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Institute for Applied Cancer Science

Drug Metabolism and Pharmacokinetics

The drug metabolism and pharmacokinetics (DMPK) group ensures that novel therapeutics developed by IACS scientists are safe, effective and stable enough to be dosed to humans. To be therapeutically effective, a drug must reach the protein target in the tumor for a sufficient amount of time and at a specific concentration. It also need to be devoid of any impact on other co-administered medicines.

A drug’s journey generally begins in the stomach where it arrives after being swallowed and subsequently gets absorbed from the gastro-intestinal tract. A drug must have properties that promote stable circulation in the blood, prevent degradation by metabolic enzymes, and to avoid elimination by efflux transporters, present in the body (most notably the liver). Once the drug has reached the site of action within the tumor, the compound must cross the cell membrane to engage the protein of interest.

To ensure that candidate drug compounds have all the necessary properties to become an approved drug, the DMPK scientists use a variety of high-throughput in vitro, as well as limited in vivo preclinical studies, to help the project team identify the right compound to advance into clinical testing. They use sophisticated analytical chemistry and mass spectroscopy techniques.

Besides examining the pharmacokinetic properties of new agents, DMPK scientists also ensure that no drug-drug interactions occur. Drug interactions can influence pharmacokinetics of other co-adminstered agents either increasing exposure (which can lead to toxicity) or by accelerating metabolism of a second agent (making it ineffective).

© 2015 The University of Texas MD Anderson Cancer Center