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An appropriate drug metabolism and pharmacokinetic (DMPK) profile
remains a major hurdle to reducing risk and improving productivity in
pharmaceutical R&D; accounting for about 40% of all drug failures. For
orally administered drugs, failure is often attributable to low
intestinal absorption and/or high clearance causing poor and variable
bioavailability. Additional reasons for failure include drug-drug
interactions and the presence of active metabolites. With a poor
pharmacokinetic profile, it can be difficult to achieve the dose
profile required for therapeutic efficacy. The main role of DMPK in
discovery is therefore the prediction of drug metabolism and
pharmacokinetics in humans. Successful prediction can be expected to
reduce the rate of attrition during drug discovery and development. It
is therefore now considered and essential component of the drug
discovery process. Because of this, along with the need to screen and
ever greater numbers of compounds, there have been major changes in
both technology and market dynamics.
DMPK issues are a major cause of compound attrition.
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