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Current Drug Metabolism


ISSN (Print): 1389-2002
ISSN (Online): 1875-5453

Clinical Pharmacokinetic and Metabolism of PET Radiotracers for Imaging P-glycoprotein in Chemoresistant Tumor of Colorectal Cancer

Author(s): Mariangela Cantore, Elena Capparelli, Francesco Berardi, Roberto Perrone and Nicola Antonio Colabufo

Volume 12, Issue 10, 2011

Page: [985 - 988] Pages: 4

DOI: 10.2174/138920011798062292

Price: $65


The pharmacological treatment of colorectal tumour leads to MultiDrug Resistance due to overexpression of several ABC transporters such as P-glycoprotein and some Multidrug associated Resistance Proteins (MRPs) that are able to efflux the chemotherapeutic agent out of the cell. A strategy to reverse MDR is the co-administration of antineoplastic agent with a P-glycoprotein inhibitor. These inhibitors are an useful tool for investigating, by PET, the expression and the activity of P-gp and MRPs that are overexpressed in chemoresistant colorectal tumor cells. In this review will be focused the aspect on P-gp and MRPs ligands employed as PET radiotracers considering their pharmacokinetic pharmacodynamic profile and their selectivity towards ABC transporters involved in chemoresistant cell of colorectal tumour.

Keywords: Colorectal, cancer, PET, P-glycoprotein, MultiDrug Resistance, 11-C radiotracers, Everted gut sac, neuroblastoma, epipodophyllotoxins, Nucleotide Binding domains (NBDs)

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