Chemistry:Etrolizumab
| Monoclonal antibody | |
|---|---|
| Type | Whole antibody |
| Source | Humanized (from rat) |
| Target | β7 subunit of α4β7 and αEβ7 integrin heterodimers |
| Clinical data | |
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| Identifiers | |
| CAS Number | |
| IUPHAR/BPS | |
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| Chemical and physical data | |
| Formula | C6396H9874N1702O2010S42 |
| Molar mass | 144119.77 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, abandoned further efforts to develop etrolizumab for ulcerative colitis, but continued development for Crohn's disease, [8] until disappointing trial results led to this being abandoned too in Feb 2022. [9]
References
- ↑ Adis Insight Etrolizumab Latest Information Update: 16 Dec 2015
- ↑ 2.0 2.1 UK Medicines Information. etrolizumab at UKMI Page accessed May 10, 2016
- ↑ "Genentech: Our Pipeline". https://www.gene.com/medical-professionals/pipeline.
- ↑ "Methods of administering beta7 integrin antagonists" WO patent 2012135589, 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. "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. November 1994. doi:10.4049/jimmunol.153.9.3847. PMID 7523506. as referenced in paragraph 146 of the PCT application.
- ↑ "Etrolizumab for ulcerative colitis: the new kid on the block?". Expert Opinion on Biological Therapy 16 (4): 567–72. 2016. doi:10.1517/14712598.2016.1158807. PMID 26914639.
- ↑ "Etrolizumab for induction of remission in ulcerative colitis". The Cochrane Database of Systematic Reviews 2015 (12): CD011661. December 2015. doi:10.1002/14651858.CD011661.pub2. PMID 26630451.
- ↑ "Etrolizumab versus infliximab in the treatment of induction phase of ulcerative colitis: A systematic review and indirect comparison". Pharmacological Research 139: 120–125. January 2019. doi:10.1016/j.phrs.2018.11.003. PMID 30395950. https://www.researchgate.net/publication/328722610.
- ↑ Tong, Amber (October 15, 2020). "Roche writes off ulcerative colitis portion of etrolizumab program, days after dissecting PhIII setback". Endpoints. https://endpts.com/roche-writes-off-ulcerative-colitis-portion-of-etrolizumab-program-days-after-dissecting-phiii-setback. Retrieved 2 January 2021.
- ↑ "Error: no
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