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

Stem definitionDrug idCAS RN
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: ONP

  • 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

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 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 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 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 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 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:

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 0006-0033 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