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Monocarboxylate Transporters in Drug Disposition: Characterization, Regulation and Significance
Monday, November 12
2:00 pm – 4:30 pm
Symposium
ACPE #073-999-07-551-L04
Monocarboxylate anions are important metabolic products, as well as representing important drugs and naturally occurring dietary compounds. Since these compounds are largely ionized at physiological pH values, they do not freely diffuse across membranes, requiring transport mechanisms to facilitate their transport across membranes. Although organic anion transporters (OATs) have been well studied, the same is not true for monocarboxylic acid transporters (MCTs). Our knowledge with regards to the importance of MCTs in drug and botanical (plant-derived compounds) is limited, although studies have indicated that MCTs may be important for the transport of flavonoids and for the drugs, valproic acid, nonsteroidal anti-inflammatory drugs, beta-lactam antibiotics, phenethicillin and 6-mercaptopurine. Drug delivery by targeting MCT1 in the intestine has been used to successfully increase the bioavailability of gabapentin. The MCT family may also represent an important therapeutic target, as MCT1 has been identified as a new immunosuppression target. This symposium will include presentations on both the monocarboxylate proton-coupled transporters (SLC16 family) and the sodium-dependent transporters (two members of the SLC5A family). Presentations will address the characterization, function and regulationof MCTs in the body, and the importance of MCTs in health, disease and drug transport, pharmacokinetics and biopharmaceutics.
Moderators
Marilyn E. Morris, Ph.D.
University at Buffalo, State University of New York
Reina Bendayan, Pharm.D.
University of Toronto
Overview of the Proton-coupled MCT (SLC16) Family of Transporters: Characterization, Function and Role in Drug Transport
Marilyn E. Morris, Ph.D.
University at Buffalo, State University of New York
Monocarboxylate Transporters in the Central Nervous System: Distribution, Regulation and Function
Lester R. Drewes, Ph.D.
University of Minnesota Medical School, Duluth
Sodium-coupled MCTs: Role in Health and Disease and in Drug Transport
Vadivel Ganapathy, Ph.D.
Medical College of Georgia
Targeting the MCT Transporter in Drug Delivery to Increase Bioavailability
Mark S. Warren, Ph.D.
Xenoport, Inc.