Of the thousands of novel compounds that a drug discovery project
team invents and that bind to the therapeutic target, only a
fraction have sufficient ADME (absorption, distribution,
metabolism, elimination) properties, and acceptable toxicology
properties, to become a drug product that will successfully
complete human Phase I clinical trials. Drug-Like Properties:
Concepts, Structure Design and Methods from ADME to Toxicity
Optimization, Second Edition, provides scientists and students the
background and tools to understand, discover, and develop optimal
clinical candidates. This valuable resource explores physiochemical
properties, including solubility and permeability, before exploring
how compounds are absorbed, distributed, and metabolized safely and
stably. Review chapters provide context and underscore the
importance of key concepts such as pharmacokinetics, toxicity, the
blood-brain barrier, diagnosing drug limitations, prodrugs, and
formulation. Building on those foundations, this thoroughly updated
revision covers a wide variety of current methods for the screening
(high throughput), diagnosis (medium throughput) and in-depth (low
throughput) analysis of drug properties for process and product
improvement. From conducting key assays for interpretation and
structural analysis, the reader learns to implement modification
methods and improve each ADME property. Through valuable case
studies, structure-property relationship descriptions, and
structure modification strategies, Drug-Like Properties, Second
Edition, offers tools and methods for ADME/Tox scientists through
all aspects of drug research, discovery, design, development, and
optimization.
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