Liver-selective distribution in rats supports the importance of active uptake into the liver via organic anion transporting polypeptides (OATPs) in humans

Organic anion transporting polypeptide (OATP) 1B1 and 1B3 are key molecules that are involved in hepatic uptake related to drug elimination, and OATP-mediated drug interactions are of clinical concern. In this study, with an aim to determine a cutoff value for the potential involvement of OATP, we c...

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Veröffentlicht in:Drug metabolism and pharmacokinetics 2015-10, Vol.30 (5), p.334-340
Hauptverfasser: Mikkaichi, Tsuyoshi, Nakai, Daisuke, Yoshigae, Yasushi, Imaoka, Tomoki, Okudaira, Noriko, Izumi, Takashi
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Sprache:eng
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Zusammenfassung:Organic anion transporting polypeptide (OATP) 1B1 and 1B3 are key molecules that are involved in hepatic uptake related to drug elimination, and OATP-mediated drug interactions are of clinical concern. In this study, with an aim to determine a cutoff value for the potential involvement of OATP, we collected data on the distribution of 12 human OATP and 24 non-OATP radiolabeled substrates in rats. The OATP substrates exhibited a higher tissue-to-plasma ratio (Kp) in the liver than that in the other tissues. As an index of liver-specific distribution, a hepatic Kp ratio (the ratio of Kp in the liver to that in other tissues) was introduced, and a hepatic Kp ratio
ISSN:1347-4367
1880-0920
DOI:10.1016/j.dmpk.2015.06.003