Etaracizumab Overview

Introduction of Etaracizumab

Etaracizumab, also known as MEDI-522, is a humanized monoclonal IgG1 antibody that targets alpha v beta 3 integrin (αVβ3 integrin), which is a receptor of vitronectin. This drug was developed by MedImmune and has been used for the clinical trials studying the treatment of psoriasis, renal cell carcinoma, stage IV renal cell cancer, recurrent renal cell cancer, and stage III renal cell cancer.

Actually, studies of etaracizumab were conducted as early as 2006. A study to evaluate the effects of etaracizumab of direct targeting of tumor cells found high-dose administration of etaracizumab can actively impair the antitumor activity. Results have shown that the inhibition of etaracizumab on tumor growth of αvβ3-expressing tumor cells was in a dose-dependent manner, further supporting the concept that etaracizumab could be used to therapy tumor cancer via targeting αvβ3 integrin. Then, a phase I study of etaracizumab in patients with advanced solid tumors was conducted to assess the safety, immunogenicity, and pharmacokinetics. The result showed that etaracizumab was well-tolerated at doses up to 6 mg/kg with no evidence of immunogenicity. A randomized phase 2 study of etaracizumab to assess its safety and antitumor efficacy in combination with dacarbazine in patients with stage IV metastatic melanoma. The conclusion of the experiment is that the combined use of drugs is not more effective than the single use of drugs. A study to evaluate the characteristics of etaracizumab in vivo and in vitro, and whether the expression of αvβ3 integrin in tumor cells could be imaged with (111)In-labeled etaracizumab was conducted in 2011, with the conclusion that (111)In-DOTA-Abegrin might be used to evaluate tumor angiogenic status and monitor the therapeutic efficacy of Abegrin-based cancer therapy.

Mechanism of Action of Etaracizumab

Etaracizumab is a protein-based drug binding to αVβ3 integrin, which is important for endothelial cell proliferation, maturation, and survival. The αVβ3 integrin is a member of integrins, which is a family of transmembrane proteins that exist as heterodimers consisting of noncovalently linked alpha and beta subunits. Integrins are found to involve in diverse processes including cell adhesion, signal transduction, cell migration, and differentiation. Integrins play important roles in the adhesion of stimulated endothelial cells to the extracellular matrix (ECM), the ECM-rearranging proteases and the signal transduction of survival and differentiation of cells in newly formed vasculature. Among all the integrins, αVβ3 seems to be the most important one during tumor angiogenesis. The αVβ3 integrin is a cell adhesion and signaling receptor that is highly expressed on the surface of tumor vessel endothelial cells, new-born vessels as well as some tumor cells, but is not present in resting endothelial cells and most normal organ systems, making it a suitable target for anti-angiogenic therapy. Inhibitors of integrin αVβ3 like antibodies, peptides, peptidomimetics, and other antagonists are considered as great potential therapeutic drugs in the treatment of cancer. Etaracizumab is one of the antagonists of αVβ3 and acts as a type of antiangiogenesis agent or a type of metastasis inhibitor. Upon administration, etaracizumab binds to a protein on the surface of blood vessels and blocks the binding of αVβ3 integrin and its ligands，preventing the growth of new blood vessels and resulting in inhibition of angiogenesis and metastasis.

Fig.1 Mechanism of action of Etaracizumab

What We Provide

Therapeutic Antibody

Etaracizumab

We provide high-quality Etaracizumab for use in WB, FC, IP, ELISA, Neut, FuncS, IF and most other immunological methods. For lab research use only, not for diagnostic, therapeutic or any in vivo human use.

For research use only. Not intended for any clinical use.