Zaptuzumab

Zaptuzumab (AD5-10) is a DR5-specific humanized monoclonal antibody that selectively binds to DR5 with high affinity. Zaptuzumab specifically induces cancer cell death by both caspase-apoptosis and autophagic cell death (ACD). Zaptuzumab activates both ADCC and CDC. Zaptuzumab induces ROS generation and GSH level reduction. Zaptuzumab shows a significant suppression of the tumor growth and good safety in various xenografts mice tumor models^{[1][2][3][4][5]}.

References:

[1]. Zhang S, et al. A novel anti-DR5 antibody-drug conjugate possesses a high-potential therapeutic efficacy for leukemia and solid tumors. Theranostics. 2019 Jul 13;9(18):5412-5423.

[2]. Zhang S, et al. Preclinical evaluation of a novel antibody-drug conjugate targeting DR5 for lymphoblastic leukemia therapy. Mol Ther Oncolytics. 2021 Apr 29;21:329-339.

[3]. Chen L, et al. A novel humanized anti-tumor necrosis factor-related apoptosis-inducing ligand-R2 monoclonal antibody induces apoptotic and autophagic cell death. IUBMB Life. 2017 Sep;69(9):735-744.

[4]. Tang W, et al. TRAIL receptor mediates inflammatory cytokine release in an NF-kappaB-dependent manner. Cell Res. 2009 Jun;19(6):758-67.

[5]. Chen C, et al. An agonistic monoclonal antibody against DR5 induces ROS production, sustained JNK activation and Endo G release in Jurkat leukemia cells. Cell Res. 2009 Aug;19(8):984-95.

Zaptuzumab (AD5-10) 是一种针对死亡受体 5 (DR5) 的人源化的单克隆抗体，对 DR5 具有选择性的高结合亲和力。Zaptuzumab 通过 caspase 介导的凋亡 (apoptosis) 和自噬性细胞死亡 (ACD)，特异性诱导癌细胞死亡。Zaptuzumab 可以激活抗体依赖的细胞介导的细胞毒性作用 (ADCC) 和补体依赖的细胞毒性作用 (CDC)。Zaptuzumab 可以诱导活性氧 (ROS) 产生并降低 谷胱甘肽 (GSH) 水平。Zaptuzumab 在多种异种移植小鼠肿瘤模型中显示出显著的抑制肿瘤生长的作用和良好的安全性