suvorexant 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: 4.79
  • 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 554.93 23.13 512 4512 816733 52527309
Nightmare 167.70 23.13 63 4961 17688 53326354
Insomnia 146.70 23.13 129 4895 186943 53157099
Abnormal dreams 143.01 23.13 49 4975 10552 53333490
Somnolence 116.27 23.13 108 4916 167626 53176416
Sleep paralysis 115.70 23.13 23 5001 567 53343475
Poor quality sleep 92.98 23.13 41 4983 17282 53326760
Wrong technique in product usage process 87.68 23.13 60 4964 59972 53284070
No adverse event 81.52 23.13 49 4975 39216 53304826
Product dose omission issue 78.10 23.13 93 4931 191527 53152515
Feeling abnormal 74.67 23.13 77 4947 135224 53208818
Initial insomnia 58.64 23.13 21 5003 5134 53338908
Product packaging quantity issue 57.40 23.13 15 5009 1274 53342768
Middle insomnia 49.98 23.13 23 5001 10685 53333357
Product blister packaging issue 46.20 23.13 9 5015 199 53343843
Hallucination 45.75 23.13 39 4985 53799 53290243
Therapeutic product effect incomplete 39.69 23.13 46 4978 91738 53252304
Sleep terror 38.49 23.13 10 5014 830 53343212
Sleep disorder 36.99 23.13 36 4988 58834 53285208
Altered state of consciousness 36.62 23.13 25 4999 24811 53319231
Inappropriate schedule of product administration 31.48 23.13 37 4987 74841 53269201
Suicidal ideation 25.59 23.13 30 4994 60481 53283561
Headache 24.87 23.13 108 4916 536713 52807329
Product quality issue 23.92 23.13 23 5001 37000 53307042
Circumstance or information capable of leading to medication error 23.79 23.13 10 5014 3744 53340298

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 419.90 24.01 317 2758 383160 32127291
Nightmare 139.99 24.01 51 3024 13115 32497336
Poor quality sleep 84.73 24.01 31 3044 8043 32502408
Abnormal dreams 82.95 24.01 31 3044 8533 32501918
Somnolence 81.92 24.01 72 3003 103725 32406726
Wrong technique in product usage process 65.66 24.01 41 3034 35018 32475433
Insomnia 55.05 24.01 57 3018 100291 32410160
Sleep paralysis 53.25 24.01 10 3065 180 32510271
Hepatic function abnormal 47.56 24.01 37 3038 44803 32465648
No adverse event 46.71 24.01 27 3048 20026 32490425
Delirium 41.69 24.01 34 3041 44012 32466439
Sleep disorder 39.55 24.01 27 3048 26725 32483726
Therapeutic product effect incomplete 39.31 24.01 32 3043 41309 32469142
Middle insomnia 36.84 24.01 16 3059 6468 32503983
Hangover 35.79 24.01 10 3065 1089 32509362
Interstitial lung disease 32.16 24.01 35 3040 64966 32445485
Oesophageal dilatation 30.30 24.01 6 3069 144 32510307
Initial insomnia 29.28 24.01 11 3064 3061 32507390
Product packaging quantity issue 29.07 24.01 8 3067 823 32509628
Feeling abnormal 28.95 24.01 32 3043 60391 32450060

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 CNS depressants
CHEBI has role CHEBI:83296 orexin receptor antagonists

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Insomnia indication 193462001
Narcolepsy contraindication 60380001 DOID:8986

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
C551624 MESH_SUPPLEMENTAL_RECORD_UI
2890 IUPHAR_LIGAND_ID
9435 INN_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 0006-0033 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 0006-0335 TABLET, FILM COATED 20 mg ORAL NDA 36 sections