose	22.80	20.54	39	5743	115039	63368201
Poor quality product administered	22.29	20.54	9	5773	3147	63480093
Headache	21.64	20.54	114	5668	633127	62850113
Therapeutic product effect delayed	21.05	20.54	8	5774	2383	63480857
Abnormal sleep-related event	20.59	20.54	6	5776	787	63482453

FDA Adverse Event Reporting System (Male)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Drug ineffective	363.77	21.37	328	3317	456423	34496863
Nightmare	148.60	21.37	56	3589	14335	34938951
Abnormal dreams	94.85	21.37	34	3611	7544	34945742
Somnolence	82.94	21.37	78	3567	111038	34842248
Poor quality sleep	77.51	21.37	30	3615	8226	34945060
Wrong technique in product usage process	63.40	21.37	42	3603	35944	34917342
Sleep paralysis	52.60	21.37	10	3635	174	34953112
Delirium	51.39	21.37	40	3605	43951	34909335
Hepatic function abnormal	51.09	21.37	40	3605	44323	34908963
No adverse event	48.39	21.37	30	3615	22897	34930389
Interstitial lung disease	36.03	21.37	39	3606	65243	34888043
Hangover	35.26	21.37	10	3635	1041	34952245
Therapeutic product effect incomplete	34.77	21.37	34	3611	50507	34902779
Middle insomnia	34.60	21.37	16	3629	6786	34946500
Product packaging quantity issue	31.89	21.37	9	3636	920	34952366
Sleep disorder	31.01	21.37	26	3619	31662	34921624
Oesophageal dilatation	27.40	21.37	6	3639	215	34953071
Feeling abnormal	26.83	21.37	33	3612	63202	34890084
Altered state of consciousness	24.94	21.37	20	3625	22873	34930413
Therapeutic product effect delayed	24.78	21.37	8	3637	1290	34951996
Initial insomnia	24.58	21.37	10	3635	3114	34950172

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Drug ineffective	621.53	18.42	649	7611	1080264	78655864
Nightmare	272.52	18.42	102	8158	25759	79710369
Abnormal dreams	188.89	18.42	63	8197	11349	79724779
Somnolence	168.24	18.42	162	8098	238819	79497309
Sleep paralysis	153.66	18.42	30	8230	608	79735520
Poor quality sleep	133.62	18.42	59	8201	22663	79713465
Wrong technique in product usage process	108.72	18.42	77	8183	73798	79662330
Feeling abnormal	76.16	18.42	88	8172	159111	79577017
Delirium	72.19	18.42	64	8196	84563	79651565
Hallucination	69.49	18.42	63	8197	85682	79650446
Initial insomnia	68.06	18.42	26	8234	6912	79729216
Altered state of consciousness	65.18	18.42	46	8214	43776	79692352
Middle insomnia	64.32	18.42	32	8228	16037	79720091
Hepatic function abnormal	59.78	18.42	54	8206	73053	79663075
Hangover	44.45	18.42	14	8246	2098	79734030
Sleep disorder	43.70	18.42	49	8211	85628	79650500
Interstitial lung disease	43.64	18.42	56	8204	112544	79623584
Therapeutic product effect incomplete	42.16	18.42	62	8198	141583	79594545
Product packaging quantity issue	41.58	18.42	12	8248	1337	79734791
Inappropriate schedule of product administration	40.51	18.42	59	8201	133569	79602559
Therapeutic product effect delayed	39.42	18.42	14	8246	3032	79733096
Somnambulism	37.34	18.42	16	8244	5705	79730423
Suicidal ideation	34.45	18.42	41	8219	76299	79659829
Restlessness	24.39	18.42	27	8233	46465	79689663
Product dose omission issue	24.07	18.42	68	8192	247469	79488659
Stoma site hypergranulation	23.26	18.42	6	8254	439	79735689
Oesophageal dilatation	23.13	18.42	6	8254	449	79735679
Radiation pneumonitis	22.42	18.42	10	8250	3923	79732205
Circumstance or information capable of leading to medication error	22.38	18.42	10	8250	3938	79732190
Anxiety	20.12	18.42	64	8196	248448	79487680
Joint swelling	20.05	18.42	3	8257	288643	79447485
Liver disorder	19.12	18.42	30	8230	72387	79663741
Underdose	18.69	18.42	20	8240	33131	79702997

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	N05CM19	NERVOUS SYSTEM PSYCHOLEPTICS HYPNOTICS AND SEDATIVES Other hypnotics and sedatives
MeSH PA	D002491	Central Nervous System Agents
MeSH PA	D002492	Central Nervous System Depressants
MeSH PA	D006993	Hypnotics and Sedatives
MeSH PA	D018377	Neurotransmitter Agents
MeSH PA	D000068796	Orexin Receptor Antagonists
MeSH PA	D000068776	Sleep Aids, Pharmaceutical
FDA MoA	N0000185503	P-Glycoprotein Inhibitors
FDA MoA	N0000190114	Cytochrome P450 3A Inhibitors
FDA MoA	N0000190998	Orexin Receptor Antagonists
FDA EPC	N0000191000	Orexin Receptor Antagonist
CHEBI has role	CHEBI:35488	central nervous system depressants
CHEBI has role	CHEBI:83296	orexin receptor antagonists

Drug Use | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
Insomnia	indication	193462001
Narcolepsy	contraindication	60380001	DOID:8986

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	0.96	Basic

Orange Book patent data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
10MG	BELSOMRA	MERCK SHARP DOHME	N204569	Aug. 13, 2014	RX	TABLET	ORAL	7951797	Nov. 20, 2029	TREATMENT OF INSOMNIA
15MG	BELSOMRA	MERCK SHARP DOHME	N204569	Aug. 13, 2014	RX	TABLET	ORAL	7951797	Nov. 20, 2029	TREATMENT OF INSOMNIA
20MG	BELSOMRA	MERCK SHARP DOHME	N204569	Aug. 13, 2014	RX	TABLET	ORAL	7951797	Nov. 20, 2029	TREATMENT OF INSOMNIA
5MG	BELSOMRA	MERCK SHARP DOHME	N204569	Aug. 13, 2014	RX	TABLET	ORAL	7951797	Nov. 20, 2029	TREATMENT OF INSOMNIA

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
10MG	BELSOMRA	MERCK SHARP DOHME	N204569	Aug. 13, 2014	RX	TABLET	ORAL	Jan. 29, 2023	INFORMATION ADDED TO THE LABELING TO DESCRIBE STUDY P061, A RANDOMIZED, PLACEBO-CONTROLLED, PARALLEL GROUP, MULTI-SITE, DOUBLE-BLIND STUDY TO EVALUATE SAFETY AND EFFICACY OF SUVOREXANT FOR THE TREATMENT OF INSOMNIA IN SUBJECTS WITH ALZHEIMERS DISEASE
15MG	BELSOMRA	MERCK SHARP DOHME	N204569	Aug. 13, 2014	RX	TABLET	ORAL	Jan. 29, 2023	INFORMATION ADDED TO THE LABELING TO DESCRIBE STUDY P061, A RANDOMIZED, PLACEBO-CONTROLLED, PARALLEL GROUP, MULTI-SITE, DOUBLE-BLIND STUDY TO EVALUATE SAFETY AND EFFICACY OF SUVOREXANT FOR THE TREATMENT OF INSOMNIA IN SUBJECTS WITH ALZHEIMERS DISEASE
20MG	BELSOMRA	MERCK SHARP DOHME	N204569	Aug. 13, 2014	RX	TABLET	ORAL	Jan. 29, 2023	INFORMATION ADDED TO THE LABELING TO DESCRIBE STUDY P061, A RANDOMIZED, PLACEBO-CONTROLLED, PARALLEL GROUP, MULTI-SITE, DOUBLE-BLIND STUDY TO EVALUATE SAFETY AND EFFICACY OF SUVOREXANT FOR THE TREATMENT OF INSOMNIA IN SUBJECTS WITH ALZHEIMERS DISEASE
5MG	BELSOMRA	MERCK SHARP DOHME	N204569	Aug. 13, 2014	RX	TABLET	ORAL	Jan. 29, 2023	INFORMATION ADDED TO THE LABELING TO DESCRIBE STUDY P061, A RANDOMIZED, PLACEBO-CONTROLLED, PARALLEL GROUP, MULTI-SITE, DOUBLE-BLIND STUDY TO EVALUATE SAFETY AND EFFICACY OF SUVOREXANT FOR THE TREATMENT OF INSOMNIA IN SUBJECTS WITH ALZHEIMERS DISEASE

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Orexin receptor type 1	GPCR	O43613	OX1R_HUMAN	ANTAGONIST	Ki	9.26	SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
Orexin receptor type 2	GPCR	O43614	OX2R_HUMAN	ANTAGONIST	Ki	9.46	SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
Orexin receptor type 2	GPCR		OX2R_MOUSE		Ki	8.06	CHEMBL
Orexin receptor type 1	GPCR		OX1R_MOUSE		Ki	8.77	CHEMBL

External reference:

ID	Source
081L192FO9	UNII
D10082	KEGG_DRUG
4033910	VUID
N0000191283	NUI
4033910	VANDF
C3179535	UMLSCUI
CHEBI:82698	CHEBI
SUV	PDB_CHEM_ID
CHEMBL1083659	ChEMBL_ID
24965990	PUBCHEM_CID
DB09034	DRUGBANK_ID
9435	INN_ID
C551624	MESH_SUPPLEMENTAL_RECORD_UI
2890	IUPHAR_LIGAND_ID
1547099	RXNORM
227824	MMSL
30487	MMSL
d08281	MMSL
015650	NDDF
708714001	SNOMEDCT_US
715609002	SNOMEDCT_US

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
BELSOMRA	HUMAN PRESCRIPTION DRUG LABEL	1	0006-0005	TABLET, FILM COATED	5 mg	ORAL	NDA	36 sections
BELSOMRA	HUMAN PRESCRIPTION DRUG LABEL	1	0006-0005	TABLET, FILM COATED	5 mg	ORAL	NDA	36 sections
BELSOMRA	HUMAN PRESCRIPTION DRUG LABEL	1	0006-0005	TABLET, FILM COATED	5 mg	ORAL	NDA	36 sections
BELSOMRA	HUMAN PRESCRIPTION DRUG LABEL	1	0006-0033	TABLET, FILM COATED	10 mg	ORAL	NDA	36 sections
BELSOMRA	HUMAN PRESCRIPTION DRUG LABEL	1	0006-0033	TABLET, FILM COATED	10 mg	ORAL	NDA	36 sections
BELSOMRA	HUMAN PRESCRIPTION DRUG LABEL	1	0006-0033	TABLET, FILM COATED	10 mg	ORAL	NDA	36 sections
BELSOMRA	HUMAN PRESCRIPTION DRUG LABEL	1	0006-0325	TABLET, FILM COATED	15 mg	ORAL	NDA	36 sections
BELSOMRA	HUMAN PRESCRIPTION DRUG LABEL	1	0006-0325	TABLET, FILM COATED	15 mg	ORAL	NDA	36 sections
BELSOMRA	HUMAN PRESCRIPTION DRUG LABEL	1	0006-0325	TABLET, FILM COATED	15 mg	ORAL	NDA	36 sections
BELSOMRA	HUMAN PRESCRIPTION DRUG LABEL	1	0006-0335	TABLET, FILM COATED	20 mg	ORAL	NDA	36 sections
BELSOMRA	HUMAN PRESCRIPTION DRUG LABEL	1	0006-0335	TABLET, FILM COATED	20 mg	ORAL	NDA	36 sections
BELSOMRA	HUMAN PRESCRIPTION DRUG LABEL	1	0006-0335	TABLET, FILM COATED	20 mg	ORAL	NDA	36 sections