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综述了提高蛋白质药物半衰期技术的最新进展。由于蛋白质药物在体内会被快速清除,所以患者必须频繁用药才能保持药物浓度,限制了其治疗效果。因此,延长蛋白质药物体内的半衰期并阻止其被快速清除已成为近年来的研究热点。已建立的提高蛋白质药物半衰期的技术包括化学修饰、蛋白质融合、微囊化、糖基化、抗蛋白酶突变体等,许多长效蛋白质药物已经研制成功并应用于临床治疗。阐述了这些技术的原理并通过实例比较和评价了各种技术的优点和适用范围。
The recent progress in improving the half-life of protein drugs is reviewed. Because protein drugs are rapidly cleared in the body, patients must be frequently administered to maintain their drug concentration, limiting their effectiveness. Therefore, prolonging the half-life of protein drugs in vivo and preventing them from being rapidly cleared has become a research hotspot in recent years. Established technology to improve the half-life of protein drugs, including chemical modification, protein fusion, microencapsulation, glycosylation, anti-protease mutants, many long-acting protein drugs have been developed and applied to clinical treatment. The principles of these technologies are expounded and the advantages and scope of various technologies are compared and evaluated through examples.