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 586.06 23.67 493 4046 677345 46004178
Nightmare 162.58 23.67 61 4478 16537 46664986
Abnormal dreams 131.37 23.67 46 4493 10233 46671290
Insomnia 128.70 23.67 115 4424 164809 46516714
Somnolence 108.11 23.67 102 4437 156419 46525104
Sleep paralysis 107.79 23.67 21 4518 450 46681073
Poor quality sleep 93.44 23.67 40 4499 15213 46666310
Wrong technique in product usage process 84.08 23.67 57 4482 54365 46627158
Feeling abnormal 75.90 23.67 76 4463 124984 46556539
No adverse event 67.98 23.67 42 4497 34189 46647334
Product dose omission issue 65.30 23.67 81 4458 168439 46513084
Initial insomnia 53.33 23.67 19 4520 4433 46677090
Middle insomnia 42.44 23.67 20 4519 9495 46672028
Therapeutic product effect incomplete 41.02 23.67 44 4495 78109 46603414
Product packaging quantity issue 39.66 23.67 11 4528 1133 46680390
Hallucination 39.08 23.67 35 4504 49916 46631607
Sleep terror 38.85 23.67 10 4529 774 46680749
Sleep disorder 37.03 23.67 33 4506 46762 46634761
Altered state of consciousness 34.92 23.67 24 4515 23324 46658199
Inappropriate schedule of product administration 29.61 23.67 34 4505 64979 46616544
Product blister packaging issue 28.48 23.67 6 4533 192 46681331
Headache 28.23 23.67 106 4433 478246 46203277

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 447.32 23.28 307 2377 340080 29609714
Nightmare 143.19 23.28 50 2634 12026 29937768
Abnormal dreams 86.23 23.28 31 2653 8084 29941710
Somnolence 83.47 23.28 69 2615 96694 29853100
Poor quality sleep 82.00 23.28 29 2655 7212 29942582
Wrong technique in product usage process 66.88 23.28 39 2645 31116 29918678
Sleep paralysis 56.22 23.28 10 2674 139 29949655
Insomnia 49.91 23.28 51 2633 93285 29856509
Therapeutic product effect incomplete 46.60 23.28 32 2652 33802 29915992
No adverse event 46.00 23.28 25 2659 17394 29932400
Delirium 43.54 23.28 33 2651 40598 29909196
Sleep disorder 40.59 23.28 26 2658 24453 29925341
Hepatic function abnormal 36.20 23.28 30 2654 41915 29907879
Middle insomnia 36.06 23.28 15 2669 5758 29944036
Hangover 31.92 23.28 9 2675 1069 29948725
Initial insomnia 31.70 23.28 11 2673 2578 29947216
Oesophageal dilatation 30.91 23.28 6 2678 137 29949657
Product packaging quantity issue 30.91 23.28 8 2676 688 29949106
Feeling abnormal 28.44 23.28 30 2654 56726 29893068
Interstitial lung disease 25.28 23.28 29 2655 60168 29889626

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)

None

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 1 GPCR Ki 8.77 CHEMBL
Orexin receptor type 2 GPCR Ki 8.06 CHEMBL

External reference:

IDSource
D10082 KEGG_DRUG
4033910 VUID
N0000191283 NUI
4033910 VANDF
C3854974 UMLSCUI
CHEBI:82698 CHEBI
SUV PDB_CHEM_ID
CHEMBL1083659 ChEMBL_ID
C551624 MESH_SUPPLEMENTAL_RECORD_UI
24965990 PUBCHEM_CID
9435 INN_ID
DB09034 DRUGBANK_ID
081L192FO9 UNII
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 0006-0033 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