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Reactive Drug Metabolites (Hardcover)
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Reactive Drug Metabolites (Hardcover)
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Closing a gap in the scientific literature, this first
comprehensive introduction to the topic is based on current best
practice in one of the largest pharmaceutical companies worldwide.
The first chapters trace the development of our understanding of
drug metabolite toxicity, covering basic concepts and techniques in
the process, while the second part details chemical toxicophores
that are prone to reactive metabolite formation. This section also
reviews the various drug-metabolizing enzymes that can participate
in catalyzing reactive metabolite formation, including a discussion
of the structure-toxicity relationships for drugs. Two chapters are
dedicated to the currently hot topics of herbal constituents and
IADRs. The next part covers current strategies and approaches to
evaluate the reactive metabolite potential of new drug candidates,
both by predictive and by bioanalytical methods. There then follows
an in-depth analysis of the toxicological potential of the top 200
prescription drugs, illustrating the power and the limits of the
toxicophore concept, backed by numerous case studies. Finally, a
risk-benefit approach to managing the toxicity risk of reactive
metabolite-prone drugs is presented. Since the authors carefully
develop the knowledge needed, from fundamental considerations to
current industry standards, no degree in pharmacology is required
to read this book, making it perfect for medicinal chemists without
in-depth pharmacology training.
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