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新型生物工程化单克隆抗体 ON203 针对氧化型巨噬细胞移动抑制因子的临床前评估,作为一种抗癌治疗药物。

Preclinical Evaluation of ON203, A Novel Bioengineered mAb Targeting Oxidized Macrophage Migration Inhibitory Factor as an Anticancer Therapeutic.

机构信息

OncoOne Research & Development GmbH, Vienna, Austria.

出版信息

Mol Cancer Ther. 2023 May 4;22(5):555-569. doi: 10.1158/1535-7163.MCT-22-0676.

Abstract

High levels of macrophage migration inhibitory factor (MIF) in patients with cancer are associated with poor prognosis. Its redox-dependent conformational isoform, termed oxidized MIF (oxMIF), is a promising tumor target due to its selective occurrence in tumor lesions and at inflammatory sites. A first-generation anti-oxMIF mAb, imalumab, was investigated in clinical trials in patients with advanced solid tumors, where it was well tolerated and showed signs of efficacy. However, imalumab has a short half-life in humans, increased aggregation propensity, and an unfavorable pharmacokinetic profile. Here, we aimed to optimize imalumab by improving its physicochemical characteristics and boosting its effector functions. Point mutations introduced into the variable regions reduced hydrophobicity and the antibodies' aggregation potential, and increased plasma half-life and tumor accumulation in vivo, while retaining affinity and specificity to oxMIF. The introduction of mutations into the Fc region known to increase antibody-dependent cellular cytotoxicity resulted in enhanced effector functions of the novel antibodies in vitro, whereas reduced cytokine release from human peripheral blood mononuclear cells in the absence of target antigen by the engineered anti-oxMIF mAb ON203 versus imalumab reveals a favorable in vitro safety profile. In vivo, ON203 mAb demonstrated superior efficacy over imalumab in both prophylactic and established prostate cancer (PC3) mouse xenograft models. In summary, our data highlight the potential of the second-generation anti-oxMIF mAb ON203 as a promising immunotherapy for patients with solid tumors, warranting clinical evaluation.

摘要

高水平的巨噬细胞移动抑制因子(MIF)在癌症患者中与预后不良有关。其氧化依赖的构象同工型,称为氧化 MIF(oxMIF),由于其在肿瘤病变和炎症部位的选择性发生,是一个很有前途的肿瘤靶点。第一代抗 oxMIF mAb,imalumab,在晚期实体瘤患者的临床试验中进行了研究,结果显示其具有良好的耐受性,并显示出一定的疗效。然而,imalumab 在人体内的半衰期短,聚集倾向增加,药代动力学特性不理想。在这里,我们旨在通过改善 imalumab 的理化特性和增强其效应功能来对其进行优化。引入可变区的点突变降低了抗体的疏水性和聚集倾向,增加了其在体内的血浆半衰期和肿瘤蓄积,同时保留了对 oxMIF 的亲和力和特异性。在已知能增加抗体依赖性细胞毒性的 Fc 区引入突变,导致新型抗体在体外的效应功能增强,而与 imalumab 相比,工程化的抗 oxMIF mAb ON203 在没有靶抗原的情况下,从人外周血单核细胞中释放细胞因子减少,揭示了其有利的体外安全性特征。在体内,ON203 mAb 在预防和已建立的前列腺癌(PC3)小鼠异种移植模型中均表现出优于 imalumab 的疗效。总之,我们的数据强调了第二代抗 oxMIF mAb ON203 作为一种有前途的免疫疗法,用于治疗实体瘤患者的潜力,值得临床评估。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fea5/10157364/860a0a48abbe/overview_graphic_mct-22-0676.jpg

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