抗体偶联药物（ADC）是一类意义非凡的高效生物药，有望成为广泛应用的癌症治疗方法。ADC是由单克隆抗体与细胞毒性药物通过生物活性连接子偶联而成的化合物分子。与化疗不同，ADC的研究理念是仅标记并杀死癌细胞，因而成为靶向性较高的治疗方法。ADC在癌症领域发挥着举足轻重的作用，全球市场上约有12种ADC用于血液瘤和恶性实体瘤。辉瑞公司、基因泰克公司、吉利德科学公司以及许多其他药企都在大力投资ADC，市场竞争处于白热化状态。作为靶向肿瘤的生物治疗药物，ADC的治疗潜力非比寻常；ADC只有在内化到肿瘤细胞后才会启动其作用机制，然后释放细胞毒性有效载荷，从而选择性地杀死恶性肿瘤细胞。ADC无疑是近几年最火的领域之一，2022年全球销售规模超过70亿美元，去年前九个月主要产品销售额已超过70亿美元，全年有望突破百亿美元大关，目前全球已经有15个ADC获批上市，在中国获批的有7个。目前比较热门的靶点有CD22、HER2、EGFR、Trop-2、BCMA、Nectin-4等，常见适应症主要包括乳腺癌、肺癌、胃癌和血癌等肿瘤。ADC赛道席卷全球，在研的ADC药物多达几百款，国内外药企不惜重金纷纷布局ADC，如辉瑞斥资430亿美元收购Seagen，近期默沙东以高达220亿美元与第一三共达成合成协议，共同开发第一三共的三款ADC产品。国内也有通过自研、并购或License in等模式布局ADC管线的药企，其中科伦药业的HER2 ADC产品A166正在申报上市，科伦药业的SKB264、恒瑞医药的SHR-A1811、石药的DP303c和乐普生物的MRG002等都处于临床3期。越来越多的ADC的获批上市，截至目前，全球获批上市ADC药物有15个，在中国获批上市的产品有7个。也有多款药物进入临床阶段，其中靶向HER2的ADC研究最火热，其次是Trop-2等。图1. 获批上市的ADC药物（药时代整理）图2. 部分在研的临床3期ADC药物（药时代整理）图3. 部分临床2期在研的ADC药物（药时代整理）图4. 部分临床1期在研的ADC药物（药时代整理）值新书佳节之际，小编精选了ADC药物在研发、生产、注册、临床及市场的8本书籍和大家一起学习交流，有兴趣的老师可以扫码登记，符合要求方可加入我们学习行列。快快加入我们喔，一起过一个充实而又愉快的春节！Antibody-Drug Conjugates and Cellular Metabolic DynamicsThis book summarizes the related research achievements in Antibody-drug conjugates (ADCs) and their cell metabolism kinetics. The book has three main parts. The first part describes the basic theory of ADCs, including the basic concept and structure of ADCs, and the relationship between the targets of ADCs and their specific functions. The second part mainly introduces the endocytosis and intracellular metabolism of ADCs, including the relationship between endocytosis and ADC activity, the endocytosis and intracellular transport of ADCs, the distribution and metabolism of ADC in vivo. Then it discusses the new formats and research technology of ADCs, including the application of miniaturized antibodies in ADC synthesis, novel carriers for ADC design, the technology and application of site-specific conjugation, and approaches for analyzing the drug: antibody ratio (DAR), the study of pharmacokinetics of ADCs. This book combines the basic theory with the research technology. It can be used as a reference book for students, teachers and researchers of biomedical field.Chemical Linkers in Antibody-Drug Conjugates (ADCs) 2021The 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 Conjugatesaims 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.Antibody-Drug Conjugates: Methods and ProtocolsThis volume looks at key methodologies that are commonly used across antibody drug conjugates (ADCs) programs. The chapters in this book cover topics such as conjugations to endogenous cysteine residues; click chemistry conjugations; antibody conjugations via glycosyl remodeling; analysis of ADCs by native mass spectrometry; characterization of ADCs by capillary electrophoresis; LC/MS methods for studying lysosomal ADC catabolism; and determination of ADC concentration by ligand-binding assays. Written in the highly successful Methods in Molecular Biology series format, chapters include introductions to their respective topics, lists of the necessary materials and reagents, step-by-step, readily reproducible laboratory protocols, and tips on troubleshooting and avoiding known pitfalls. Cutting-edge and practical, Antibody-Drug Conjugates: Methods and Protocols is a valuable resource that aims to lower the “activation barrier” when undertaking a new discipline, and provides a “toolbox” for the next generation of ADC scientists.Next Generation Antibody Drug Conjugates (ADCs) and ImmunotoxinsThis book describes the newest developments in antibody drug conjugates and immunotoxins, paving their way to clinical application. Lessons learned from the current state of the art are used to further improve our understanding of their mechanisms of action and off target activities.The book introduces scientists to all of the prerequisites that must be properly addressed, including identification of the right target, specific traits of target binding antibodies, proper selection of the toxic payload, internalization induced by binding, and next generation conjugation and linker technologies. These knowledge-based, revolutionary new drug principles will form the cornerstone of the future standard of care and will lead to major advances in application, as well as improved quality of life and patient survival rates. This book will be of interest to biotech companies and researchers working in the fields of immunology, pharmacology, and oncology.Antibody-Drug Conjugates: Fundamentals, Drug Development, and Clinical Outcomes to Target CancerProviding practical and proven solutions for antibody-drug conjugate (ADC) drug discovery success in oncology, this book helps readers improve the drug safety and therapeutic efficacy of ADCs to kill targeted tumor cells.• Discusses the basics, drug delivery strategies, pharmacology and toxicology, and regulatory approval strategies• Covers the conduct and design of oncology clinical trials and the use of ADCs for tumor imaging• Includes case studies of ADCs in oncology drug development• Features contributions from highly-regarded experts on the frontlines of ADC research and developmentAntibody-Drug Conjugates and Immunotoxins: From Pre-Clinical Development to Therapeutic ApplicationsThis volume gathers the leading research on antibody-drug conjugates and immunotoxins. Following a rigorous overview, the volume delves into focused sections on all aspects of ADCs and ITs from clinical development through to targeted therapeutic applications and the latest technologies.Antibody-Drug Conjugates: The 21st Century Magic Bullets for CancerThis authoritative volume provides a holistic picture of antibody-drug conjugates (ADCs). Fourteen comprehensive chapters are divided into six sections including an introduction to ADCs, the ADC construct, development issues, landscape, IP and pharmacoeconomics, case studies, and the future of the field. The book examines everything from the selection of the antibody, the drug, and the linker to a discussion of developmental issues such as formulations, bio-analysis, pharmacokinetic-pharmacodynamic relationships, and toxicological and regulatory challenges. It also explores pharmacoecomonics and intellectual properties, including recently issued patents and the cost analysis of drug therapy. Case studies are presented for the three ADCs that have received FDA approval: gemtuzumab ozogamicin (Mylotarg®), Brentuximab vedotin (Adcetris®), and ado-trastuzumab emtansine (Kadcyla®), as well as an ADC in late-stage clinical trials, glembatumumab vedotin (CDX-011). Finally, the volume presents a perspective by the editors on the future directions of ADC development and clinical applications.Antibody-Drug Conjugates is a practical and systematic resource for scientists, professors, and students interested in expanding their knowledge of cutting-edge research in this exciting field.Innovations for Next-Generation Antibody-Drug Conjugates Antibody-drug conjugates (ADCs) stand at the verge of a transformation. Scores of clinical programs have yielded only a few regulatory approvals, but a wave of technological innovation now empowers us to overcome past technical challenges. This volume focuses on the next generation of ADCs and the innovations that will enable them. The book inspires the future by integrating the field’s history with novel strategies and cutting-edge technologies. While the book primarily addresses ADCs for solid tumors, the last chapter explores the emerging interest in using ADCs to treat other diseases.The therapeutic rationale of ADCs is strong: to direct small molecules to the desired site of action (and away from normal tissues) by conjugation to antibodies or other targeting moieties. However, the combination of small and large molecules imposes deep complexity to lead optimization, pharmacokinetics, toxicology, analytics and manufacturing. The field has made significant advances in all of these areas by improving target selection, ADC design, manufacturing methods and clinical strategies. These innovations will inspire and educate scientists who are designing next-generation ADCs with the potential to transform the lives of patients.识别微信二维码，添加生物制品圈小编，符合条件者即可加入生物制品微信群！请注明：姓名+研究方向！版权声明本公众号所有转载文章系出于传递更多信息之目的，且明确注明来源和作者，不希望被转载的媒体或个人可与我们联系(cbplib@163.com)，我们将立即进行删除处理。所有文章仅代表作者观点，不代表本站立场。
