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

Stem definitionDrug idCAS RN
orexin receptor antagonists 4881 1030377-33-3

Description:

MoleculeDescription

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:

PropertyValueReference
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:

DateAgencyCompanyOrphan
Aug. 13, 2014 FDA MERCK SHARP DOHME

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients 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 termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients 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 termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients 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:

SourceCodeDescription
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|

DiseaseRelationSNOMED_IDDOID
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 levelDissociation constantType (acidic/basic)
pKa1 0.96 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent 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 strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
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:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Orexin receptor type 1 GPCR ANTAGONIST Ki 9.26 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Orexin receptor type 2 GPCR ANTAGONIST Ki 9.46 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Orexin receptor type 2 GPCR Ki 8.06 CHEMBL
Orexin receptor type 1 GPCR Ki 8.77 CHEMBL

External reference:

IDSource
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:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
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