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 516.49 22.37 526 4918 918463 55368160
Nightmare 172.99 22.37 64 5380 16762 56269861
Abnormal dreams 150.22 22.37 50 5394 9599 56277024
Insomnia 140.83 22.37 129 5315 191731 56094892
Somnolence 127.96 22.37 114 5330 163299 56123324
Sleep paralysis 121.90 22.37 24 5420 547 56286076
Poor quality sleep 90.95 22.37 41 5403 17714 56268909
Wrong technique in product usage process 90.31 22.37 61 5383 58107 56228516
No adverse event 83.78 22.37 49 5395 36325 56250298
Feeling abnormal 73.74 22.37 77 5367 133525 56153098
Product dose omission issue 71.15 22.37 93 5351 204660 56081963
Initial insomnia 63.89 22.37 23 5421 5556 56281067
Product packaging quantity issue 62.78 22.37 16 5428 1198 56285425
Hallucination 54.39 22.37 42 5402 49107 56237516
Product blister packaging issue 47.46 22.37 9 5435 167 56286456
Middle insomnia 45.84 22.37 22 5422 10928 56275695
Altered state of consciousness 40.18 22.37 26 5418 22995 56263628
Sleep terror 39.27 22.37 10 5434 746 56285877
Therapeutic product effect incomplete 34.93 22.37 47 5397 105984 56180639
Inappropriate schedule of product administration 33.84 22.37 41 5403 83346 56203277
Sleep disorder 32.00 22.37 36 5408 67627 56218996
Product quality issue 30.55 22.37 25 5419 31711 56254912
Suicidal ideation 27.78 22.37 31 5413 57711 56228912
Anxiety 26.53 22.37 58 5386 193114 56093509
Delirium 26.11 22.37 26 5418 42491 56244132
Circumstance or information capable of leading to medication error 24.35 22.37 10 5434 3438 56283185
Headache 23.21 22.37 111 5333 558933 55727690
Poor quality product administered 22.51 22.37 9 5435 2890 56283733

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 384.85 22.95 323 3103 395250 31298668
Nightmare 144.74 22.95 53 3373 12084 31681834
Abnormal dreams 88.25 22.95 32 3394 7076 31686842
Somnolence 86.01 22.95 77 3349 99368 31594550
Poor quality sleep 78.59 22.95 30 3396 7648 31686270
Insomnia 63.90 22.95 64 3362 94772 31599146
Wrong technique in product usage process 62.50 22.95 41 3385 33302 31660616
Sleep paralysis 52.29 22.95 10 3416 173 31693745
Hepatic function abnormal 50.24 22.95 39 3387 41183 31652735
No adverse event 49.07 22.95 29 3397 19596 31674322
Delirium 43.67 22.95 36 3390 41385 31652533
Therapeutic product effect incomplete 37.96 22.95 34 3392 43662 31650256
Sleep disorder 36.66 22.95 27 3399 26321 31667597
Middle insomnia 35.72 22.95 16 3410 6083 31687835
Hangover 35.55 22.95 10 3416 975 31692943
Interstitial lung disease 35.09 22.95 38 3388 61365 31632553
Product packaging quantity issue 32.70 22.95 9 3417 810 31693108
Oesophageal dilatation 29.67 22.95 6 3420 140 31693778
Initial insomnia 28.44 22.95 11 3415 2898 31691020
Feeling abnormal 26.98 22.95 32 3394 56970 31636948

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 666.33 20.33 646 7080 939106 69981612
Nightmare 271.72 20.33 99 7627 22057 70898661
Abnormal dreams 178.40 20.33 60 7666 10543 70910175
Somnolence 169.78 20.33 159 7567 215447 70705271
Insomnia 145.83 20.33 147 7579 217659 70703059
Sleep paralysis 141.29 20.33 28 7698 583 70920135
Poor quality sleep 137.04 20.33 59 7667 20290 70900428
Wrong technique in product usage process 105.64 20.33 75 7651 68623 70852095
Feeling abnormal 78.90 20.33 87 7639 142232 70778486
Initial insomnia 76.54 20.33 28 7698 6281 70914437
Middle insomnia 66.87 20.33 32 7694 14021 70906697
Delirium 66.25 20.33 59 7667 74555 70846163
Hallucination 65.14 20.33 59 7667 76201 70844517
Altered state of consciousness 57.60 20.33 42 7684 39980 70880738
Sleep disorder 53.75 20.33 51 7675 69821 70850897
Hepatic function abnormal 53.01 20.33 50 7676 67946 70852772
Therapeutic product effect incomplete 47.79 20.33 62 7664 119820 70800898
Hangover 44.98 20.33 14 7712 1919 70918799
Interstitial lung disease 43.07 20.33 55 7671 104630 70816088
Product packaging quantity issue 42.96 20.33 12 7714 1130 70919588
Inappropriate schedule of product administration 40.35 20.33 54 7672 107501 70813217
Therapeutic product effect delayed 36.25 20.33 13 7713 2754 70917964
Suicidal ideation 32.52 20.33 39 7687 69557 70851161
Somnambulism 28.17 20.33 13 7713 5247 70915471
Sleep terror 24.95 20.33 8 7718 1207 70919511
Product dose omission issue 24.41 20.33 65 7661 217403 70703315
Oesophageal dilatation 24.26 20.33 6 7720 352 70920366
Stoma site hypergranulation 23.46 20.33 6 7720 403 70920315
Circumstance or information capable of leading to medication error 22.81 20.33 10 7716 3580 70917138
Radiation pneumonitis 22.54 20.33 10 7716 3683 70917035
Restlessness 22.00 20.33 25 7701 42103 70878615
Anxiety 21.90 20.33 63 7663 220267 70700451
Headache 20.33 20.33 120 7606 580285 70340433

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