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    Drug Metab Dispos. 2005 May;33(5):619-22. Epub 2005 Feb 11.

    Possible involvement of organic anion transporter 2 on the interaction of theophylline with erythromycin in the human liver.

    Kobayashi Y, Sakai R, Ohshiro N, Ohbayashi M, Kohyama N, Yamamoto T.

    Source

    Department of Clinical Pharmacy, School of Pharmaceutical Sciences, Showa University, Shinagawa-ku, Tokyo, Japan.

    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 in 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 Xenopus oocytes, hOat2 mediated the transport of theophylline and erythromycin. The finding indicates that the two compounds are novel substrates for hOat2. The apparent K(m) values for the uptake of hOat2 that mediated the transport of theophylline and erythromycin were 12.6 muM and 18.5 muM, respectively. The hOat2-mediated uptake of [(14)C]theophylline and [(14)C]erythromycin was 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.

    PMID:
    15708966
    [PubMed - indexed for MEDLINE]
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