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

Stem definition	Drug id	CAS RN
	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: ONP 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: ONP

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

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	516.49	22.37	526	4918	918463	55368160
Nightmare	172.99	22.37	64	5380	16762	56269861
Abnormal dreams	150.22	22.37	50	5394	9599	56277024
Insomnia	140.83	22.37	129	5315	191731	56094892
Somnolence	127.96	22.37	114	5330	163299	56123324
Sleep paralysis	121.90	22.37	24	5420	547	56286076
Poor quality sleep	90.95	22.37	41	5403	17714	56268909
Wrong technique in product usage process	90.31	22.37	61	5383	58107	56228516
No adverse event	83.78	22.37	49	5395	36325	56250298
Feeling abnormal	73.74	22.37	77	5367	133525	56153098
Product dose omission issue	71.15	22.37	93	5351	204660	56081963
Initial insomnia	63.89	22.37	23	5421	5556	56281067
Product packaging quantity issue	62.78	22.37	16	5428	1198	56285425
Hallucination	54.39	22.37	42	5402	49107	56237516
Product blister packaging issue	47.46	22.37	9	5435	167	56286456
Middle insomnia	45.84	22.37	22	5422	10928	56275695
Altered state of consciousness	40.18	22.37	26	5418	22995	56263628
Sleep terror	39.27	22.37	10	5434	746	56285877
Therapeutic product effect incomplete	34.93	22.37	47	5397	105984	56180639
Inappropriate schedule of product administration	33.84	22.37	41	5403	83346	56203277
Sleep disorder	32.00	22.37	36	5408	67627	56218996
Product quality issue	30.55	22.37	25	5419	31711	56254912
Suicidal ideation	27.78	22.37	31	5413	57711	56228912
Anxiety	26.53	22.37	58	5386	193114	56093509
Delirium	26.11	22.37	26	5418	42491	56244132
Circumstance or information capable of leading to medication error	24.35	22.37	10	5434	3438	56283185
Headache	23.21	22.37	111	5333	558933	55727690
Poor quality product administered	22.51	22.37	9	5435	2890	56283733

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	384.85	22.95	323	3103	395250	31298668
Nightmare	144.74	22.95	53	3373	12084	31681834
Abnormal dreams	88.25	22.95	32	3394	7076	31686842
Somnolence	86.01	22.95	77	3349	99368	31594550
Poor quality sleep	78.59	22.95	30	3396	7648	31686270
Insomnia	63.90	22.95	64	3362	94772	31599146
Wrong technique in product usage process	62.50	22.95	41	3385	33302	31660616
Sleep paralysis	52.29	22.95	10	3416	173	31693745
Hepatic function abnormal	50.24	22.95	39	3387	41183	31652735
No adverse event	49.07	22.95	29	3397	19596	31674322
Delirium	43.67	22.95	36	3390	41385	31652533
Therapeutic product effect incomplete	37.96	22.95	34	3392	43662	31650256
Sleep disorder	36.66	22.95	27	3399	26321	31667597
Middle insomnia	35.72	22.95	16	3410	6083	31687835
Hangover	35.55	22.95	10	3416	975	31692943
Interstitial lung disease	35.09	22.95	38	3388	61365	31632553
Product packaging quantity issue	32.70	22.95	9	3417	810	31693108
Oesophageal dilatation	29.67	22.95	6	3420	140	31693778
Initial insomnia	28.44	22.95	11	3415	2898	31691020
Feeling abnormal	26.98	22.95	32	3394	56970	31636948

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	666.33	20.33	646	7080	939106	69981612
Nightmare	271.72	20.33	99	7627	22057	70898661
Abnormal dreams	178.40	20.33	60	7666	10543	70910175
Somnolence	169.78	20.33	159	7567	215447	70705271
Insomnia	145.83	20.33	147	7579	217659	70703059
Sleep paralysis	141.29	20.33	28	7698	583	70920135
Poor quality sleep	137.04	20.33	59	7667	20290	70900428
Wrong technique in product usage process	105.64	20.33	75	7651	68623	70852095
Feeling abnormal	78.90	20.33	87	7639	142232	70778486
Initial insomnia	76.54	20.33	28	7698	6281	70914437
Middle insomnia	66.87	20.33	32	7694	14021	70906697
Delirium	66.25	20.33	59	7667	74555	70846163
Hallucination	65.14	20.33	59	7667	76201	70844517
Altered state of consciousness	57.60	20.33	42	7684	39980	70880738
Sleep disorder	53.75	20.33	51	7675	69821	70850897
Hepatic function abnormal	53.01	20.33	50	7676	67946	70852772
Therapeutic product effect incomplete	47.79	20.33	62	7664	119820	70800898
Hangover	44.98	20.33	14	7712	1919	70918799
Interstitial lung disease	43.07	20.33	55	7671	104630	70816088
Product packaging quantity issue	42.96	20.33	12	7714	1130	70919588
Inappropriate schedule of product administration	40.35	20.33	54	7672	107501	70813217
Therapeutic product effect delayed	36.25	20.33	13	7713	2754	70917964
Suicidal ideation	32.52	20.33	39	7687	69557	70851161
Somnambulism	28.17	20.33	13	7713	5247	70915471
Sleep terror	24.95	20.33	8	7718	1207	70919511
Product dose omission issue	24.41	20.33	65	7661	217403	70703315
Oesophageal dilatation	24.26	20.33	6	7720	352	70920366
Stoma site hypergranulation	23.46	20.33	6	7720	403	70920315
Circumstance or information capable of leading to medication error	22.81	20.33	10	7716	3580	70917138
Radiation pneumonitis	22.54	20.33	10	7716	3683	70917035
Restlessness	22.00	20.33	25	7701	42103	70878615
Anxiety	21.90	20.33	63	7663	220267	70700451
Headache	20.33	20.33	120	7606	580285	70340433

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	0006-0033	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	0006-0335	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