"This comprehensive ebook covers all the aspects of ADME/PK modeling including solubility, absorption, formulation, metabolic stability, drug-drug interaction potential and a special delivery tool of drug candidates. The book provides an integrated view of"

Of the thousands of novel compounds that a drug discovery project team invents and that bind to the therapeutic target, typically only a fraction of these have sufficient ADME/Tox properties to become a drug product. Understanding ADME/Tox is critical for all drug researchers, owing to its increasing importance in advancing high quality candidates to clinical studies and the processes of drug discovery. If the properties are weak, the candidate will have a high risk of failure or be less desirable as a drug product. This book is a tool and resource for scientists engaged in, or preparing for, the selection and optimization process. The authors describe how properties affect in vivo pharmacological activity and impact in vitro assays. Individual drug-like properties are discussed from a practical point of view, such as solubility, permeability and metabolic stability, with regard to fundamental understanding, applications of property data in drug discovery and examples of structural modifications that have achieved improved property performance. The authors also review various methods for the screening (high throughput), diagnosis (medium throughput) and in-depth (low throughput) analysis of drug properties. - Serves as an essential working handbook aimed at scientists and students in medicinal chemistry - Provides practical, step-by-step guidance on property fundamentals, effects, structure-property relationships, and structure modification strategies - Discusses improvements in pharmacokinetics from a practical chemist's standpoint

Medicinal chemistry is both science and art. The science of medicinal chemistry offers mankind one of its best hopes for improving the quality of life. The art of medicinal chemistry continues to challenge its practitioners with the need for both intuition and experience to discover new drugs. Hence sharing the experience of drug research is uniquely beneficial to the field of medicinal chemistry. Drug research requires interdisciplinary team-work at the interface between chemistry, biology and medicine. Therefore, the topic-related series Topics in Medicinal Chemistry covers all relevant aspects of drug research, e.g. pathobiochemistry of diseases, identification and validation of (emerging) drug targets, structural biology, drugability of targets, drug design approaches, chemogenomics, synthetic chemistry including combinatorial methods, bioorganic chemistry, natural compounds, high-throughput screening, pharmacological in vitro and in vivo investigations, drug-receptor interactions on the molecular level, structure-activity relationships, drug absorption, distribution, metabolism, elimination, toxicology and pharmacogenomics. In general, special volumes are edited by well known guest editors.

This authoritative volume provides a contemporary view on the latest research in molecules with optimal drug-like properties. It is a valuable source to access current best practices as well as new research techniques and strategies. Written by leading scientists in their fields, the text consists of fourteen chapters with an underlying theme of early collaborative opportunities between pharmaceutical and discovery sciences. The book explores the practical realities of performing physical pharmaceutical and biopharmaceutical research in the context of drug discovery with short timelines and low compound availability. Chapters cover strategies and tactics to enable discovery as well as predictive approaches to establish, understand and communicate risks in early development. It also examines the detection, characterization, and assessment of risks on the solid state properties of advanced discovery and early development candidates, highlighting the link between solid state properties and critical development parameters such as solubility and stability. Final chapters center on techniques to improve molecular solubilization and prevent precipitation, with particularly emphasis on linking physiochemical properties of molecules to formulation selection in preclinical and clinical settings.

Focused on central nervous system (CNS) drug discovery efforts, this book educates drug researchers about the blood-brain barrier (BBB) so they can affect important improvements in one of the most significant – and most challenging – areas of drug discovery. • Written by world experts to provide practical solutions to increase brain penetration or minimize CNS side-effects • Reviews state-of-the-art in silico, in vitro, and in vivo tools to assess brain penetration and advanced CNS drug delivery strategies • Covers BBB physiology, medicinal chemistry design principles, free drug hypothesis for the BBB, and transport mechanisms including passive diffusion, uptake/efflux transporters, and receptor-mediated processes • Highlights the advances in modelling BBB pharmacokinetics and dynamics relationships (PK/PD) and physiologically-based pharmacokinetics (PBPK) • Discusses case studies of successful CNS and non-CNS drugs, lessons learned and paths to the market

The complexity of cancer demands an integrated approach from both a cancer biology standpoint and a pharmaceutical basis to understand the different anticancer modalities. Current research has been focused on conventional and newer anticancer modalities, recent discoveries in cancer research, and also the advancements in cancer treatment. There is a current need for more research on the advances in cancer therapeutics that bridge the gap between basic research (pharmaceutical drug development processes, regulatory issues, and translational experimentation) and clinical application. Recent promising discoveries such as immunotherapies, promising therapies undergoing clinical trials, synthetic lethality, carbon beam radiation, and other exciting targeted therapies are being studied to improve and advance the studies of modern cancer treatment. The Handbook of Research on Advancements in Cancer Therapeutics serves as a comprehensive guide in modern cancer treatment by combining and merging the knowledge from both cancer biology and the pharmacology of anticancer modalities. The chapters come from multi-disciplinary backgrounds, including scientists and clinicians from both academia and various industries, to discuss nascent personalized therapies and big data-driven cancer treatment. While highlighting topic areas that include cancer prevention, cancer therapeutics, and cancer treatments through the lenses of technology, medicine/drugs, and alternate therapies, this book is ideally intended for oncologists, radiation oncologists, surgical oncologists, and cancer biologists, along with practitioners, stakeholders, researchers, academicians, and students who are interested in understanding the most fundamental aspects of cancer and the available therapeutic opportunities.

Aqueous solubility is one of the major challenges in the early stages of drug discovery. One of the most common and effective methods for enhancing solubility is the addition of an organic solvent to the aqueous solution. Along with an introduction to cosolvency models, the Handbook of Solubility Data for Pharmaceuticals provides an extensive datab

Silver nanoparticles are the subject of immense interest because of their distinct chemical and physical properties that are different from their bulk counterpart. This makes these nanoparticles very important in many fields including antimicrobial applications, biosensor materials, composite fibers, cryogenic superconducting materials, cosmetic products, and electronic components. This book aims to provide in-depth study and analysis of various fabrication, characterization, and application techniques of silver nanoparticles that lead these nanoparticles very important in the recent technology. This book presents deep understanding of the new techniques from basic to the advanced level. This book addresses scientists, engineers, doctoral and postdoctoral fellows, and technical professionals working in specialized fields.