Transporters as Targets for Drug Delivery

For several therapeutic purposes, it is desirable to aim for excretion of drugs via canalicular transporters. First, delivery of drugs to bile can promote drug action in the biliary tree. Second, it may be attractive in terms of pharmacokinetics to have a drug that undergoes enterohepatic circulation that involves transport via canalicular transporters. Examples of these applications will be discussed hereafter. 

Surgery is currently the only treatment option for biliary tract cancer. Patients with 

Therefore, total inhibition of ABCC2 in humans could also lead to increased absorbance of PhIP and its metabolites. 

2 Dubin. I.N. and Johnson, F.B. (1954) Chronic idiopathic jaundice with unidentified pigment in liver cells a new clinicopathologic entity with a report of 12 cases. Medicine, 33 (3), 155-197. 

5 Paulusma, C.C., van Geer, M.A., Evers, R., Heijn, M., Ottenhoff, R. Borst, P. et al. (1999) Canalicular multispecific organic anion transporter/multidrug resistance protein 2 mediates low-affinity transport of reduced glutathione. The Biochemical Journal, 338 (Pt 2), 393-401. 

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