{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,9,29]],"date-time":"2026-09-29T20:42:31Z","timestamp":1790714551112,"version":"4.1.0"},"reference-count":34,"publisher":"Ovid Technologies (Wolters Kluwer Health)","issue":"1","license":[{"start":{"date-parts":[[2002,7,1]],"date-time":"2002-07-01T00:00:00Z","timestamp":1025481600000},"content-version":"tdm","delay-in-days":0,"URL":"http:\/\/doi.wiley.com\/10.1002\/tdm_license_1.1"},{"start":{"date-parts":[[2003,12,30]],"date-time":"2003-12-30T00:00:00Z","timestamp":1072742400000},"content-version":"vor","delay-in-days":547,"URL":"http:\/\/onlinelibrary.wiley.com\/termsAndConditions#vor"}],"funder":[{"DOI":"10.13039\/501100001711","name":"Swiss National Science Foundation","doi-asserted-by":"crossref","award":["3200-065173.01"],"award-info":[{"award-number":["3200-065173.01"]}],"id":[{"id":"10.13039\/501100001711","id-type":"DOI","asserted-by":"crossref"}]},{"name":"Karin Fattinger is a recipient of a SCORE A Career Development Award from the Swiss National Science Foundation"}],"content-domain":{"domain":["lww.com","ovid.com"],"crossmark-restriction":true},"short-container-title":[],"published-print":{"date-parts":[[2002,7]]},"abstract":"<jats:sec>\n            <jats:title\/>\n            <jats:p>The antibiotics rifamycin SV and rifampicin substantially reduce sulfobromophthalein (BSP) elimination in humans. In rats, rifamycin SV and rifampicin were shown to interfere with hepatic organic anion uptake by inhibition of the organic anion transporting polypeptides Oatp1 and Oatp2. Therefore, we investigated the effects of rifamycin SV and rifampicin on the OATPs of human liver and determined whether rifampicin is a substrate of 1 or several of these carriers. In complementary RNA (cRNA)-injected <jats:italic toggle=\"yes\">Xenopus laevis<\/jats:italic> oocytes, rifamycin SV (10 \u03bcmol\/L) <jats:italic toggle=\"yes\">cis<\/jats:italic>-inhibited human organic anion transporting polypeptide C (<jats:italic toggle=\"yes\">SLC21A6<\/jats:italic>) (OATP-C), human organic anion transporting polypeptide 8 (<jats:italic toggle=\"yes\">SLC21A8<\/jats:italic>) (OATP8), human organic anion transporting polypeptide B (<jats:italic toggle=\"yes\">SLC21A9<\/jats:italic>) (OATP-B), and human organic anion transporting polypeptide A (<jats:italic toggle=\"yes\">SLC21A3<\/jats:italic>) (OATP-A) mediated BSP uptake by 69%, 79%, 89%, and 57%, respectively, as compared with uptake into control oocytes. In the presence of 100 \u03bcmol\/L rifamycin SV, BSP uptake was almost completely abolished. Approximate <jats:italic toggle=\"yes\">Ki\n                                 <\/jats:italic> values were 2 \u03bcmol\/L for OATP-C, 3 \u03bcmol\/L for OATP8, 3 \u03bcmol\/L for OATP-B and 11 \u03bcmol\/L for OATP-A. Rifampicin (10 \u03bcmol\/L) inhibited OATP8-mediated BSP uptake by 50%, whereas inhibition of OATP-C-, OATP-B-, and OATP-A-mediated BSP transport was below 15%. 100 \u03bcmol\/L rifampicin inhibited OATP-C- and OATP8-, OATP-B- and OATP-A-mediated BSP uptake by 66%, 96%, 25%, and 49%, respectively. The corresponding <jats:italic toggle=\"yes\">Ki\n                                 <\/jats:italic> values were 17 \u03bcmol\/L for OATP-C, 5 \u03bcmol\/L for OATP8, and 51 \u03bcmol\/L for OATP-A. Direct transport of rifampicin could be shown for OATP-C (apparent <jats:italic toggle=\"yes\">Km\n                                 <\/jats:italic> value 13 \u03bcmol\/L) and OATP8 (2.3 \u03bcmol\/L). In conclusion, these results show that rifamycin SV and rifampicin interact with OATP-mediated substrate transport to different extents. Inhibition of human liver OATPs can explain the previously observed effects of rifamycin SV and rifampicin on hepatic organic anion elimination.<\/jats:p>\n          <\/jats:sec>","DOI":"10.1053\/jhep.2002.34133","type":"journal-article","created":{"date-parts":[[2003,2,17]],"date-time":"2003-02-17T22:18:10Z","timestamp":1045520290000},"page":"164-172","update-policy":"https:\/\/doi.org\/10.1097\/lww.0000000000001000","source":"Crossref","is-referenced-by-count":321,"title":["Interactions of rifamycin SV and rifampicin with organic anion uptake systems of human liver"],"prefix":"10.1097","volume":"36","author":[{"given":"Stephan R.","family":"Vavricka","sequence":"first","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Jessica","family":"Van Montfoort","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Huy Riem","family":"Ha","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Peter J.","family":"Meier","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Karin","family":"Fattinger","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"276","reference":[{"key":"10.1053\/jhep.2002.34133-BIB1|cit1","volume-title":"The Use of Antibiotics: A Clinical Review of Antibacterial, Antifungal and Antiviral Drugs","author":"Kucers","year":"1997"},{"key":"10.1053\/jhep.2002.34133-BIB2|cit2","volume-title":"Swiss Pharmaceutical Society. 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