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

Stem definitionDrug idCAS RN
human origin 5500 1572943-04-4

Description:

MoleculeDescription

Molfile

Synonyms:

  • tezepelumab
  • tezepelumab-ekko
  • tezspire
  • MEDI19929
  • AMG 157
Tezepelumab-ekko is a thymic stromal lymphopoietin (TSLP) blocker, human monoclonal antibody IgG2lambda that binds to human TSLP with a dissociation constant of 15.8 pM and blocks its interaction with the heterodimeric TSLP receptor. TSLP is a cytokine mainly derived from epithelial cells and occupies an upstream position in the asthma inflammatory cascade. Airway inflammation is an important component in the pathogenesis of asthma. Multiple cell types (e.g., mast cells, eosinophils, neutrophils, macrophages, lymphocytes, ILC2 cells) and mediators (e.g., histamine, eicosanoids, leukotrienes, cytokines) are involved in airway inflammation. Blocking TSLP with tezepelumab-ekko reduces biomarkers and cytokines associated with inflammation including blood eosinophils, airway submucosal eosinophils, IgE, FeNO, IL-5, and IL-13; however, the mechanism of tezepelumab-ekko action in asthma has not been definitively established.
  • Molecular weight:
  • Formula:
  • CLOGP:
  • LIPINSKI: None
  • HAC: None
  • HDO: None
  • TPSA:
  • ALOGS:
  • ROTB: None

Drug dosage:

DoseUnitRoute
7.50 mg P

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

None

Approvals:

DateAgencyCompanyOrphan
Dec. 17, 2021 FDA ASTRAZENECA AB
Sept. 19, 2022 EMA ASTRAZENECA AB
Sept. 26, 2022 PMDA ASTRAZENECA K.K

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
Asthma 273.89 24.07 188 6523 241972 90379764
Dyspnoea 184.85 24.07 272 6439 880683 89741053
Arthralgia 153.83 24.07 234 6477 778288 89843448
Cough 139.09 24.07 153 6558 368809 90252927
Wheezing 107.83 24.07 109 6602 237971 90383765
Chest discomfort 69.30 24.07 67 6644 138298 90483438
Rhinitis allergic 60.51 24.07 28 6683 16757 90604979
Back pain 58.83 24.07 93 6618 317082 90304654
Anaphylactic reaction 58.78 24.07 50 6661 87474 90534262
Drug ineffective 46.22 24.07 213 6498 1384085 89237651
Quality of life decreased 40.27 24.07 19 6692 11870 90609866
Neonatal infection 40.02 24.07 8 6703 260 90621476
COVID-19 39.11 24.07 55 6656 168788 90452948
Impaired quality of life 38.47 24.07 23 6688 23121 90598615
Productive cough 37.94 24.07 37 6674 77026 90544710
Injection site pain 36.46 24.07 54 6657 173645 90448091
Throat tightness 35.75 24.07 24 6687 29460 90592276
Death 34.16 24.07 92 6619 456459 90165277
Urticaria 34.16 24.07 73 6638 312661 90309075
Device leakage 33.94 24.07 16 6695 9975 90611761
Pneumonia pseudomonal 31.45 24.07 11 6700 3192 90618544
Illness 30.71 24.07 34 6677 81935 90539801
Myalgia 30.55 24.07 50 6661 175075 90446661
Upper-airway cough syndrome 30.37 24.07 17 6694 15118 90606618
Device use issue 29.86 24.07 11 6700 3702 90618034
Insurance issue 29.58 24.07 15 6696 10943 90610793
Bronchiectasis 29.07 24.07 19 6692 22311 90599425
Gastrooesophageal reflux disease 28.35 24.07 47 6664 166290 90455446
Oropharyngeal pain 27.37 24.07 38 6673 115149 90506587
Dysphonia 26.85 24.07 28 6683 63056 90558680
Seasonal allergy 26.18 24.07 18 6693 22965 90598771
Rash 25.25 24.07 121 6590 795979 89825757
Incorrect dose administered by device 25.23 24.07 11 6700 5726 90616010
Pneumonia 24.75 24.07 103 6608 637956 89983780
Eosinophil count increased 24.37 24.07 14 6697 13067 90608669
Secretion discharge 24.37 24.07 15 6696 15881 90605855

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
Asthma 113.36 35.44 57 2040 62257 42556981
Wheezing 81.98 35.44 44 2053 54737 42564501
Arthralgia 78.47 35.44 71 2026 205167 42414071
Dyspnoea 59.17 35.44 89 2008 442532 42176706
Cough 57.17 35.44 56 2041 178047 42441191
Chronic obstructive pulmonary disease 43.62 35.44 31 2066 63083 42556155
Death 38.10 35.44 76 2021 471109 42148129

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
Asthma 209.81 26.65 140 5487 250151 110333521
Cough 147.44 26.65 147 5480 461494 110122178
Dyspnoea 138.52 26.65 220 5407 1106652 109477020
Arthralgia 138.31 26.65 183 5444 779449 109804223
Wheezing 117.79 26.65 100 5527 255130 110328542
Chest discomfort 65.88 26.65 61 5566 173787 110409885
Productive cough 46.97 26.65 42 5585 114263 110469409
Rhinitis allergic 45.82 26.65 21 5606 17901 110565771
Drug ineffective 41.17 26.65 169 5458 1520371 109063301
Chronic obstructive pulmonary disease 40.72 26.65 38 5589 109120 110474552
Snoring 38.20 26.65 14 5613 6770 110576902
Upper-airway cough syndrome 35.64 26.65 17 5610 15840 110567832
Insurance issue 35.42 26.65 15 5612 10597 110573075
Secretion discharge 34.55 26.65 18 5609 20226 110563446
Back pain 34.44 26.65 65 5562 370931 110212741
Nasal congestion 30.62 26.65 31 5596 98251 110485421
Pneumonia 29.82 26.65 105 5522 876609 109707063
Device use issue 29.70 26.65 10 5617 3774 110579898
Device leakage 29.50 26.65 15 5612 16033 110567639
Bronchiectasis 29.42 26.65 20 5607 36473 110547199
Anaphylactic reaction 28.44 26.65 32 5595 114268 110469404
COVID-19 27.94 26.65 47 5580 245013 110338659
Illness 27.59 26.65 27 5600 82144 110501528

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC R03DX11 RESPIRATORY SYSTEM
DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
OTHER SYSTEMIC DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
Other systemic drugs for obstructive airway diseases
MeSH PA D018927 Anti-Asthmatic Agents
MeSH PA D019141 Respiratory System Agents
FDA EPC N0000194010 Thymic Stromal Lymphopoietin Blocker
FDA MoA N0000194011 Thymic Stromal Lymphopoietin Blockers
CHEBI has role CHEBI:50177 dermatologic drug
CHEBI has role CHEBI:65023 anti-asthmatic agent

Related Drugs by ATC class:

R03DX Other systemic drugs for obstructive airway diseases 10 drugs
amlexanoxbenralizumabdepemokimab-ulaaeprozinolfenspiridemepolizumabomalizumabreslizumabroflumilastseratrodast

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

DiseaseRelationSNOMED_IDDOID
Severe asthma indication 370221004




🐶 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
Thymic stromal lymphopoietin Cytokine BLOCKER 10.80 DRUG LABEL DRUG LABEL

External reference:

IDSource
CHEBI:755742 CHEBI
CHEMBL3707229 ChEMBL_ID
C000622721 MESH_SUPPLEMENTAL_RECORD_UI
8933 IUPHAR_LIGAND_ID
DB15090 DRUGBANK_ID
1331983003 SNOMEDCT_US
1332043006 SNOMEDCT_US
4041094 VANDF
4041095 VANDF
C4550163 UMLSCUI
D11771 KEGG_DRUG
10172 INN_ID
354400 MMSL
40182 MMSL
d09841 MMSL
018915 NDDF
RJ1IW3B4QX UNII
2587789 RXNORM

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
TEZSPIRE HUMAN PRESCRIPTION DRUG LABEL 1 55513-100 INJECTION, SOLUTION 210 mg SUBCUTANEOUS BLA 28 sections
TEZSPIRE HUMAN PRESCRIPTION DRUG LABEL 1 55513-100 INJECTION, SOLUTION 210 mg SUBCUTANEOUS BLA 28 sections
TEZSPIRE HUMAN PRESCRIPTION DRUG LABEL 1 55513-112 INJECTION, SOLUTION 210 mg SUBCUTANEOUS BLA 28 sections
TEZSPIRE HUMAN PRESCRIPTION DRUG LABEL 1 55513-112 INJECTION, SOLUTION 210 mg SUBCUTANEOUS BLA 28 sections
TEZSPIRE HUMAN PRESCRIPTION DRUG LABEL 1 55513-123 INJECTION, SOLUTION 210 mg SUBCUTANEOUS BLA 28 sections
TEZSPIRE HUMAN PRESCRIPTION DRUG LABEL 1 55513-123 INJECTION, SOLUTION 210 mg SUBCUTANEOUS BLA 28 sections