乌司奴单抗的发现和作用机制:一种针对白细胞介素-12 和白细胞介素-23 的人源化单克隆抗体,用于治疗免疫介导性疾病。
Discovery and mechanism of ustekinumab: a human monoclonal antibody targeting interleukin-12 and interleukin-23 for treatment of immune-mediated disorders.
机构信息
Centocor Research & Development, a division of Johnson and Johnson Pharmaceutical Research & Development, LLC, Malvern, PA, USA.
出版信息
MAbs. 2011 Nov-Dec;3(6):535-45. doi: 10.4161/mabs.3.6.17815. Epub 2011 Nov 1.
Monoclonal antibody (mAb) therapy was first established upon the approval of a mouse antibody for treatment of human acute organ rejection. However, the high incidence of immune response against the mouse mAb restricted therapeutic utility. Development of chimeric, "humanized" and human mAbs broadened therapeutic application to immune-mediated diseases requiring long-term treatment. Indeed, mAb therapeutics targeting soluble cytokines are highly effective in numerous immune-mediated disorders. A recent example is ustekinumab, a first-in-class therapeutic human immunoglobulin G1 kappa mAb that binds to the interleukins (IL)-12 and IL-23, cytokines that modulate lymphocyte function, including T-helper (Th) 1 and Th17 cell subsets. Ustekinumab was generated via recombinant human IL-12 immunization of human immunoglobulin (hu-Ig) transgenic mice. Ustekinumab binds to the p40 subunit common to IL-12 and IL-23 and prevents their interaction with the IL-12 receptor β1 subunit of the IL-12 and IL-23 receptor complexes. Ustekinumab is approved for treatment of moderate-to-severe plaque psoriasis and has demonstrated efficacy in Crohn disease and psoriatic arthritis. The clinical characterization of ustekinumab continues to clarify our understanding of human immune pathologies and may offer a novel therapeutic option for certain immune-mediated diseases.
单克隆抗体(mAb)治疗最初是在批准一种用于治疗人类急性器官排斥反应的鼠抗体的基础上建立的。然而,针对鼠 mAb 的高发生率免疫反应限制了其治疗用途。嵌合、“人源化”和人源 mAb 的开发拓宽了治疗应用范围,可用于需要长期治疗的免疫介导性疾病。事实上,针对可溶性细胞因子的 mAb 治疗在许多免疫介导性疾病中非常有效。最近的一个例子是乌司奴单抗,这是一种首创的人免疫球蛋白 G1 kappa mAb 治疗药物,可与白细胞介素(IL)-12 和 IL-23 结合,这些细胞因子调节淋巴细胞功能,包括辅助性 T 细胞(Th)1 和 Th17 细胞亚群。乌司奴单抗是通过对人免疫球蛋白(hu-Ig)转基因小鼠进行重组人 IL-12 免疫产生的。乌司奴单抗结合到 IL-12 和 IL-23 的共同 p40 亚基上,并阻止它们与 IL-12 和 IL-23 受体复合物的 IL-12 受体 β1 亚基相互作用。乌司奴单抗已被批准用于治疗中度至重度斑块状银屑病,并已证明在克罗恩病和银屑病关节炎中有效。乌司奴单抗的临床特征不断阐明我们对人类免疫病理学的理解,并可能为某些免疫介导性疾病提供新的治疗选择。