Pharmacokinetics has evolved from its origin into a complex discipline with numerous subspecialties and applications in patient management, drug development, and regulatory issues. This expansion has made it difficult for any one individual to become a full-fledged expert in all areas. Fulfilling the need for a wide-ranging guide to the many existi

This book describes the processes that are involved in the development of new drugs. The authors discuss the history, role of natural products and concept of receptor interactions with regard to the initial stages of drug discovery. In a single, highly readable volume, it outlines the basics of pharmacological screening, drug target identification, and genetics involved in early drug discovery. The final chapters introduce readers to stem therapeutics, pharmacokinetics, pharmacovigilance, and toxicological testing. Given its scope, the book will enable research scholars, professionals and young scientists to understand the key fundamentals of drug discovery, including stereochemistry, pharmacokinetics, clinical trials, statistics and toxicology.

Basic Principles of Drug Discovery and Development presents the multifaceted process of identifying a new drug in the modern era, which requires a multidisciplinary team approach with input from medicinal chemists, biologists, pharmacologists, drug metabolism experts, toxicologists, clinicians, and a host of experts from numerous additional fields. Enabling technologies such as high throughput screening, structure-based drug design, molecular modeling, pharmaceutical profiling, and translational medicine are critical to the successful development of marketable therapeutics. Given the wide range of disciplines and techniques that are required for cutting edge drug discovery and development, a scientist must master their own fields as well as have a fundamental understanding of their collaborator's fields. This book bridges the knowledge gaps that invariably lead to communication issues in a new scientist's early career, providing a fundamental understanding of the various techniques and disciplines required for the multifaceted endeavor of drug research and development. It provides students, new industrial scientists, and academics with a basic understanding of the drug discovery and development process. The fully updated text provides an excellent overview of the process and includes chapters on important drug targets by class, in vitro screening methods, medicinal chemistry strategies in drug design, principles of in vivo pharmacokinetics and pharmacodynamics, animal models of disease states, clinical trial basics, and selected business aspects of the drug discovery process. - Provides a clear explanation of how the pharmaceutical industry works, as well as the complete drug discovery and development process, from obtaining a lead, to testing the bioactivity, to producing the drug, and protecting the intellectual property - Includes a new chapter on the discovery and development of biologics (antibodies proteins, antibody/receptor complexes, antibody drug conjugates), a growing and important area of the pharmaceutical industry landscape - Features a new section on formulations, including a discussion of IV formulations suitable for human clinical trials, as well as the application of nanotechnology and the use of transdermal patch technology for drug delivery - Updated chapter with new case studies includes additional modern examples of drug discovery through high through-put screening, fragment-based drug design, and computational chemistry

Pharmacology in Drug Discovery and Development: Understanding Drug Response, Second Edition, is an introductory resource illustrating how pharmacology can be used to furnish the tools necessary to analyze different drug behavior and trace this behavior to its root cause or molecular mechanism of action. The concepts discussed in this book allow for the application of more predictive pharmacological procedures aimed at increasing therapeutic efficacy that will lead to more successful drug development. Chapters logically build upon one another to show how to characterize the pharmacology of any given molecule and allow for more informed predictions of drug effects in all biological systems. New chapters are dedicated to the interdisciplinary drug discovery environment in both industry and academia, and special techniques involved in new drug screening and lead optimization. This edition has been fully revised to address the latest advances and research related to real time kinetic assays, pluridimensional efficacy, signaling bias, irreversible and chemical antagonism, allosterically-induced bias, pharmacokinetics and safety, target and pathway validation, and much more. With numerous valuable chapter summaries, detailed references, practical examples and case studies throughout, Dr. Kenakin successfully navigates a highly complex subject, making it accessible for students, professors, and new researchers working in pharmacology and drug discovery. - Includes example-based cases that illustrate how the pharmacological concepts discussed in this book lead to practical outcomes for further research - Provides vignettes on those researchers and scientists who have contributed significantly to the fields of pharmacology and drug discovery throughout history - Offers sample questions throughout the book and an appendix containing answers for self-testing and retention

Drug Metabolism and Pharmacokinetics Quick Guide covers a number of aspects of drug assessment at drug discovery and development stages, topics such as pharmacokinetics, absorption, metabolism, enzyme kinetics, drug transporters, drug interactions, drug-like properties, assays and in silico calculations. It covers key concepts, with useful tables on physiological parameters (eg. blood flow to organs in x-species, expression and localization of enzymes and transporters), chemical structure, nomenclature, and moieties leading to bioactivation (with examples). Overall it includes a number of key topics useful at the drug discovery stage, which would serve as a quick reference with several examples from the literature to illustrate the concept.

This first ever coverage of the pharmacokinetic and pharmacodynamic characteristics of biopharmaceuticals meets the need for a comprehensive book in this field. It spans all topics from lead identification right up to final-stage clinical trials. Following an introduction to the role of PK and PD in the development of biotech drugs, the book goes on to cover the basics, including the pharmacokinetics of peptides, monoclonal antibodies, antisense oligonucleotides, as well as viral and non-viral gene delivery vectors. The second section discusses such challenges and opportunities as pulmonary delivery of proteins and peptides, and the delivery of oligonucleotides. The final section considers the integration of PK and PD concepts into the biotech drug development plan, taking as case studies the preclinical and clinical drug development of tasidotin, as well as the examples of cetuximab and pegfilgrastim. The result is vital reading for all pharmaceutical researchers.

Emphasizes the integration of major areas of drug discovery and their importance in candidate evaluation It is believed that selecting the "right" drug candidate for development is the key to success. In the last decade, pharmaceutical R&D departments have integrated pharmacokinetics and drug metabolism, pharmaceutics, and toxicology into early drug discovery to improve the assessment of potential drug compounds. Now, Evaluation of Drug Candidates for Preclinical Development provides a complete view and understanding of why absorption-distribution-metabolism-excretion-toxicology (ADMET) plays a pivotal role in drug discovery and development. Encompassing the three major interrelated areas in which optimization and evaluation of drug developability is most critical—pharmacokinetics and drug metabolism, pharmaceutics, and safety assessment—this unique resource encourages integrated thinking in drug discovery. The contributors to this volume: Cover drug transporters, cytochrome P-450 and drug-drug interactions, plasma protein binding, stability, drug formulation, preclinical safety assessment, toxicology, and toxicokinetics Address developability issues that challenge pharma companies, moving beyond isolated experimental results Reveal connections between the key scientific areas that are critical for successful drug discovery and development Inspire forward-thinking strategies and decision-making processes in preclinical evaluation to maximize the potential of drug candidates to progress through development efficiently and meet the increasing demands of the marketplace Evaluation of Drug Candidates for Preclinical Development serves as an introductory reference for those new to the pharmaceutical industry and drug discovery in particular. It is especially well suited for scientists and management teams in small- to mid-sized pharmaceutical companies, as well as academic researchers and graduate students concerned with the practical aspects related to the evaluation of drug developability.

-A landmark in the continuously changing world of drugs -Essential reading for scientists and managers in the pharmaceutical industry involved in drug finding, drug development and decision making in the development process -Of use for government institutions and committees working on official guidelines for drug evaluation worldwide

In this new edition of a bestseller, all the contents have been updated and new material has been added, especially in the areas of toxicity testing and high throughput analysis. The authors, all of them employed at Pfizer in the discovery and development of new active substances, discuss the significant parameters and processes important for the absorption, distribution and retention of drug compounds in the body, plus the potential problems created by their transformation into toxic byproducts. They cover everything from the fundamental principles right up to the impact of pharmacokinetic parameters on the discovery of new drugs. While aimed at all those dealing professionally with the development and application of pharmaceutical substances, the readily comprehensible style makes this book equally suitable for students of pharmacy and related subjects.

This volume is an important advancement in the application ofpharmacokinetic (PK) and pharmacodynamic (PO) principles to . drug development. The series of topics presented deal with the application of these tools to everyday decisions that a pharmaceutical scientist encounters. The ability to integrate these topics using PK and PO methods has optimized drug development pathways in the clinic. New technologies in the areas of in vitro assays that are more predictive of human absorption and metabolism and advancement in bioanalytical assays are leading the way to minimize drug failures in later, more expensive clinical development programs. of Pharmacokinetics and pharmacodynamics have become an important component understanding the drug action on the body and is becoming increasingly important in drug labeling due to it's potential for predicting drug behavior in populations that may be difficult to study in adequate numbers during drug development. The ability to correlate drug exposure to effect and model it during the drug development value chain provides valuable insight into optimizing the next steps to derive maximum information from each study. These principles and modeling techniques have resulted in an expanded and integrated view of PK and PO and have led to the expectations that we may be able to optimally design clinical trials and eventually lead us to identifying the optimal therapy for the patient, while minimizing cost and speeding up drug development. There is wide utility for the book both as a text and as a reference.