tezepelumab 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
human origin	5500	1572943-04-4

Description:

Molecule	Description
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

Molecule

Description

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:

None

ADMET properties:

None

Approvals:

Date	Agency	Company
Sept. 19, 2022	EMA	ASTRAZENECA AB
Dec. 17, 2021	FDA	ASTRAZENECA AB
Sept. 26, 2022	PMDA	ASTRAZENECA K.K

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Arthralgia	54.52	41.58	50	766	569660	62918546
Anaphylactic reaction	47.46	41.58	21	795	66079	63422127

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Arthralgia	59.12	40.56	41	525	571762	79172060

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	R03DX11	RESPIRATORY SYSTEM DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES OTHER SYSTEMIC DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES Other systemic drugs for obstructive airway diseases
FDA EPC	N0000194010	Thymic Stromal Lymphopoietin Blocker
FDA MoA	N0000194011	Thymic Stromal Lymphopoietin Blockers

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

Disease	Relation	SNOMED_ID	DOID
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:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Thymic stromal lymphopoietin	Cytokine	Q969D9	TSLP_HUMAN	BLOCKER		10.80		DRUG LABEL	DRUG LABEL

External reference:

ID	Source
CHEMBL3707229	ChEMBL_ID
C000622721	MESH_SUPPLEMENTAL_RECORD_UI
8933	IUPHAR_LIGAND_ID
DB15090	DRUGBANK_ID
018915	NDDF
4041094	VANDF
4041095	VANDF
D11771	KEGG_DRUG
C4550163	UMLSCUI
CHEMBL2109595	ChEMBL_ID
10172	INN_ID
2587789	RXNORM
354400	MMSL
40182	MMSL
d09841	MMSL
RJ1IW3B4QX	UNII

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
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	55513-100	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	55513-112	INJECTION, SOLUTION	210 mg	SUBCUTANEOUS	BLA	28 sections
TEZSPIRE	HUMAN PRESCRIPTION DRUG LABEL	1	55513-123	INJECTION, SOLUTION	210 mg	SUBCUTANEOUS	BLA	28 sections