Etrolizumab

Etrolizumab
Monoclonal antibody
Type	Whole antibody
Source	Humanized (from rat)
Target	β7 subunit of α4β7 and αEβ7 integrin heterodimers
Clinical data
ATC code	none;
Legal status
Legal status	Investigational;
Identifiers
CAS Number	1044758-60-2 ;
IUPHAR/BPS	8407;
ChemSpider	none;
UNII	I2A72G2V3J;
KEGG	D09901 ;
Chemical and physical data
Formula	C6396H9874N1702O2010S42
Molar mass	144119.77 g·mol−1
	(what is this?)

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[]

^ Adis Insight Etrolizumab Latest Information Update: 16 Dec 2015
^ ^a ^b UK Medicines Information. etrolizumab at UKMI Page accessed May 10, 2016
^ "Genentech: Our Pipeline".
^ 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.
^ 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.
^ 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.
^ 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.
^ 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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[1] Adis Insight Etrolizumab Latest Information Update: 16 Dec 2015

[ukmi-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.

[pmid26914639-5] 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.

[pmid26630451-6] 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.

[pmid30395950-7] 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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