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

[ Vol. 12 , Issue. 10 ]

Author(s):

Mariangela Cantore, Elena Capparelli, Francesco Berardi, Roberto Perrone and Nicola Antonio Colabufo   Pages 985 - 988 ( 4 )

Abstract:


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)

Affiliation:

Dipartimento Farmacochimico, Universita degli Studi di Bari, via Orabona 4, 70125, Bari, Italy.



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