This book explains how peptide-based drug design works, what steps are needed to develop a peptide-based therapeutic, and challenges in synthesis as well as regulatory issues. It covers the design concept of peptide therapeutics from fundamental principles using structural biology and computational approaches. The chapters are arranged in a linear fashion. A fresh graduate or a scientist who works on small molecules can use this to follow the design and development of peptide therapeutics to use as understanding the basic concepts. Each chapter is written by experts from academia as well as industry. Rather than covering extensive literature, the book provides concepts of design, synthesis, delivery, as well as regulatory affairs and manufacturing of peptides in a systematic way with examples in each case. The book can be used as a reference for a pharmaceutical or biomedical scientist or graduate student who wants to pursue their career in peptide therapeutics. Some chapters will be written as a combination of basic principles and protocol so that scientists can adopt these methods to their research work. The examples provided can be used to perform peptide formulation considerations for the designed peptides. The book has nine chapters, and each chapter can be read as an independent unit on a particular concept.

This thorough book explores some of the most important methods and concepts affecting the quantitative analysis of the transport, targeting, and disposition of chemicals within cells, which in turn impact the macroscopic pharmacokinetics of chemical agents in the whole organism. The first half of the volume focuses on small organic molecules with drug-like characteristics, while the second half delves into the cellular pharmacokinetics of biologics and other macromolecules, including peptide therapeutics, cyclotides, antibodies, as well as nanoparticles, thus creating a comprehensive treatise that approaches cellular pharmacokinetics from the different perspectives of pharmaceutical scientists, chemical biologists, medicinal chemists, and protein engineers dealing with very different chemical agents spanning a wide range of sizes, physicochemical properties, and targeting mechanisms. Written for the Methods in Pharmacology and Toxicology series, chapters provide the kind of key detail and expert implementation advice that leads to excellent results in the lab. Synthetic biologists, biophysicists, and bioengineers are amongst the long list of scientists who could benefit from reading this book or from using it as a textbook. Authoritative and practical, Quantitative Analysis of Cellular Drug Transport, Disposition, and Delivery builds on a long history of drug development and the adding of quantitative methods at the cellular scale in order to inspire new approaches to drug development that are better able to take advantage of phenomena such as soluble-to-insoluble phase transitions or bispecific targeting, which could ultimately be exploited for the development of more effective drug delivery systems and therapeutic agents.

CONTEMPORARY ACCOUNTS IN DRUG DISCOVERY AND DEVELOPMENT A useful guide for medicinal chemists and pharmaceutical scientists Drug discovery is a lengthy and complex process that typically involves identifying an unmet medical need, determining a biological target, chemical library screening to identify a lead, chemical optimization, preclinical studies and clinical trials. This process often takes many years to complete, and relies on practitioners’ knowledge of chemistry and biology, but also—and perhaps more importantly—on experience. Improving the success rate in discovery and development through a thorough knowledge of drug discovery principles and advances in technology is critical for advancement in the field. Contemporary Accounts in Drug Discovery and Development provides drug discovery scientists with the knowledge they need to quickly gain mastery of the drug discovery process. A thorough accounting is given for each drug covered within the book, as the authors provide pharmacology, drug metabolism, biology, drug development, and clinical studies for every case, with modern drug discovery principles and technologies incorporated throughout. Contemporary Accounts in Drug Discovery and Development readers will also find Case histories used as an engaging way of learning about the drug discovery/development process Detailed biological rational and background information, drug design principles, SAR development, ADMET considerations, and clinical studies The full history of individual marketed small molecule drugs Coverage of drug candidates that have passed Phase I clinical trials with different modalities, such as antibody drug conjugates (ADC), proteolysis-targeting chimera (PROTAC), and peptide drugs The application of new technologies in drug discovery such as DNA-encoded libraries (DEL), positron emission tomography (PET), and physics-based computational modeling employing free energy perturbation (FEP) Contemporary Accounts in Drug Discovery and Development is a helpful tool for medicinal chemists, organic chemists, pharmacologists, and other scientists in drug research and process development. It may be considered essential reading for graduate courses in drug discovery, medicinal chemistry, drug synthesis, pharmaceutical science, and pharmacology. It is also a useful resource for pharmaceutical industry labs, as well as for libraries.

ORAL BIOAVAILABILITY AND DRUG DELIVERY Improve the performance and viability of newly-developed and approved drugs with this crucial guide Bioavailability is the parameter which measures the rate and extent to which a drug reaches a user’s circulatory system depending on the method of administration. For example, intravenous administration produces a bioavailability of 100%, since the drugs are injected directly into the circulatory system; in the case of oral administration, however, bioavailability can vary widely based on factors which, if not properly understood, can result in a failure in drug development, adverse effects, and other complications. The mechanics of oral bioavailability are therefore critical aspects of drug development. Oral Bioavailability and Drug Delivery provides a comprehensive coverage of this subject as well as its drug development applications. Beginning with basic terminology and fundamental concepts, it provides a thorough understanding of the challenges and barriers to oral bioavailability as well as the possibilities for improving this parameter. The resulting book is an indispensable tool for drug development research. Oral Bioavailability and Drug Delivery readers will also find: Discussion questions in many chapters to facilitate comprehension Detailed discussion of topics including dissolution, absorption, metabolism, and more Real-world examples of methods in actions throughout Oral Bioavailability and Drug Delivery is ideal for pharmaceutical and biotechnology scientists working in drug discovery and development; researchers in chemistry, biology, pharmacology, immunology, neuroscience, and other related fields; and graduate courses in drug development and delivery.

A comprehensive guide to the current research, major challenges, and future prospects of controlled drug delivery systems Controlled drug delivery has the potential to significantly improve therapeutic outcomes, increase clinical benefits, and enhance the safety of drugs in a wide range of diseases and health conditions. Fundamentals of Drug Delivery provides comprehensive and up-to-date coverage of the essential principles and processes of modern controlled drug delivery systems. Featuring contributions by respected researchers, clinicians, and pharmaceutical industry professionals, this edited volume reviews the latest research in the field and addresses the many issues central to the development of effective, controlled drug delivery. Divided in three parts, the book begins by introducing the concept of drug delivery and discussing both challenges and opportunities within the rapidly evolving field. The second section presents an in-depth critique of the common administration routes for controlled drug delivery, including delivery through skin, the lungs, and via ocular, nasal, and otic routes. The concluding section summarizes the current state of the field and examines specific issues in drug delivery and advanced delivery technologies, such as the use of nanotechnology in dermal drug delivery and advanced drug delivery systems for biologics. This authoritative resource: Covers each main stage of the drug development process, including selecting pharmaceutical candidates and evaluating their physicochemical characteristics Describes the role and application of mathematical modelling and the influence of drug transporters in pharmacokinetics and drug disposition Details the physiology and barriers to drug delivery for each administration route Presents a historical perspective and a look into the possible future of advanced drug delivery systems Explores nanotechnology and cell-mediated drug delivery, including applications for targeted delivery and toxicological and safety issues Includes comprehensive references and links to the primary literature Edited by a team of of internationally-recognized experts, Fundamentals of Drug Delivery is essential reading for researchers, industrial scientists, and advanced students in all areas of drug delivery including pharmaceutics, pharmaceutical sciences, biomedical engineering, polymer and materials science, and chemical and biochemical engineering.

ORAL DRUG DELIVERY FOR MODIFIED RELEASE FORMULATIONS Provides pharmaceutical development scientists with a detailed reference guide for the development of MR formulations Oral Drug Delivery for Modified Release Formulations is an up-to-date review of the key aspects of oral absorption from modified-release (MR) dosage forms. This edited volume provides in-depth coverage of the physiological factors that influence drug release and of the design and evaluation of MR formulations. Divided into three sections, the book begins by describing the gastrointestinal tract (GIT) and detailing the conditions and absorption processes occurring in the GIT that determine a formulation’s oral bioavailability. The second section explores the design of modified release formulations, covering early drug substance testing, the biopharmaceutics classification system, an array of formulation technologies that can be used for MR dosage forms, and more. The final section focuses on in vitro, in silico, and in vivo evaluation and regulatory considerations for MR formulations. Topics include biorelevant dissolution testing, preclinical evaluation, and physiologically-based pharmacokinetic modelling (PBPK) of in vivo behaviour. Featuring contributions from leading researchers with expertise in the different aspects of MR formulations, this volume: Provides authoritative coverage of physiology, physicochemical determinants, and in-vitro in-vivo correlation (IVIVC) Explains the different types of MR formulations and defines the key terms used in the field Discusses the present status of MR technologies and identifies current gaps in research Includes a summary of regulatory guidelines from both the US and the EU Shares industrial experiences and perspectives on the evaluation of MR dosage formulations Oral Drug Delivery for Modified Release Formulations is an invaluable reference and guide for researchers, industrial scientists, and graduate students in general areas of drug delivery including pharmaceutics, pharmaceutical sciences, biomedical engineering, polymer and materials science, and chemical and biochemical engineering.