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First published on February 11, 2005; DOI: 10.1124/dmd.104.003301

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Received for publication December 21, 2004.
Revised February 8, 2005.
Accepted for publication February 9, 2005.

Possible Involvement of Organic Anion Transporter 2 on the Interaction of Theophylline with Erythromycin in the Human Liver

Yasuna Kobayashi 1, Ryoko Sakai 1, Naomi Ohshiro 2, Masayuki Ohbayashi 1, Noriko Kohyama 1, Toshinori Yamamoto 1*

1 SHOWA UNIVERSITY 2 University of Texas Medical Branch

* Address correspondence to: E-mail: yamagen{at}pharm.showa-u.ac.jp

Abstract

ABSTRACT: Organic anion transporter 2 (Oat2 [SLC22A7]) is a multispecific organic anion transporter. Although several substrates of human Oat2 (hOat2) have been elucidated, a possible involvement of hOat2 on the drug interaction is less defined. The purpose of this study was to investigate the interaction of theophylline with erythromycin mediated by hOat2 using a Xenopus laevis oocyte expression system. When expressed in X. oocytes, hOat2 mediated the transport of theophylline and erythromycin. The finding indicates that the two compounds are novel substrates for hOat2. The apparent Km values for the uptake of hOat2 which mediated the transport of theophylline and erythromycin were 18.5 µM and 12.6 µM, respectively. The hOat2-mediated uptake of [14C]theophylline and [14C]erythromycin were cis-inhibited by adding erythromycin and theophylline, respectively. Our present findings suggest that hOat2 may, at least in part, be involved in the theophylline-erythromycin interaction in the human liver.


Key words: ABC transporters, drug transport, drug-drug interactions, hepatic transport, hepatic uptake, liver disease, liver toxicity, membrane transport, organic anion transport, transporters


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[Abstract] [Full Text] [PDF]


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