Vedolizumab Monoclonal Antibody for Ulcerative Colitis

English name：Vedolizumab
CAS number：943609-66-3
molecular formula
Molecular weight: 0
EINECS No
Related categories: drug substance; mAb 22; control substance; chemical reagent
The Mol file,:Mol File
constitutional formula:

Vydozumab properties
Storage conditions: Store at-80 C
Solubility: dissolved in dimethyl sulfoxide
Form: solid
Color: white to off-white
 

Monoclonal antibody

Vedozumab (vedolizumab) is a fully humanized monoclonal antibody that specifically antagonizes α 4 β 7 integrin and inhibits the binding of α 4 β 7 integrin to the intestinal mucosal cell adhesion molecule MAdCAM-1.

In May 2014, the US FDA approved vedocizumab for the treatment of adults with moderate to severe active ulcerative colitis (UC) or Crohn'sdisease (CD) who do not tolerate or no longer respond to a TNF- α antagonist or Chemicalbook.

Bioactivity

Vedolizumab Is a humanized monoclonal antibody targeting α 4 β 7 integral protein (integrin) for ulcerative colitis and Crohn's disease.

Target spot

Integrin

In vitro study 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.

In vivo research

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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MSDS information

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