Nimotuzumab 是一种靶向 EGFR 的人源化 IgG1 单克隆抗体，KD 为 0.21 nM。Nimotuzumab 针对 EGFR 的细胞外结构域，阻断与其配体的结合。Nimotuzumab 是一种强抗肿瘤药物，通过其引起抗体依赖性细胞介导的细胞毒性 (ADCC) 和补体依赖性细胞毒性(CDC) 的能力，对靶肿瘤具有溶细胞作用。
Nimotuzumab is a humanized IgG1 monoclonal antibody targeting EGFR with a KD of 0.21 nM. Nimotuzumab is directed against the extracellular domain of the EGFR blocking the binding to its ligands. Nimotuzumab, a strong antitumor drug, is cytolytic on target tumors by its capacity to cause antibody dependent cell mediated cytotoxicity (ADCC) and complement dependent cytotoxicity (CDC)[1][2].
Nimotuzumab (10 μg/mL; 24 hours) induces significant downregulation of CD16 on NK cells[1]. Nimotuzumab (10 μg/mL; 48 hours) induces the upregulation of PD-L1 molecule on DCs when co-cultured with the NK: DC: HNSCC cells[1]. The intrinsic properties of Nimotuzumab requires bivalent binding (i.e., binding with both antibody arms to two targets simultaneously) for stable attachment to cellular surface, which leads to Nimotuzumab selectively binding to cells that express moderate to high EGFR levels[2].
[1]. Zaima Mazorra, et al. Nimotuzumab Induces NK Cell Activation, Cytotoxicity, Dendritic Cell Maturation and Expansion of EGFR-Specific T Cells in Head and Neck Cancer Patients. Front Pharmacol. 2017 Jun 19;8:382.
[2]. Melarkode S Ramakrishnan, et al. Nimotuzumab, a promising therapeutic monoclonal for treatment of tumors of epithelial origin. MAbs. Jan-Feb 2009;1(1):41-8.
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