Tezepelumab

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Tezepelumab
Structural basis for inhibition of TSLP-signaling by Tezepelumab.png
Structural basis for inhibition of TSLP-signaling by Tezepelumab (PDB 5J13)[1]
Monoclonal antibody
TypeWhole antibody
SourceHuman
Targetthymic stromal lymphopoietin (TSLP)
Clinical data
Trade namesTezspire
Other namesMEDI9929, AMG 157, tezepelumab-ekko
License data
Routes of
administration
Subcutaneous
ATC code
Legal status
Legal status
Identifiers
CAS Number
DrugBank
ChemSpider
  • None
UNII
KEGG
Chemical and physical data
FormulaC6400H9844N1732O1992S52
Molar mass144590.40 g·mol−1

Tezepelumab, sold under the brand name Tezspire, is a human monoclonal antibody used for the treatment of asthma.[4][5]

It blocks thymic stromal lymphopoietin (TSLP),[2] an epithelial cytokine that has been suggested to be critical in the initiation and persistence of airway inflammation.[6]

It was approved for medical use in the United States in December 2021.[2][3]

Medical uses

Tezepelumab is indicated for the add-on maintenance treatment of people aged twelve years and older with severe asthma.[2]

Research

In Phase III trials, tezepelumab demonstrated efficacy compared to placebo for patients with severe, uncontrolled asthma.[7][8]

Structural studies by X-ray crystallography showed that Tezepelumab competes against a critical part of the TSLPR binding site on TSLP.[1]

It is being studied for the treatment of chronic obstructive pulmonary disease, chronic rhinosinusitis with nasal polyps, chronic spontaneous urticaria and eosinophilic esophagitis (EoE).[3]

References

  1. ^ a b Verstraete K, Peelman F, Braun H, Lopez J, Van Rompaey D, Dansercoer A, et al. (April 2017). "Structure and antagonism of the receptor complex mediated by human TSLP in allergy and asthma". Nature Communications. 8 (1): 14937. Bibcode:2017NatCo...814937V. doi:10.1038/ncomms14937. PMC 5382266. PMID 28368013.
  2. ^ a b c d "Tezspire- tezepelumab-ekko injection, solution". DailyMed. Retrieved 24 December 2021.
  3. ^ a b c "Tezspire (tezepelumab) approved in the US for severe asthma". AstraZeneca (Press release). 17 December 2021. Retrieved 17 December 2021.
  4. ^ Marone G, Spadaro G, Braile M, Poto R, Criscuolo G, Pahima H, et al. (November 2019). "Tezepelumab: a novel biological therapy for the treatment of severe uncontrolled asthma". Expert Opinion on Investigational Drugs. 28 (11): 931–940. doi:10.1080/13543784.2019.1672657. PMID 31549891. S2CID 202746054.
  5. ^ Matera MG, Rogliani P, Calzetta L, Cazzola M (February 2020). "TSLP Inhibitors for Asthma: Current Status and Future Prospects". Drugs. 80 (5): 449–458. doi:10.1007/s40265-020-01273-4. PMID 32078149. S2CID 211194472.
  6. ^ "Tezepelumab granted Breakthrough Therapy Designation by US FDA". AstraZeneca (Press release). 7 September 2018.
  7. ^ "Studies found for: Tezepelumab". ClinicalTrials.Gov. National Library of Medicine, National Institutes of Health, U.S. Department of Health and Human Services.
  8. ^ Menzies-Gow A, Corren J, Bourdin A, Chupp G, Israel E, Wechsler ME, et al. (May 2021). "Tezepelumab in Adults and Adolescents with Severe, Uncontrolled Asthma". New England Journal of Medicine. 384 (19): 1800–09. doi:10.1056/NEJMoa2034975. PMID 33979488. S2CID 234484931.

External links

  • "Tezepelumab". Drug Information Portal. U.S. National Library of Medicine.
  • Clinical trial number NCT02054130 for "Study to Evaluate the Efficacy and Safety of MEDI9929 (AMG 157) in Adult Subjects With Inadequately Controlled, Severe Asthma" at ClinicalTrials.gov
  • Clinical trial number NCT03347279 for "Study to Evaluate Tezepelumab in Adults & Adolescents With Severe Uncontrolled Asthma (NAVIGATOR)" at ClinicalTrials.gov