Etrolizumab

Etrolizumab
Monoclonal antibody
TypeWhole antibody
SourceHumanized (from rat)
Targetβ7 subunit of α4β7 and αEβ7 integrin heterodimers
Clinical data
ATC code
  • none
Legal status
Legal status
  • Investigational
Identifiers
CAS Number
IUPHAR/BPS
ChemSpider
  • none
UNII
KEGG
Chemical and physical data
FormulaC6396H9874N1702O2010S42
Molar mass144119.77 g·mol−1
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Etrolizumab (rhuMAb Beta7) is a biopharmaceutical drug candidate being developed for the treatment of ulcerative colitis and Crohn's disease. It is a humanized monoclonal antibody against the β7 subunit of integrins α4β7 and αEβ7.[1] Etrolizumab was developed by Genentech[2][3] by engineering the FIB504 antibody to include human IgGl-heavy chain and κ-light chain frameworks; it is manufactured in CHO cells.[4]

As of 2016 it was in phase III studies for induction and maintenance therapy in people with ulcerative colitis and Crohn's.[2][5][6] According to data of one meta-analysis efficacy of Etrolizumab is comparable with conventional therapies such as Infliximab with less adverse events [7]

Phase III clinical trials produced mixed results; and, on October 14, 2020, Hoffmann-La Roche, the parent company of Genentech, announced that it had abandoned further efforts to develop etrolizumab for ulcerative colitis, but continues development for Crohn's disease.[8]

References

  1. ↑ Adis Insight Etrolizumab Latest Information Update: 16 Dec 2015
  2. 1 2 UK Medicines Information. etrolizumab at UKMI Page accessed May 10, 2016
  3. ↑ "Genentech: Our Pipeline".
  4. ↑ WO 2012135589, "Methods of administering beta7 integrin antagonists", assigned to Genentech and Roche For the FIB504 mAb, see Andrew DP et al. Distinct but overlapping epitopes are involved in alpha 4 beta 7-mediated adhesion to vascular cell adhesion molecule-1, mucosal addressin-1, fibronectin, and lymphocyte aggregation. Andrew DP, Berlin C, Honda S, Yoshino T, Hamann A, Holzmann B, Kilshaw PJ, Butcher EC (November 1994). "Distinct but overlapping epitopes are involved in alpha 4 beta 7-mediated adhesion to vascular cell adhesion molecule-1, mucosal addressin-1, fibronectin, and lymphocyte aggregation". Journal of Immunology. 153 (9): 3847–61. PMID 7523506. as referenced in paragraph 146 of the PCT application.
  5. ↑ Makker J, Hommes DW (2016). "Etrolizumab for ulcerative colitis: the new kid on the block?". Expert Opinion on Biological Therapy. 16 (4): 567–72. doi:10.1517/14712598.2016.1158807. PMID 26914639. S2CID 24706213.
  6. ↑ Rosenfeld G, Parker CE, MacDonald JK, Bressler B (December 2015). "Etrolizumab for induction of remission in ulcerative colitis". The Cochrane Database of Systematic Reviews. 2015 (12): CD011661. doi:10.1002/14651858.CD011661.pub2. PMC 8612697. PMID 26630451.
  7. ↑ Motaghi E, Ghasemi-Pirbaluti M, Zabihi M (January 2019). "Etrolizumab versus infliximab in the treatment of induction phase of ulcerative colitis: A systematic review and indirect comparison". Pharmacological Research. 139: 120–125. doi:10.1016/j.phrs.2018.11.003. PMID 30395950. S2CID 53235342.
  8. ↑ Tong, Amber (October 15, 2020). "Roche writes off ulcerative colitis portion of etrolizumab program, days after dissecting PhIII setback". Endpoints. Retrieved 2 January 2021.


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