The application of these technologies will dramatically enhance the efficiency of lead discovery as well as improve the quality of the resultant drug candidates, thereby not only reducing their risk of failure in development but ultimately resulting in the creation of better medicines. And of the drugs that are actually successfully developed, an alarming number still suffer deficiencies that are sufficient to warrant labeling on their drug package insert. It is apparent that significant bottlenecks remain in the drug discovery process, in particular in the later stages of lead discovery, which are centered on the analysis of the ADME and overt toxicity properties of drug compounds. Absorption generally refers to the amount of drug compound that enters the portal vein following oral administration. The transfer of compound from the site of administration to the total systemic circulation and then to the various tissues of the body is called distribution .
Metabolism is the enzymatic conversion of one chemical species to another.
Elimination is the removal of compounds from the body via a number of pathways, primarily through urine and bile. Tox Profiles ADME profiles refer to the drug concentration at various sites in the body over time. The cumulative effects of rate of absorption, distribution, metabolism, and elimination determine drug concentration at the intended site. Tox profiles refer to the toxic side effect of the drug on various tissues. Combinatorial Chemistry Combinatorial chemistry is the process by which large libraries of drug-like molecules, based upon a shared chemistry, can be efficiently assembled in modular fashion using sets of individual building blocks or monomers.