Scientific Report 2007

Scripps Florida

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Translational Research Institute

Drug Metabolism and Pharmacokinetics Laboratory

M.D. Cameron, L. Lin, C. Ruiz, S. Khan

The Drug Metabolism and Pharmacokinetics Laboratory at Scripps Florida provides in vitro and in vivo evaluation of the pharmacokinetic and pharmacodynamic properties of new chemical entities. We work on project teams within the Drug Discovery group of the Department of Molecular Therapeutics and support chemistry efforts within the Scripps Research Institute Molecular Screening Center. We help bridge medicinal chemistry and pharmacology by evaluating the metabolic fate and identifying the liabilities of compounds. Pharmacokinetic studies provide basic parameters, including peak plasma concentration, bioavailability, exposure, half-life, clearance, volume of distribution, and tissue distribution. Research interests include P450 structure-function relationships and the formation of reactive intermediates during metabolism. The laboratory is equipped with liquid chromatography–tandem mass spectrometry system and a Q-trap hybrid triple quadrupole/linear ion-trap mass spectrometer.

Publications

Cameron, M.D., Wright, J., Black, C.B., Ye, N. In vitro prediction and in vivo verification of enantioselective human tofisopam metabolite profiles. Drug Metab. Dispos., in press.

Feng, Y., Cameron, M.D., Frackowiak, B., Griffin, E., Lin, L., Ruiz, C., Schröter, T., LoGrasso, P. Structure-activity relationships, and drug metabolism and pharmacokinetic properties for indazole piperazine and indazole piperidine inhibitors of ROCK-II. Bioorg. Med. Chem. Lett. 17:2355, 2007.