Fan Wenlu, Chen Yonglu, Zhou Zhenxing, Duan Wenwen, Yang Chengcheng, Sheng Shimei, Wang Yongwei, Wei Xinru, Liu Ying, Huang Yanshan
Department of Biochemistry, and Department of Cardiology of the Second Affiliated Hospital, Zhejiang University School of Medicine, Hangzhou, China; Department of Innovative Drug Discovery and Development, Zhejiang Doer Biologics Co., Ltd., Hangzhou, China.
Department of Innovative Drug Discovery and Development, Zhejiang Doer Biologics Co., Ltd., Hangzhou, China.
Int Immunopharmacol. 2024 Mar 30;130:111698. doi: 10.1016/j.intimp.2024.111698. Epub 2024 Feb 20.
Immunosuppressive pathways in the tumor microenvironment (TME) are inextricably linked to tumor progression. Mono-therapeutics of immune checkpoint inhibitors (ICIs, e.g. antibodies against programmed cell death protein-1/programmed cell death ligand-1, PD-1/PD-L1) is prone to immune escape while combination therapeutics tends to cause high toxicity and side effects. Therefore, using multi-functional molecules to target multiple pathways simultaneously is becoming a new strategy for cancer therapies. Here, we developed a trifunctional fusion protein, DR30206, composed of Bevacizumab (an antibody against VEGF), and a variable domain of heavy chain of heavy chain antibody (VHH) against PD-L1 and the extracellular domain (ECD) protein of TGF-β receptor II (TGF-β RII), which are fused to the N- and C-terminus of Bevacizumab, respectively. The original intention of DR30206 design was to enhance the immune responses pairs by targeting PD-L1 while inhibiting VEGF and TGF-β in the TME. Our data demonstrated that DR30206 exhibits high antigen-binding affinities and efficient blocking capabilities, the principal drivers of efficacy in antibody therapy. Furthermore, the capability of eliciting antibody-dependent cellular cytotoxicity (ADCC) and mixed lymphocyte reaction (MLR) provides a greater possibility to enhance the immune response. Finally, in vivo experiments showed that the antitumor activity of DR30206 was superior to those of monoclonal antibody of PD-L1 or VEGF, PD-L1 and TGF-β bispecific antibody or the combination inhibition of PD-L1 and VEGF. Our findings suggest there is a great potential for DR30206 to become a therapeutic for the treatment of multiple cancer types, especially lung cancer, colon adenocarcinoma and breast carcinoma.
肿瘤微环境(TME)中的免疫抑制途径与肿瘤进展有着千丝万缕的联系。免疫检查点抑制剂(ICIs,例如抗程序性细胞死亡蛋白1/程序性细胞死亡配体1的抗体,PD-1/PD-L1)单药治疗容易出现免疫逃逸,而联合治疗则往往会导致高毒性和副作用。因此,使用多功能分子同时靶向多种途径正成为癌症治疗的新策略。在此,我们开发了一种三功能融合蛋白DR30206,它由贝伐单抗(一种抗VEGF的抗体)、抗PD-L1的重链抗体可变区(VHH)以及转化生长因子β受体II(TGF-β RII)的细胞外结构域(ECD)蛋白组成,分别融合于贝伐单抗的N端和C端。设计DR30206的初衷是通过靶向PD-L1同时抑制TME中的VEGF和TGF-β来增强免疫反应。我们的数据表明,DR30206具有高抗原结合亲和力和高效阻断能力,这是抗体治疗疗效的主要驱动因素。此外,引发抗体依赖性细胞毒性(ADCC)和混合淋巴细胞反应(MLR)的能力为增强免疫反应提供了更大的可能性。最后,体内实验表明,DR30206的抗肿瘤活性优于PD-L1或VEGF单克隆抗体、PD-L1和TGF-β双特异性抗体或PD-L1与VEGF联合抑制。我们的研究结果表明,DR30206有很大潜力成为治疗多种癌症类型的药物,尤其是肺癌、结肠腺癌和乳腺癌。