| Making effective use of pharmacokinetic
information to improve drug discovery productivity
For a compound to become a successful drug, it needs not only to
perform the right molecular interactions with its target to make
it effective, but also to be processed correctly by the body. For
the majority of projects the ideal compound is soluble, able to
pass through the gut wall, not broken down too quickly by liver
enzymes and have a minimal affinity to fatty tissues and blood proteins.
Collectively these properties are known as the ADME properties (for
absorption, distribution, metabolism and excretion) and getting
the right blend is critical to success.
Traditionally, testing compounds to see if they had the right ADME
properties was carried out on relatively few compounds at a time,
often using full animal studies. Now, the industry is turning to
faster, more cost-efficient evaluation methods in order to screen
the glut of compounds that have arisen as a result of advances in
target discovery and chemical synthesis.
But simply generating large spreadsheets of ADME data for all the
compounds in the discovery bottleneck is only part of the solution.
What drug discovery researchers really need to know is whether a
compound will exist in the body long enough to have a therapeutic
effect - referred to as its pharmacokinetics. In this section we
describe our experimental in vitro ADME screening technologies and
how we can use these results for accurate pharmacokinetic prediction.
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