teprotumumab 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
human origin 5387 1036734-93-6

Description:

MoleculeDescription

Synonyms:

  • teprotumumab
  • teprotumumab-trbw
  • tepezza
  • RO4858696-000
  • R 1507
  • RG 1507
Teprotumumab-trbw’s mechanism of action in patients with Thyroid Eye Disease has not been fully characterized. Teprotumumab-trbw binds to IGF-1R and blocks its activation and signaling
  • Molecular weight:
  • Formula:
  • CLOGP:
  • LIPINSKI: None
  • HAC: None
  • HDO: None
  • TPSA:
  • ALOGS:
  • ROTB: None

Drug dosage:

None

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

None

Approvals:

DateAgencyCompanyOrphan
Jan. 21, 2020 FDA HORIZON THERAPEUTICS IRELAND

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
Tinnitus 351.43 38.22 109 3350 42993 90581995
Muscle spasms 233.60 38.22 135 3324 251748 90373240
Hypoacusis 233.32 38.22 72 3387 27778 90597210
Economic problem 202.62 38.22 42 3417 3239 90621749
Ear discomfort 183.82 38.22 48 3411 10152 90614836
Deafness neurosensory 182.13 38.22 44 3415 6797 90618191
Physical disability 177.74 38.22 39 3420 3942 90621046
Deafness permanent 151.68 38.22 25 3434 536 90624452
Deafness 146.28 38.22 48 3411 22466 90602522
Concomitant disease aggravated 127.65 38.22 37 3422 11481 90613507
Emotional distress 123.41 38.22 48 3411 36614 90588374
Amenorrhoea 118.21 38.22 35 3424 11687 90613301
Blood glucose increased 106.71 38.22 58 3401 95188 90529800
Exophthalmos 105.03 38.22 22 3437 1780 90623208
Diplopia 98.04 38.22 38 3421 28676 90596312
Disability 91.66 38.22 40 3419 40705 90584283
Glycosylated haemoglobin increased 80.59 38.22 28 3431 15534 90609454
Impaired quality of life 76.76 38.22 30 3429 23114 90601874
Autophony 68.93 38.22 9 3450 32 90624956
Auditory disorder 65.85 38.22 14 3445 1216 90623772
Hyperglycaemia 51.41 38.22 29 3430 50941 90574047
Anxiety 51.27 38.22 61 3398 309711 90315277
Deafness unilateral 47.08 38.22 13 3446 3378 90621610
Eyelid retraction 46.51 38.22 7 3452 81 90624907
Blood thyroid stimulating hormone increased 45.57 38.22 16 3443 9139 90615849
Onychoclasis 44.90 38.22 15 3444 7384 90617604
Thyroid stimulating immunoglobulin increased 43.21 38.22 7 3452 134 90624854
Injury 41.39 38.22 44 3415 197305 90427683
Product quality issue 39.65 38.22 29 3430 79296 90545692
Eye pain 38.86 38.22 23 3436 44145 90580843

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
Tinnitus 101.26 49.86 35 1055 28903 42591342
Muscle spasms 96.93 49.86 46 1044 85998 42534247
Physical disability 94.89 49.86 19 1071 1854 42618391
Deafness permanent 94.06 49.86 14 1076 231 42620014
Economic problem 83.72 49.86 17 1073 1778 42618467
Hypoacusis 78.67 49.86 26 1064 18676 42601569
Emotional distress 70.18 49.86 23 1067 16070 42604175
Deafness 66.37 49.86 21 1069 13119 42607126
Injury 59.13 49.86 22 1068 22294 42597951
Disability 58.80 49.86 16 1074 5917 42614328
Blood glucose increased 58.08 49.86 31 1059 73668 42546577
Diplopia 53.71 49.86 20 1070 20296 42599949
Concomitant disease aggravated 52.61 49.86 15 1075 6571 42613674

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
Tinnitus 362.46 39.89 120 3945 60420 110524814
Economic problem 293.36 39.89 59 4006 4072 110581162
Physical disability 275.14 39.89 58 4007 5048 110580186
Deafness permanent 235.72 39.89 39 4026 892 110584342
Muscle spasms 212.57 39.89 130 3935 278027 110307207
Deafness neurosensory 208.21 39.89 52 4013 9567 110575667
Emotional distress 198.41 39.89 71 3994 44776 110540458
Concomitant disease aggravated 180.83 39.89 52 4013 16312 110568922
Ear discomfort 176.15 39.89 47 4018 11202 110574032
Disability 165.01 39.89 56 4009 30167 110555067
Hypoacusis 156.67 39.89 56 4009 35135 110550099
Deafness 136.07 39.89 47 4018 26662 110558572
Impaired quality of life 119.51 39.89 44 4021 29973 110555261
Blood glucose increased 108.75 39.89 65 4000 132431 110452803
Diplopia 101.92 39.89 43 4022 41851 110543383
Injury 93.77 39.89 66 3999 177199 110408035
Anxiety 88.11 39.89 84 3981 344994 110240240
Auditory disorder 87.22 39.89 18 4047 1406 110583828
Glycosylated haemoglobin increased 77.25 39.89 30 4035 23589 110561645
Exophthalmos 73.48 39.89 17 4048 2256 110582978
Discomfort 71.99 39.89 61 4004 214646 110370588
Autophony 69.27 39.89 9 4056 32 110585202
Product quality issue 68.80 39.89 40 4025 77259 110507975
Amenorrhoea 61.92 39.89 20 4045 9211 110576023
Blood thyroid stimulating hormone increased 41.54 39.89 16 4049 12285 110572949

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L04AG13 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
IMMUNOSUPPRESSANTS
IMMUNOSUPPRESSANTS
Monoclonal antibodies
FDA EPC N0000193926 Insulin-like Growth Factor-1 Receptor Inhibitor
FDA MoA N0000193927 Insulin-like Growth Factor-1 Receptor Inhibitors
CHEBI has role CHEBI:35610 antineoplastic agent

Related Drugs by ATC class:

L04AG Monoclonal antibodies 14 drugs
alemtuzumabanifrolumabaxatilimab-csfrbelimumabefalizumabemapalumabinebilizumabmuromonab-CD3natalizumabocrelizumabofatumumabsibeprenlimab-szsi show all 14 →

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Thyroid eye disease indication 276177000




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Insulin-like growth factor 1 receptor Kinase ANTAGONIST IC50 9 SCIENTIFIC LITERATURE DRUG LABEL

External reference:

IDSource
Y64GQ0KC0A UNII
4039110 VANDF
4039111 VANDF
C2987429 UMLSCUI
CHEBI:750156 CHEBI
CHEMBL1743079 ChEMBL_ID
DB06343 DRUGBANK_ID
9107 INN_ID
C551399 MESH_SUPPLEMENTAL_RECORD_UI
C558734 MESH_SUPPLEMENTAL_RECORD_UI
D09680 KEGG_DRUG
10612 IUPHAR_LIGAND_ID
840364008 SNOMEDCT_US
840397009 SNOMEDCT_US
329754 MMSL
37968 MMSL
d09494 MMSL
5376617 PUBCHEM_CID
018259 NDDF
2274802 RXNORM

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
TEPEZZA HUMAN PRESCRIPTION DRUG LABEL 1 75987-130 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 500 mg INTRAVENOUS BLA 30 sections
TEPEZZA HUMAN PRESCRIPTION DRUG LABEL 1 75987-130 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 500 mg INTRAVENOUS BLA 30 sections