Enavatuzumab (PDL192; ABT-361) 是一种人源化 IgG1 单克隆抗体，靶向 TNF 样细胞凋亡弱诱导剂受体 (TWEAK)。TWEAK (Fn14; TNFRSF12A) 是 TWEAK 受体 (TweakR) 的天然配体，可刺激多种细胞反应。Enavatuzumab 通过直接的 TweakR 信号和抗体依赖性细胞介导的细胞毒性 (ADCC) 诱导肿瘤生长抑制。Enavatuzumab 可以主动募集和激活骨髓效应细胞来杀死肿瘤细胞。Enavatuzumab 在体外和体内抑制各种人类 TweakR 阳性癌细胞系和异种移植物的生长。

Enavatuzumab (PDL192; ABT-361) is a humanized IgG1 monoclonal antibody targeting the receptor of TNF-like weak inducer of apoptosis (TWEAK). TWEAK (Fn14; TNFRSF12A), the natural ligand of the TWEAK receptor (TweakR), stimulates multiple cellular responses. Enavatuzumab induces tumor growth inhibition through direct TweakR signaling and antibody dependent cell-mediated cytotoxicity (ADCC). Enavatuzumab can actively recruits and activates myeloid effectors to kill tumor cells. Enavatuzumab inhibits the growth of various human TweakR-positive cancer cell lines and xenografts in vitro and in vivo .

Enavatuzumab (0.1-1000 ng/mL; 4 小时) 在体外诱导效应细胞活化和肿瘤细胞杀伤。
Enavatuzumab (10μg/mL; 24 小时) 导致免疫效应细胞向 SN12C 和 A375 肿瘤细胞的迁移显着增加。
has not independently confirmed the accuracy of these methods. They are for reference only.Cell Viability Assay

Enavatuzumab (10mg/kg; 腹腔注射; 每周 3 次; 6, 7 或者 9 剂) 对不同的异种移植肿瘤表现出不同的抗肿瘤活性。
has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: 6-week old SCID mice with SN12C or HCT116 or DLD-1 or A37

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[1]. Shiming Ye, et al. Enavatuzumab, a Humanized Anti-TWEAK Receptor Monoclonal Antibody, Exerts Antitumor Activity through Attracting and Activating Innate Immune Effector Cells. J Immunol Res. 2017;2017:5737159.
[2]. Ludmilla de Plater, et al. Predictive gene signature of response to the anti-TweakR mAb PDL192 in patient-derived breast cancer xenografts. PLoS One. 2014 Nov 6;9(11):e104227.