Research Division, Chugai Pharmaceutical Co., Ltd., Shizuoka, Japan.
Covance Preclinical Services GmbH, Muenster, Germany.
Birth Defects Res. 2017 Jul 3;109(11):843-856. doi: 10.1002/bdr2.1036. Epub 2017 May 15.
SA237 is a humanized anti-interleukin-6 receptor (IL-6R) monoclonal antibody in which the constant and variable regions have been engineered for a longer plasma half-life. According to literature, blocking of IL-6 related functions could have an influence on pregnancy sustainment, development of the immune system, and brain growth.
SA237 effects on dams, embryo-fetal development, parturition and postnatal development were investigated in an enhanced pre- and postnatal development study, in which SA237 was subcutaneously administered to pregnant cynomolgus monkeys at dose levels of 2 or 50 mg/kg once weekly from gestation day 20 until parturition. Infant development, including immune function and learning ability tests, was comprehensively assessed at multiple examinations until approximately 10 months after birth.
SA237 plasma concentrations were almost equivalent between dams and their infants and dropped throughout the postnatal period, pharmacologically relevant exposure was maintained for 147 days after birth at 50 mg/kg. Because the binding of SA237 to IL-6R inhibited IL-6R-mediated clearance of IL-6, serum IL-6 increased in dams and infants. However, there were no SA237-related adverse effects on dams, embryos, fetuses, or infants. SA237 pharmacological effects contributed to the suppression of plasma cell differentiation and antibody production by inhibiting IL-6 signaling, and T cell-dependent antibody reaction was minimally suppressed in infants, but physiological immunoglobulin class switching and general antibody production against a T cell-dependent antigen were maintained.
The exposure to SA237 did not adversely affect dams, embryo-fetal development, parturition, and postnatal development, including immune function and neuronal development. Birth Defects Research 109:843-856, 2017. © 2017 Wiley Periodicals, Inc.
SA237 是一种人源化抗白细胞介素-6 受体(IL-6R)单克隆抗体,其恒定区和可变区经过工程改造以延长血浆半衰期。根据文献,阻断 IL-6 相关功能可能会对妊娠维持、免疫系统发育和大脑生长产生影响。
在一项增强的孕前和孕后发育研究中,研究了 SA237 对母体、胚胎-胎儿发育、分娩和产后发育的影响,其中 SA237 从妊娠第 20 天到分娩时以 2 或 50mg/kg 的剂量每周一次皮下给药给妊娠食蟹猴。通过多次检查全面评估婴儿发育,包括免疫功能和学习能力测试,直到出生后约 10 个月。
SA237 母体和婴儿的血浆浓度几乎相等,并且在整个产后期间下降,在 50mg/kg 时,出生后 147 天维持了药理学相关的暴露。由于 SA237 与 IL-6R 的结合抑制了 IL-6R 介导的 IL-6 清除,因此母体内和婴儿体内的血清 IL-6 增加。然而,SA237 对母体、胚胎、胎儿或婴儿没有任何不良反应。SA237 的药理作用通过抑制 IL-6 信号抑制浆细胞分化和抗体产生,从而导致 T 细胞依赖性抗体反应受到抑制,但婴儿的 T 细胞依赖性抗体反应受到最小抑制,而生理性免疫球蛋白类别转换和针对 T 细胞依赖性抗原的一般抗体产生得到维持。
暴露于 SA237 不会对母体、胚胎-胎儿发育、分娩和产后发育产生不利影响,包括免疫功能和神经发育。出生缺陷研究 109:843-856,2017。©2017 年 Wiley 期刊,Inc.