etrolizumab   Click here for help

GtoPdb Ligand ID: 8407

Synonyms: PRO145223 | RG-7413 | RG7413 | rhuMAb Beta7
Immunopharmacology Ligand
Compound class: Antibody
Comment: Etrolizumab is a humanized monoclonal antibody targeting integrin receptors containing the ITGB7 (β7) subunit (namely α4β7 and αEβ7).
Peptide sequence information for this antibody is available from its IMGT/mAb-DB record. Peptide sequence matches indicate that US7528236 is the covering patent [4]. The likely candidate antibody clone is that designated hu504.32R.
Etrolizumab has a slightly different mechanism of action compared to the already approved ulcerative colitis biologic vedolizumab (Entyvio®), which targets only α4β7 integrin.
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Bioactivity Comments
hu504.32R inhibits cell adhesion in assays performed as part of the patent application [4]; inhibiting α4β7-MAdCAM-1-mediated adhesion with an IC50 of 0.075nM, and αEβ7-E-cadherin-mediated adhesion with an IC50 of 3.96nM.
Selectivity at catalytic receptors
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Value Parameter Concentration range (M) Reference
integrin α4β7 Primary target of this compound Hs Inhibitor Binding 10.1 pIC50 - 4
pIC50 10.1 (IC50 7.5x10-11 M) [4]
Description: Inhibition of β7-MAdCAM-1-mediated cell adhesion.
integrin, alpha 7 subunit Hs Antibody Binding - - - 9
integrin αEβ7 Hs Antibody Inhibition - - - 9