This book reviews biotherapeutics from a medicinal chemistry perspective. It covers proteins, nucleic acids, low molecular weight hormones, small peptides, extracellular vesicles, gene therapy, cell-based products, and tissue-engineered products. Expert contributors provide insights into the mechanisms of action and translational processes of biotherapeutics. Particular attention is given to the latest developments in therapeutic proteins and nucleic acids. Biotherapeutic formulation developments like encapsulation, structural modifications and nanovehiculization are also presented in this book. Divided into 15 chapters, the book begins with basic concepts and definitions of biotherapeutics from a medicinal chemistry standpoint. The following chapters focus on therapeutic proteins, monoclonal antibodies, protein production, and structural modifications. Other chapters cover topics such as antisense oligonucleotides, aptamers, mRNA, gene therapy, as well as other biotherapeutics like low molecular weight hormones and small peptides. The book concludes with an overview of biotherapeutic formulations and an authoritative discussion on regulatory aspects. Throughout the book, readers will learn how biotherapeutics, whether obtained through bioprocesses or not, impact bioresponses and can be utilized for therapeutic purposes. Given its breadth, the book appeals to researchers in medicinal chemistry and biotherapeutics, scholars of medicinal chemistry, students at all levels of biochemical studies, practitioners in the medical field, and anyone interested in biotherapeutics.