Etrolizumab (rhuMAb Beta7) 是一种肠道选择性抗-β7 整合素单克隆抗体。Etrolizuma b是针对 α4β7 和 αEβ7 整合素的 β7 亚基的特异性靶向药物。Etrolizumab 可用于炎症性肠病 (IBD) 的研究。

Etrolizumab (rhuMAb Beta7) is a gut-selective, anti-β7 integrin monoclonal antibody. Etrolizumab is specific targeting of the β7 subunit of α4β7 and αEβ7 integrins with K i values of 18 nM and 1800 pM for Human α4β7 and Human αEβ7-293, respectively. Etrolizumab can be used in research of inflammatory bowel disease (IBD).

Liquid

α4β7 αEβ7

Etrolizumab (rhuMAb Beta7) binds the β7 subunit of both α4β7 and αEβ7 integrins with high affinity, with Kd values of 18 nM, 1800 pM, 181 pM, 116 pM, 57 pM, 31.7 pM, and 25.7 pM for Human α4β7, Human αEβ7-293, Mouse α4β7-38C13, Human α4β7-293, Rabbit PBLs, Human PBLs, and Cyno PBLs, respectively.
Etrolizumab (RPMI 8866 cells and αEβ7-293 cells) blocks the interaction of α4β7 with its cognate ligands MAdCAM-1 and VCAM-1 with IC50 values of 0.075 and 0.089 nM, respectively, and blocks the interaction between αEβ7 and its ligand E-cadherin with an IC50 value of 3.96 nM.
has not independently confirmed the accuracy of these methods. They are for reference only.

Etrolizumab (rhuMAb Beta7; 5 mg/kg; i.v.; once; normal female BALB/c mice) decreases β7 integrins on T lymphocytes.
Etrolizumab (200 μg (100 μL); i.p.; once) inhibits lymphocyte homing in the CD45RB T cell-reconstituted SCID mouse model of colitis.
has not independently confirmed the accuracy of these methods. They are for reference only.

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[1]. Tang MT, et, al. Review article: nonclinical and clinical pharmacology, pharmacokinetics and pharmacodynamics of etrolizumab, an anti-β7 integrin therapy for inflammatory bowel disease. Aliment Pharmacol Ther. 2018 Jun;47(11):1440-1452.
[2]. Stefanich EG, et, al. A humanized monoclonal antibody targeting the β7 integrin selectively blocks intestinal homing of T lymphocytes. Br J Pharmacol. 2011 Apr;162(8):1855-70.