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Mass Spectrometry in Drug Metabolism and Pharmacokinetics Book

EBook NameMass Spectrometry in Drug Metabolism and Pharmacokinetics Book
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EBook Category Category: Pharmacology

EBook Description: The first step in discovering a new medicine is to identify a therapeutic target. Drugs in today’s market as well as those in recent clinical testing target less than 500 biomolecules, with more than 10 times that many potential therapeutic targets waiting to be discovered and developed (Drews, 2000). More than 50% of the newly approved drugs result from R&D involving previously clinically tested and validated targets. Once a target has been validated (proven to be related to the disease process), high-throughput screening methods may be used to determine initial structural leads. Compounds are assessed for target affinity and for their “druglike” properties, including absorption, distribution, metabolism, and excretion (ADME) using a series of in vivo and in vitro tests. The results of these tests are used to improve the structure and therefore the properties of the next round of test compounds, until ultimately one or more acceptable compounds are advanced forward in the process. This stage of discovery, which can be lengthy and difficult to predict, is generally referred to as lead optimization.

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