Bernard Testa, Han Walker, Gerd Folkers, Richard Guy, "Pharmacokinetic Optimization in Drug Research"
2002 | pages: 643 | ISBN: 3906390225 | PDF | 5,8 mb
In our age of combinatorial chemistry and high-throughput technologies, bioactive compounds called ‘hits' are discovered by the thousands. However, the road is very long indeed that leads from hits to lead compounds and then to pharmacokinetically well-behaved clinical and drug candidates. As a result, the screening, design, and optimization of pharmacokinetic properties has become a bottleneck and a major challenge in drug research. To shorten the time-consuming development and high rate of attrition of active com-pounds ultimately doomed by hidden pharmacokinetic defects, drug research-ers are coming to incorporate structure-permeation, structure-distribution, structure-metabolism, and structure-toxicity relations into drug-design strate-gies. To this end, powerful biological, physicochemical, and computational strategies are being developed the objectives of which are to increase the clin-ical relevance of drug design and to eliminate as early as possible compounds with unfavorable physicochemical properties, pharmacokinetic profiles, or toxicity.
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