Tenatumomab (ST2146) is a murine monoclonal antibody against tenascin-C. And tenascin-C, the large extracellular cancer. Tenatumomab has been used for Pretargeted Antibody Guided Radioimmunoresearch (PAGRIT), and delivering radionuclides to tumors via PAGRIT and direct 131Iodine labeling approach[1][2].
Tenascin-C 是一种在胚胎和成人细胞外基质中发现的六聚体糖蛋白，在恶性实体瘤和血液肿瘤中优先表达。Tenascin-C在空间和时间上与肿瘤新生血管相关，并可能发挥抗粘连和免疫抑制活性[2]。
Tenatumomab (2-5 μg/mL; 16 h) 生物素化后保持免疫反应性。并且每个单抗可以结合多达 20 个生物素，保持 50% 的免疫反应性[2]。
Tenatumomab (4 μg 每鼠; 静脉注射; 单词剂量) 在移植人 HT-29 结肠癌细胞和/或人 U-118MG 胶质母细胞瘤细胞的裸鼠中，分别显示了与低和高张力蛋白表达相关的生物分布[2]。
[1]. Giannini G, et al. Synthesis and preliminary in vitro evaluation of DOTA-Tenatumomab conjugates for theranostic applications in tenascin expressing tumors. Bioorg Med Chem. 2019 Aug 1;27(15):3248-3253.
[2]. De Santis R, et al. Low and high tenascin-expressing tumors are efficiently targeted by ST2146 monoclonal antibody. Clin Cancer Res. 2006 Apr 1;12(7 Pt 1):2191-6.