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维多珠单抗

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维多珠单抗

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CAS No. 943609-66-3

分子式 -

分子量 -

英文名称 Vedolizumab

中文同义词维多珠单抗;VEDOLIZUMAB ( 维多组单抗 );维多组单抗

基本信息

产品名称

维多珠单抗

中文同义词

维多珠单抗,VEDOLIZUMAB ( 维多组单抗 ),维多组单抗

英文名称

Vedolizumab

英文同义词

Vedolizumab;Vedolizumab USP/EP/BP;Research Grade Vedolizumab(DHC98802);Vedolizumab (anti-α4β7-integrin)

CAS No.

943609-66-3

分子式

分子量

EINECS号

MDL NO.

性质

形态

固体

颜色

白色至米白色

溶解度

溶于二甲基亚砜

储存条件

Store at -80°C

用途

靶点

Integrin

体内研究

Blockade of α4β7 receptors on T-lymphocytes has been shown to occur for several weeks after a single dose of vedolizumab. The drug concentration following the infusion has been shown to be dose related with a mean maximum concentration of 12.5 μg/mL in those receiving 0.5 mg/kg of vedolizumab and 52.0 μg/mL in those receiving 2 mg/kg. The serum half-life of these two doses is 9-12 days respectively and saturation of α4β7 receptors on T-lymphocytes is >90% at both 4-6 weeks following infusion. In a dose ranging study, the serum drug concentrations increase with increasing dose and when regular induction infusions are used (on day 1, 15, 29 and 85), the serum half-life is between 15 and 22 days across all groups.

体外研究

Vedolizumab does not bind to the majority of memory CD4+ T lymphocytes (60%), neutrophils, and most monocytes. The highest level of vedolizumab binding is to a subset (25%) of human peripheral blood memory CD4+ T lymphocytes that include gut-homing interleukin 17 T-helper lymphocytes. Vedolizumab also binds to eosinophils at high levels, and to naive T-helper lymphocytes, naive and memory cytotoxic T lymphocytes, B lymphocytes, natural killer cells, and basophils at lower levels; vedolizumab binds to memory CD4+ T and B lymphocytes with subnanomolar potency (EC 50 =0.3-0.4 nM). Vedolizumab selectively inhibits adhesion of α4β7-expressing cells to mucosal addressin cell adhesion molecule 1 (IC 50 =0.02-0.06 g/mL) and fibronectin (IC 50 =0.02 g/mL), but not vascular cell adhesion molecule 1.

生物活性

Vedolizumab是一种靶向α4β7整联蛋白 (integrin) 的人源化单克隆抗体，用于溃疡性结肠炎和克罗恩病的相关研究。

单克隆抗体

维多珠单抗（vedolizumab）是一种全人源化单克隆抗体，特异性拮抗α4β7整合素，抑制α4β7整合素对肠道黏膜细胞粘附分子MAdCAM-1的结合。2014年5月，美国FDA批准维多珠单抗上市，用于对常规疗法或一种TNF-α拮抗剂不耐受、或不再响应、或响应不足的中度至重度活动性溃疡性结肠炎（UC）或克罗恩病（Crohn's disease，CD）成人患者的治疗。

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