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四种天冬酰胺酶的物理化学性质评估

Physicochemical quality assessment of four asparaginases.

作者信息

Radtke Vanessa, König Thorsten, Radcke Christoph, Bergmann Ulf, Eichler Rene, Pohl Katja J, Schnuchel Arndt

机构信息

medac Gesellschaft für klinische Spezialpräparate m.b.H., Wedel, Germany.

Biosynth GmbH, Berlin, Germany.

出版信息

PLoS One. 2025 Jun 16;20(6):e0326106. doi: 10.1371/journal.pone.0326106. eCollection 2025.

Abstract

L-Asparaginases (ASNases) are used for the treatment of acute lymphoblastic leukaemia. There are reports of quality problems for some therapeutic asparaginase products, especially those manufactured in middle-income countries. These products may exhibit decreased potency and/or decreased specific activity, or an elevated level of impurities such as host cell proteins. In this study, four different ASNase preparations that were not modified with polyethylene glycol were compared in detail regarding their quality: Spectrila®, Celginase™, Bionase®, and L-Aspase®. Samples were analyzed for protein content, impurities, and enzyme activity. Various chromatographic methods as well as mass spectrometry were used to assess purity and identity. Sample protein content, host cell protein, and enzyme activity showed some results that were out of target range for Celginase™ and Bionase®. These ASNase preparations also showed detectable levels of endotoxins. In gel electrophoresis, additional bands were found for Bionase®. Size exclusion chromatography showed increased high and low molecular weight species for Bionase® and L-Aspase®, and reversed-phase chromatography showed increased hydrophilic and hydrophobic species for Bionase®. In capillary zone electrophoresis, increased retention time for L-Aspase® and increased levels of charge variants for Bionase®, Celginase™, and L-Aspase® were seen. ASNase quality standards are crucial to ensure patient safety and product efficacy, as decreased potency and specific activity may affect efficacy in acute lymphoblastic leukaemia treatment, and increased impurities may affect immunogenicity. Out of four ASNase preparations tested in this study, only Spectrila® did not raise any quality concerns. The other three products exhibited quality problems, rendering them unsuitable according to established quality requirements defined in European and US guidelines for pharmaceutical development of parenteral drug products.

摘要

L-天冬酰胺酶(ASNases)用于治疗急性淋巴细胞白血病。有报道称某些治疗用天冬酰胺酶产品存在质量问题,尤其是在中等收入国家生产的产品。这些产品可能表现出效力降低和/或比活性降低,或者杂质水平升高,如宿主细胞蛋白。在本研究中,对四种未用聚乙二醇修饰的不同ASNase制剂的质量进行了详细比较:Spectrila®、Celginase™、Bionase®和L-Aspase®。对样品进行了蛋白质含量、杂质和酶活性分析。使用了各种色谱方法以及质谱法来评估纯度和同一性。样品蛋白质含量、宿主细胞蛋白和酶活性的一些结果表明,Celginase™和Bionase®超出了目标范围。这些ASNase制剂还显示出可检测水平的内毒素。在凝胶电泳中,Bionase®发现了额外的条带。尺寸排阻色谱显示Bionase®和L-Aspase®的高分子量和低分子量物质增加,反相色谱显示Bionase®的亲水和疏水物质增加。在毛细管区带电泳中,观察到L-Aspase®的保留时间增加,Bionase®、Celginase™和L-Aspase®的电荷变体水平增加。ASNase质量标准对于确保患者安全和产品疗效至关重要,因为效力和比活性降低可能会影响急性淋巴细胞白血病治疗的疗效,杂质增加可能会影响免疫原性。在本研究中测试的四种ASNase制剂中,只有Spectrila®没有引起任何质量问题。其他三种产品存在质量问题,根据欧洲和美国肠胃外药品研发指南中规定的既定质量要求,它们不适合使用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8592/12169553/93623912beed/pone.0326106.g001.jpg

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