Bioanalysis Zone

Simultaneous qualitative and quantitative metabolism data generation: a convenient marriage?

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“For the [qual/quan] concept to truly revolutionize drug discovery, a way must be found to successfully combine the expertise encompassed within the biotransformation and high-throughput bioanalysis disciplines.”

As high-throughput screening approaches have accelerated the identification of potential lead compounds and series, so the desire to generate rapid information to impact drug design has increased. An understanding of metabolic clearance has long been recognized as a fundamental pillar of drug design, incorporating knowledge of intrinsic rates of metabolism, sites of metabolic vulnerability, enzymology and the impact of metabolic pathways (typically in terms of metabolite pharmacology and safety). In recent years, the revolution in automated bioanalytical approaches has enabled the routine generation of rapid absorption, distribution, metabolism, and excretion (ADME) data, providing potentially key information on the metabolism of novel compounds, as well as other important criteria, such as disposition and safety.

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