Drug metabolism & Pharmacokinetic Research has become an integral part of drug discovery and development. The major goal of this work is to attempt to optimize the metabolism and pharmacokinetic properties of new chemical entities in parallel with the optimization of the pharmacological characteristics (potency and efficacy). Ultimately this should result in a potential drug candidate and years later into a drug therapy.

Good understanding and appropriate optimization of metabolism and pharmacokinetic properties has numerous benefits;

1. good absorption and low clearance will reduce the overall necessary dose (tablet size)
2. a half-life that supports once a day dosing with adequate duration of action will improve patient compliance.
3. anticipating potential drug-drug interactions
4. minimizing the formation of reactive metabolites that may mediate acute or idiosyncratic toxicities.
5. improved human dose projections and hence reducing risk upon entry into clinical development
6. metabolite characterization to understand relevance towards pharmacological activity against the target and/or off-target activity.
7. understand and minimize drug metabolism / transporter mediated toxicities.

This are only a few considerations why drug metabolism and pharmacokinetics are key to the successful drug development. During the presentation several of these considerations will be covered in more depth.