Department of Gastroenterology, Affiliated Hospital of Nantong University, Medical School of Nantong University, Nantong 226001, Jiangsu, China.
Beijing Immunoah Pharma Tech Co., Ltd., Beijing 100141, China.
Int Immunopharmacol. 2024 Aug 20;137:112424. doi: 10.1016/j.intimp.2024.112424. Epub 2024 Jun 14.
Colorectal cancer is a major global health burden, with limited efficacy of traditional treatment modalities in improving survival rates. However, recently advances in immunotherapy has improved treatment outcomes for patients with this cancer. To address the continuing need for improved treatment efficacy, this study introduced a novel tri-specific antibody, IMT030122, that targets EpCAM, 4-1BB, and CD3. We evaluated the pharmacological efficacy and mechanism of action of IMT030122 in vitro and in vivo. In in vitro studies, IMT030122 exhibited differential binding to antigens and cells expressing EpCAM, 4-1BB, and CD3. Moreover, IMT030122 relied on EpCAM-targeted activation of intracellular CD3 and 4-1BB signaling and mediated T cell cytotoxicity specific to HCT116 colorectal cancer cells. In vivo, IMT030122 demonstrated potent anti-tumor activity, significantly inhibiting the growth of colon cancer HCT116 and MC38-hEpCAM subcutaneous grafts. Further pharmacological analysis revealed that IMT030122 recruited lymphocytes from peripheral blood into colorectal cancer tissue and exerted durable anti-tumor activity, predominantly by promoting the activation, proliferation, and differentiation of CD8T cells. Notably, IMT030122 still exhibited anti-tumor efficacy even in the presence of significantly depleted lymphocytes in colorectal cancer tissue. The potent pharmacological activity and anti-tumor effects of IMT030122 suggest it may enhance treatment efficacy and substantially extend the survival of patients with colorectal cancer in the future.
结直肠癌是全球主要的健康负担之一,传统治疗方法在提高生存率方面效果有限。然而,最近免疫疗法的进展改善了这种癌症患者的治疗结果。为了解决持续需要提高治疗效果的问题,本研究引入了一种新型三特异性抗体 IMT030122,它靶向 EpCAM、4-1BB 和 CD3。我们评估了 IMT030122 在体外和体内的药理功效和作用机制。在体外研究中,IMT030122 表现出对表达 EpCAM、4-1BB 和 CD3 的抗原和细胞的差异结合。此外,IMT030122 依赖于 EpCAM 靶向激活细胞内 CD3 和 4-1BB 信号,并介导针对 HCT116 结直肠癌细胞的 T 细胞细胞毒性。在体内,IMT030122 表现出强大的抗肿瘤活性,显著抑制结肠癌细胞 HCT116 和 MC38-hEpCAM 皮下移植物的生长。进一步的药理分析表明,IMT030122 从外周血招募淋巴细胞进入结直肠癌细胞组织,并发挥持久的抗肿瘤活性,主要通过促进 CD8T 细胞的激活、增殖和分化。值得注意的是,即使在结直肠癌细胞组织中淋巴细胞明显耗竭的情况下,IMT030122 仍表现出抗肿瘤疗效。IMT030122 的强大药理活性和抗肿瘤作用表明,它可能增强治疗效果,并在未来显著延长结直肠癌患者的生存时间。