Research Division, JCR Pharmaceuticals, 2-2-9 Murotani, Nishi-ku, Kobe 651-2241, Japan.
Research Division, JCR Pharmaceuticals, 2-2-9 Murotani, Nishi-ku, Kobe 651-2241, Japan.
Mol Ther. 2021 May 5;29(5):1853-1861. doi: 10.1016/j.ymthe.2021.01.027. Epub 2021 Jan 26.
Mucopolysaccharidosis II (MPS II), a lysosomal storage disease caused by mutations in iduronate-2-sulfatase (IDS), is characterized by a wide variety of somatic and neurologic symptoms. The currently approved intravenous enzyme replacement therapy with recombinant IDS (idursulfase) is ineffective for CNS manifestations due to its inability to cross the blood-brain barrier (BBB). Here, we demonstrate that the clearance of heparan sulfate (HS) deposited in the brain by a BBB-penetrable antibody-enzyme fusion protein prevents neurodegeneration and neurocognitive dysfunctions in MPS II mice. The fusion protein pabinafusp alfa was chronically administered intravenously to MPS II mice. The drug reduced HS and attenuated histopathological changes in the brain, as well as in peripheral tissues. The loss of spatial learning abilities was completely suppressed by pabinafusp alfa, but not by idursulfase, indicating an association between HS deposition in the brain, neurodegeneration, and CNS manifestations in these mice. Furthermore, HS concentrations in the brain and reduction thereof by pabinafusp alpha correlated with those in the cerebrospinal fluid (CSF). Thus, repeated intravenous administration of pabinafusp alfa to MPS II mice decreased HS deposition in the brain, leading to prevention of neurodegeneration and maintenance of neurocognitive function, which may be predicted from HS concentrations in CSF.
黏多糖贮积症 II 型(MPS II)是一种溶酶体贮积病,由艾杜糖-2-硫酸酯酶(IDS)基因突变引起,其特征是存在广泛的躯体和神经症状。目前批准的重组 IDS(艾杜硫酸酯酶)静脉酶替代疗法对中枢神经系统表现无效,因为它不能穿过血脑屏障(BBB)。在这里,我们证明了一种可穿透血脑屏障的抗体-酶融合蛋白清除脑内沉积的硫酸乙酰肝素(HS),可预防 MPS II 小鼠的神经退行性变和神经认知功能障碍。融合蛋白 pabinafusp alfa 被长期静脉内给药于 MPS II 小鼠。该药物降低了 HS 并减轻了脑和外周组织的组织病理学变化。空间学习能力的丧失完全被 pabinafusp alfa 抑制,但不是由 idursulfase 抑制,表明 HS 在脑内沉积、神经退行性变和这些小鼠的中枢神经系统表现之间存在关联。此外,脑内 HS 浓度及其由 pabinafusp alfa 降低的程度与脑脊液(CSF)中的 HS 浓度相关。因此,重复静脉内给予 pabinafusp alfa 可减少 MPS II 小鼠脑内 HS 沉积,从而预防神经退行性变和维持神经认知功能,这可从 CSF 中的 HS 浓度预测。