Hit and lead profiling

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This comprehensive reference outlines current methods for generating pharmacokinetic and safety profiles of drug candidates, emphasizing the balance needed for optimal candidate selection. It begins with an introduction to the filtering and risk assessment of potential drug molecules before development. The text is divided into two main sections: pharmacological (ADME) and safety (toxicity) profiling. The ADME section discusses essential physicochemical parameters like solubility and permeability, alongside complex traits such as drug-drug interactions, metabolic clearance, and protein binding. The toxicology section highlights recent advancements in genetic toxicity testing, bioactivation screening, and organ-specific toxicity assays for the liver, heart, kidneys, and blood, as well as autoimmune reaction profiling. By addressing both drug efficacy and safety, this practical guide illustrates how each aspect influences critical decisions in the drug development process. It serves as a complete toolbox for assessing the risk/benefit ratio of novel compounds during early development stages, utilizing both in vitro and in silico methods. Authored by experts from leading pharmaceutical companies, it provides invaluable insights for medicinal chemists and drug developers.