The field of antibody-drug conjugates (ADCs) has undergone remarkable advancements in recent years, marked by significant progress in both drug approvals and ongoing clinical development. Since the approval of the first ADC in 2010 (gemtuzumab ozogamicin, Mylotarg®), the landscape has expanded dramatically. Today, there are 11 FDA-approved ADCs, targeting a variety of cancers across multiple indications. The approved ADCs include a range of payloads, linkers, and antibodies, each optimized for a variety of specific therapeutic targets. The increasing diversity of ADCs reflects the growing potential of these innovative treatments to address a wide array of malignancies, from hematologic cancers to solid tumors.

This book aims to provide a comprehensive overview of the current state of the ADC field including the latest developments, challenges, and emerging trends, comprising expertise from a broad range of disciplines from basic research, industry, clinical practice and regulatory affairs. We explore not only the scientific and technical aspects of ADC design—such as payloads, linkers, and antibody selection—but also the developmental hurdles and regulatory complexities that influence the success of ADCs in clinical practice. Real-world examples of ADCs that have made it from the lab to the clinic offer invaluable insights into the trials and triumphs that shape this dynamic field. It is our hope that this book will serve as both a valuable resource for experts in the field and an accessible introduction for those new to the exciting world of ADCs.

Dr. Jennica Zaro earned her Ph.D. in Pharmaceutical Sciences from the University of Southern California (USC). Her research focuses on the targeted delivery of peptide and protein drugs, as well as the development of recombinant bifunctional fusion proteins as therapeutics. Dr. Zaro is currently an Associate Professor at the USC School of Pharmacy and Pharmaceutical Sciences. She has held several academic administrative roles, including Core Director of the Translational Research Laboratory and Assistant Dean of Assessment for Graduate Education at USC, and Assistant Dean of Assessment at West Coast University. In addition to her academic roles, she has significant experience in the pharmaceutical industry, where she contributed to the development of formulations for aerosol products and designed and validated analytical methods for protein drugs.

Dr. Jeffrey Wang received a BS degree from the School of Pharmacy, Shanghai Medical University and a PhD degree in pharmaceutical sciences from the University of Southern California. Dr. Wang’s research focuses on the application of principles of pharmacokinetics and drug metabolism in drug discovery and delivery, particularly in anti-cancer drug discovery and peptide drug delivery. He has published over 80 peer-reviewed articles and book chapters, and is the co-inventor of several US and international patents. Dr. Wang is currently a Professor of Biotechnology and Pharmaceutical Sciences and Associate Dean for Research and Global Advancement at the College of Pharmacy, Western University of Health Sciences.