Tezepelumab

Tezepelumab (INN; development codes MEDI9929 and AMG 157) is a human monoclonal antibody designed for the treatment of asthma[2][3] and atopic dermatitis.[4][5] It blocks thymic stromal lymphopoietin (TSLP), an epithelial cytokine that has been suggested to be critical in the initiation and persistence of airway inflammation.[6]

Tezepelumab
Structural basis for inhibition of TSLP-signaling by Tezepelumab (PDB 5J13)[1]
Monoclonal antibody
TypeWhole antibody
SourceHuman
TargetTSLP
Clinical data
Other namesMEDI9929, AMG 157
Routes of
administration
Subcutaneous injection
ATC code
  • none
Legal status
Legal status
  • Investigational
Identifiers
CAS Number
ChemSpider
  • none
UNII
KEGG
Chemical and physical data
FormulaC6400H9844N1732O1992S52
Molar mass144590.40 g·mol−1

This drug is being developed in collaboration by MedImmune, LLC and Amgen.

It is in Phase III trials as of October 2018.[7]

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

References

  1. 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. doi:10.1038/ncomms14937. PMC 5382266. PMID 28368013.
  2. 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.
  3. Matera MG, Rogliani P, Calzetta L, Cazzola M (February 2020). "TSLP Inhibitors for Asthma: Current Status and Future Prospects". Drugs. doi:10.1007/s40265-020-01273-4. PMID 32078149.
  4. "Statement On A Nonproprietary Name Adopted By The USAN Council - Tezepelumab" (PDF). American Medical Association. 30 December 2014.
  5. World Health Organization (2015). "International Nonproprietary Names for Pharmaceutical Substances (INN). Proposed INN: List 113" (PDF). WHO Drug Information. 29 (2).
  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.
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