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943609-66-3

中文名稱 維多珠單抗
英文名稱 Vedolizumab
CAS 943609-66-3
更新日期 2024/12/20 13:38:27
943609-66-3 結(jié)構(gòu)式 943609-66-3 結(jié)構(gòu)式

基本信息

中文別名
維多珠單抗
維多組單抗
VEDOLIZUMAB ( 維多組單抗 )
英文別名
Vedolizumab
Vedolizumab USP/EP/BP
所屬類別
原料藥:其它消化系統(tǒng)用藥

物理化學(xué)性質(zhì)

儲(chǔ)存條件Store at -80°C
溶解度溶于二甲基亞砜
形態(tài)Solid
顏色White to off-white

常見問題列表

單克隆抗體

維多珠單抗(vedolizumab)是一種全人源化單克隆抗體,特異性拮抗α4β7整合素,抑制α4β7整合素對(duì)腸道黏膜細(xì)胞粘附分子MAdCAM-1的結(jié)合。

2014年5月,美國(guó)FDA批準(zhǔn)維多珠單抗上市,用于對(duì)常規(guī)療法或一種TNF-α拮抗劑不耐受、或不再響應(yīng)、或響應(yīng)不足的中度至重度活動(dòng)性潰瘍性結(jié)腸炎(UC)或克羅恩?。–rohn's disease,CD)成人患者的治療。

生物活性
Vedolizumab是一種靶向α4β7整聯(lián)蛋白 (integrin) 的人源化單克隆抗體,用于潰瘍性結(jié)腸炎和克羅恩病的相關(guān)研究。
靶點(diǎn)

Integrin

體外研究

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.

體內(nèi)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.

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