Ganguly Bishu, Balasa Balaji, Efros Lyubov, Hinton Paul R, Hartman Stephen, Thakur Archana, Xiong Joanna M, Schmidt Brian, Robinson Randy R, Sornasse Thierry, Vexler Vladimir, Sheridan James P
a Department Translational Medicine , AbbVie Biotherapeutics , Redwood City , CA , USA.
b Department Discovery Sciences , AbbVie Biotherapeutics , Redwood City , CA , USA.
MAbs. 2016 Oct;8(7):1417-1424. doi: 10.1080/19420862.2016.1207031. Epub 2016 Jul 1.
The CD25-binding antibody daclizumab high-yield process (DAC HYP) is an interleukin (IL)-2 signal modulating antibody that shares primary amino acid sequence and CD25 binding affinity with Zenapax®, a distinct form of daclizumab, which was approved for the prevention of acute organ rejection in patients receiving renal transplants as part of an immunosuppressive regimen that includes cyclosporine and corticosteroids. Comparison of the physicochemical properties of the two antibody forms revealed the glycosylation profile of DAC HYP differs from Zenapax in both glycan distribution and the types of oligosaccharides, most notably high-mannose, galactosylated and galactose-α-1,3-galactose (α-Gal) oligosaccharides, resulting in a DAC HYP antibody material that is structurally distinct from Zenapax. Although neither antibody elicited complement-dependent cytotoxicity in vitro, DAC HYP antibody had significantly reduced levels of antibody-dependent cell-mediated cytotoxicity (ADCC). The ADCC activity required natural killer (NK) cells, but not monocytes, suggesting the effects were mediated through binding to Fc-gamma RIII (CD16). Incubation of each antibody with peripheral blood mononuclear cells also caused the down-modulation of CD16 expression on NK cells and the CD16 down-modulation was greater for Zenapax in comparison to that observed for DAC HYP. The substantive glycosylation differences between the two antibody forms and corresponding greater Fc-mediated effector activities by Zenapax, including cell killing activity, manifest as a difference in the biological function and pharmacology between DAC HYP and Zenapax.
CD25结合抗体达克珠单抗高产工艺(DAC HYP)是一种白细胞介素(IL)-2信号调节抗体,与泽帕妥(Zenapax®)具有相同的一级氨基酸序列和CD25结合亲和力,泽帕妥是达克珠单抗的一种不同形式,已被批准用于预防接受肾移植患者的急性器官排斥反应,作为包括环孢素和皮质类固醇的免疫抑制方案的一部分。两种抗体形式的物理化学性质比较显示,DAC HYP的糖基化谱在聚糖分布和寡糖类型方面与泽帕妥不同,最显著的是高甘露糖、半乳糖基化和半乳糖-α-1,3-半乳糖(α-Gal)寡糖,导致DAC HYP抗体材料在结构上与泽帕妥不同。虽然两种抗体在体外均未引发补体依赖性细胞毒性,但DAC HYP抗体的抗体依赖性细胞介导的细胞毒性(ADCC)水平显著降低。ADCC活性需要自然杀伤(NK)细胞,但不需要单核细胞,这表明其作用是通过与Fc-γRIII(CD16)结合介导的。将每种抗体与外周血单核细胞孵育也会导致NK细胞上CD16表达的下调,与DAC HYP相比,泽帕妥的CD16下调程度更大。两种抗体形式之间的实质性糖基化差异以及泽帕妥相应更强的Fc介导的效应活性,包括细胞杀伤活性,表现为DAC HYP和泽帕妥在生物学功能和药理学上的差异。