ABC Pumps and Their Role in Active Drug Transport

Author(s): Nicola A. Colabufo, Francesco Berardi, Marialessandra Contino, Mauro Niso, Roberto Perrone

Journal Name: Current Topics in Medicinal Chemistry

Volume 9 , Issue 2 , 2009

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Pharmacokinetic limitations affect drug bioavailability determining the loss or the reduction of the pharmacological effects. The Gastro Intestinal tract (GI) and the Blood Brain Barrier (BBB) are the most important restrictive and selective physiological lines of defense of the organism. Although several parameters such as LogP, LogD and Ka have been extensively employed for determining drug bioavailability, the active transports, present in these biological barriers, play an important role for dosing and limiting cell drugs concentration. In particular, ATP Binding Cassette (ABC) transporters are involved in the active transport both in GI and BBB. Their strategic activity and biochemical and pharmacological role are herein treated.

Keywords: Blood brain barrier, ABC transporters, P-glycoprotein, MRPs, drug absorption and disposition

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Article Details

Year: 2009
Page: [119 - 129]
Pages: 11
DOI: 10.2174/156802609787521553
Price: $65

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