抗体-药物偶联物（ADCs）中的化学链接器

English | December 22, 2021 | ISBN-10: 1839162635 | 476 pages| Epub PDF (True) | 30 MB

The covalent conjugation of potent cytotoxic agents to monoclonal antibodies, known as antibody-drug conjugates (ADCs) is a powerful approach in the field of targeted treatment of cancer. Clearly, both monoclonal antibody and cytotoxic payload are crucial elements in determining the clinical value of an ADC and have receive ample attention. However, the structural element connecting the two –the chemical linker– also plays an essential role in mode-of-action, efficacy, pharmacokinetics and safety profile of an ADC, but is often underappreciated in considerations of ADC design.Chemical Linkers in Antibody–Drug Conjugates aims to shine a detailed light on the various key attributes of chemical linkers in ADCs, for drug-to-antibody ratio, for stability, for release mechanism of payload, for pharmacokinetics, for stability determination, and for efficacy and safety. Ideal for postgraduate students and active researchers in drug discovery and development, this book provides a comprehensive description of linkers used in ADCs (clinical and late preclinical), insight into key quality attributes of linkers for ADCs, and aids the reader in understanding the role of linker chemistry and designing new ADCs.

抗体药物偶联物（ADC）中的共价连接剂的共价结合是癌症靶向治疗领域的一种强大方法。显然，单克隆抗体和细胞毒性载荷都是决定ADC临床价值的关键要素，并受到了充分的关注。然而，在设计ADC时往往被忽视的是连接两者之间的结构元素——化学链接剂在ADC的作用机制、疗效、药代动力学以及安全性方面都起着至关重要的作用。《抗体药物偶联物中的化学链接剂》旨在详细阐述ADC中各种关键链接器的属性，包括药物与抗体的比例、稳定性、载荷释放机制、药代动力学、稳定性的确定方法以及疗效和安全性等方面的内容。这本书适合于药物发现与开发领域的研究生及活跃的研究人员阅读，可以提供关于ADC中使用的链接剂（临床阶段和晚期前临床）的全面描述，还可以帮助读者理解链接器化学的作用及其在设计新的ADC中的作用。

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