Natalizumab是一种重组的人源化单克隆抗体，与α4β1-整联蛋白(α4β1-integrin)结合并阻断其与血管细胞粘附分子1(VCAM-1)的相互作用。Natalizumab可用于复发缓解型多发性硬化症和克罗恩氏病的研究。Natalizumab也可阻止淋巴细胞进入中枢神经系统，从而防止急性脱髓鞘复发。
Natalizumab is a recombinant, humanized monoclonal antibody, binds to α4β1-integrin and blocks its interaction with vascular cell adhesion molecule-1 (VCAM-1). Natalizumab can be used for the treatment of relapsing remitting multiple sclerosis and Crohn's disease. Natalizumab is also the first targeted therapy which blocks an essential mechanism for lymphocyte entry to the CNS and thus prevents acute demyelinating relapses[1].
Natalizumab, a recombinant, humanized antibody, binds to α4β1-integrin and blocks its interaction with VCAM-1. As a result, leukocyte migration into brain tissue is inhibited, reducing inflammation and preventing the formation of lesions. Natalizumab may also inhibit ongoing central nervous system (CNS) inflammation, mediated by leukocytes already present in the CNS, by interrupting the interactions between α4-integrin-expressing leukocytes and extracellular matrix proteins such as fibronectin and osteopontin[1].
Natalizumab binds rapidly and with high affinity to α4-integrin. Maximal binding (≥80% saturation), measured in vitro on isolated lymphocyte membranes, occurred 24 hours after intravenous (IV) doses of natalizumab 1 mg/kg to 6 mg/kg[1].
[1]. Hutchinson M. Natalizumab: A new treatment for relapsing remitting multiple sclerosis. Ther Clin Risk Manag. 2007 Jun;3(2):259-68.
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