| 生物活性： |
靶点：Integrin
通路：Cytoskeleton
背景说明：是一种肠道选择性抗-β7 整合素单克隆抗体，是针对 α4β7 和 αEβ7 整合素的 β7 亚基的特异性靶向化合物。
生物活性：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 Ki 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)[1][2].
In Vitro：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[1].
In Vivo：Etrolizumab (rhuMAb Beta7; 5 mg/kg; i.v.; once; normal female BALB/c mice) decreases β7 integrins on T lymphocytes[2].
数据来源文献：[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.
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