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	526.62	21.60	513	4576	818820	49781215
Nightmare	173.39	21.60	64	5025	16022	50584013
Abnormal dreams	145.75	21.60	49	5040	9328	50590707
Somnolence	121.42	21.60	110	4979	154875	50445160
Sleep paralysis	116.57	21.60	23	5066	509	50599526
Poor quality sleep	91.96	21.60	41	5048	16605	50583430
Wrong technique in product usage process	88.36	21.60	60	5029	55450	50544585
No adverse event	85.65	21.60	49	5040	33529	50566506
Feeling abnormal	75.29	21.60	77	5012	125415	50474620
Product dose omission issue	74.66	21.60	92	4997	183746	50416289
Product packaging quantity issue	64.02	21.60	16	5073	1064	50598971
Initial insomnia	53.76	21.60	20	5069	5095	50594940
Hallucination	50.54	21.60	40	5049	46617	50553418
Product blister packaging issue	48.02	21.60	9	5080	150	50599885
Middle insomnia	47.10	21.60	22	5067	9899	50590136
Sleep terror	39.32	21.60	10	5079	713	50599322
Altered state of consciousness	37.98	21.60	25	5064	21885	50578150
Therapeutic product effect incomplete	37.36	21.60	46	5043	91469	50508566
Inappropriate schedule of product administration	32.41	21.60	38	5051	71793	50528242
Sleep disorder	30.43	21.60	33	5056	57250	50542785
Product quality issue	28.24	21.60	24	5065	30834	50569201
Suicidal ideation	26.14	21.60	30	5059	55355	50544680
Headache	25.97	21.60	110	4979	506425	50093610
Circumstance or information capable of leading to medication error	24.73	21.60	10	5079	3178	50596857
Anxiety	23.74	21.60	54	5035	177552	50422483
Poor quality product administered	22.41	21.60	9	5080	2810	50597225

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	394.82	22.89	315	2858	362855	29208499
Nightmare	140.79	22.89	51	3122	11366	29559988
Abnormal dreams	89.33	22.89	32	3141	6888	29564466
Somnolence	82.24	22.89	73	3100	93882	29477472
Poor quality sleep	80.55	22.89	30	3143	7203	29564151
Wrong technique in product usage process	65.02	22.89	41	3132	31387	29539967
Sleep paralysis	53.04	22.89	10	3163	161	29571193
Hepatic function abnormal	52.20	22.89	39	3134	39220	29532134
No adverse event	46.99	22.89	27	3146	17451	29553903
Delirium	43.36	22.89	35	3138	39362	29531992
Therapeutic product effect incomplete	37.19	22.89	32	3141	39273	29532081
Middle insomnia	36.86	22.89	16	3157	5692	29565662
Sleep disorder	36.41	22.89	26	3147	24360	29546994
Hangover	35.70	22.89	10	3163	967	29570387
Interstitial lung disease	31.94	22.89	35	3138	57683	29513671
Oesophageal dilatation	29.75	22.89	6	3167	139	29571215
Product packaging quantity issue	28.73	22.89	8	3165	757	29570597
Feeling abnormal	28.38	22.89	32	3141	54413	29516941
Initial insomnia	25.45	22.89	10	3163	2765	29568589

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	687.39	20.28	632	6581	839615	63651904
Nightmare	274.43	20.28	99	7114	20894	64470625
Abnormal dreams	178.25	20.28	60	7153	10296	64481223
Somnolence	168.20	20.28	156	7057	203489	64288030
Sleep paralysis	143.10	20.28	28	7185	530	64490989
Poor quality sleep	139.60	20.28	59	7154	18892	64472627
Wrong technique in product usage process	107.66	20.28	75	7138	64899	64426620
Feeling abnormal	81.58	20.28	87	7126	133515	64358004
Initial insomnia	70.64	20.28	26	7187	5778	64485741
Middle insomnia	68.74	20.28	32	7181	12845	64478674
Hallucination	60.30	20.28	56	7157	72732	64418787
Delirium	58.80	20.28	54	7159	69140	64422379
Altered state of consciousness	56.38	20.28	41	7172	37861	64453658
Sleep disorder	55.46	20.28	49	7164	59660	64431859
Hepatic function abnormal	54.27	20.28	50	7163	64263	64427256
Therapeutic product effect incomplete	50.48	20.28	60	7153	103422	64388097
Hangover	44.85	20.28	14	7199	1887	64489632
Inappropriate schedule of product administration	40.92	20.28	51	7162	92235	64399284
Interstitial lung disease	40.16	20.28	52	7161	97680	64393839
Product packaging quantity issue	39.97	20.28	11	7202	955	64490564
Therapeutic product effect delayed	36.91	20.28	13	7200	2546	64488973
Suicidal ideation	33.11	20.28	39	7174	66503	64425016
Product dose omission issue	25.82	20.28	63	7150	194684	64296835
Somnambulism	25.05	20.28	12	7201	5129	64486390
Sleep terror	24.86	20.28	8	7205	1189	64490330
Oesophageal dilatation	24.37	20.28	6	7207	336	64491183
Headache	23.53	20.28	119	7094	529348	63962171
Circumstance or information capable of leading to medication error	23.25	20.28	10	7203	3330	64488189
Restlessness	20.92	20.28	24	7189	39761	64451758

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