生物活性

奥马珠单抗Omalizumab is a recombinant DNA-derived humanized IgG1k monoclonal antibody that specifically binds to free human immunoglobulin E (IgE) in the blood ａnd interstitial fluid ａnd to membrane-bound form of IgE (mIgE) on the surface of mIgE-expressing B lymphocytes. Omalizumab inhibits the binding of IgE to FcεRI on mast cells ａnd basophils by binding to an antigenic epie on IgE that overlaps with the site to which FcεRI binds. When IgE is bound to the receptor, the antigenic epie on IgE to which omalizumab binds is sterically hindered by the receptor ａnd is not accessible to omalizumab binding, thus averting the anaphylactic effects presumably unavoidable with an ordinary anti-IgE antibody . Furthermore, although the peptide elements on IgE involved in binding to low affinity IgE receptor (FcεRII) on many cell types are different from the peptide elements involved in binding to FcεRI, omalizumab, by steric hindrance, also prevents binding of IgE to FcεRII.

化学性质

储备液配制

*下述溶液配置方法仅为基于分子量计算出的理论值。不同产品在配置溶液，需考虑其在不同溶剂中的溶解度限制。

不同实验动物依据体表面积的等效剂量转换表（参考来源于公开文献）

例如，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。

参考文献

[1] Chang TW, et al. Adv Immunol. Anti-IgE antibodies for the treatment of IgE-mediated allergic diseases.

[2] Schulman ES. Am J Respir Crit Care Med. Development of a monoclonal anti-immunoglobulin E antibody (omalizumab) for the treatment of allergic respiratory disorders.