Penn State Hershey Medical Center, Department of Medicine, Hershey, PA, USA.
Expert Opin Biol Ther. 2012 Feb;12(2):251-7. doi: 10.1517/14712598.2012.646985. Epub 2011 Dec 22.
Volociximab is a first-in-class chimeric monoclonal antibody that targets α5β1 integrin. Preclinical studies have shown the ability of volociximab to inhibit tumor neoangiogenesis by blocking the interaction between α5β1 and fibronectin. Volociximab's safety profile, pharmacokinetics and pharmacodynamics have been established. Ongoing clinical trials are evaluating its efficacy in the treatment of different types of solid tumors as a single agent or in combination with chemotherapy. In this review we focus on the biological effect of volociximab and results of completed clinical trials.
This review summarizes the structures and functions of integrin α5β1 and its ligand fibronectin, provides an overview of the early development of volociximab, a targeted monoclonal antibody that specifically binds and inhibits activation of integrin α5β1, and discusses the relevant data from pre-clinical and clinical studies.
Volociximab has been well tolerated as monotherapy or in combination with chemotherapy. It has shown promising activity in different types of cancer. Randomized trials are required to validate those early results.
Volociximab 是一种首创的嵌合单克隆抗体,靶向 α5β1 整合素。临床前研究表明,Volociximab 通过阻断 α5β1 与纤维连接蛋白的相互作用,具有抑制肿瘤新生血管生成的能力。Volociximab 的安全性特征、药代动力学和药效学已经建立。正在进行的临床试验正在评估其作为单一药物或与化疗联合治疗不同类型实体瘤的疗效。在这篇综述中,我们重点关注 Volociximab 的生物学效应和已完成的临床试验结果。
本综述总结了整合素 α5β1 及其配体纤维连接蛋白的结构和功能,概述了专门结合并抑制整合素 α5β1 激活的靶向单克隆抗体 Volociximab 的早期开发,并讨论了来自临床前和临床研究的相关数据。
Volociximab 作为单一药物或与化疗联合使用时耐受性良好。它在不同类型的癌症中表现出有希望的活性。需要随机试验来验证这些早期结果。