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Background:  The metabolism of tyrosine kinase inhibitors (TKIs) is mainly mediated via hepatic route, but the mechanism responsible for their hepatocellular accumulation is still unknown. This study was designed to understand the contribution of organic anion transporting polypeptides (OATPs) in the hepatic uptake of selected TKIs – pazopanib, canertinib, erlotinib, vandetanib and nilotinib.

Role of OATP-1B1 and/or OATP-1B3 in hepatic disposition of tyrosine kinase inhibitors