长效化融合蛋白药物及其药动学分析技术的研究进展

发布时间：2018-12-30 21:34

【摘要】：融合蛋白技术应用于生物制药行业已超过25年,其目的为改善原来天然蛋白的性质,从而具有新的理化特征和生物学功能,其中最为显著的特点是改善了小分子蛋白及多肽半衰期短的缺陷。基于该技术所诞生的融合蛋白类药物已成为当前生物药研发的热点。结合已上市融合蛋白类药物,通过与传统多肽蛋白类药物比较,重点突出融合蛋白类药物自身特点,主要从融合抗体Fc段和人血清白蛋白以延长小分子蛋白及多肽半衰期的角度对融合蛋白药物长效化策略进行评述;对融合蛋白类药物在体内的吸收、分布、代谢和排泄的显著特征进行概述;综述该类药物在体内的分析技术并指出当前分析技术的优缺点及发展方向,为长效化融合蛋白药物的设计、分析研究与开发提供依据和思路。
[Abstract]:Fusion protein technology has been used in the biopharmaceutical industry for more than 25 years. Its aim is to improve the properties of the original natural proteins and thus have new physical and chemical characteristics and biological functions. The most significant feature is the improvement of short half-life of small molecular proteins and peptides. The fusion protein drugs based on this technology have become a hot spot in the research and development of biopharmaceuticals. By comparing with the traditional polypeptide and protein drugs, the characteristics of the fusion protein drugs are emphasized. The long-term strategy of fusion protein drug was reviewed from the angle of fusion antibody Fc segment and human serum albumin to prolong the half-life of small molecule protein and polypeptide. The characteristics of absorption, distribution, metabolism and excretion of fusion proteins in vivo were summarized. This paper summarizes the analytical techniques of this kind of drugs in vivo and points out the advantages and disadvantages and the development direction of the current analytical techniques, which provides the basis and train of thought for the design, analysis and development of long-acting fusion protein drugs.
【作者单位】：中国药科大学;天士力制药集团股份有限公司研究院药理毒理研究中心;
【分类号】：R96

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