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Efflux and uptake transporters involved in the disposition of bazedoxifeneTrdan Lušin, Tina ...Bazedoxifene, a novel selective estrogen receptor modulator, has complex pharmacokinetics with rapid absorption, high metabolic clearance, low oral bioavailability (6.25 %) and a slow elimination ... phase. Our hypothesis is that drug uptake and efflux transporters may play an important role in its disposition. To adequately cover all aspects of bazedoxifene transport, several approaches were undertaken: PAMPA assay, ATPase assay, membrane inside-out vesicles and Caco-2 and CHO cell lines. The results obtained from PAMPA experiments showed moderate passive permeability of bazedoxifene (P app 2 10-6cm/s), suggesting the existence of an active transport during the rapid absorption phase. The Caco-2 transport assay showed large and significant changes in the measured efflux ratios of bazedoxifene when selective transporter inhibitors were applied: verapamil (a Pgp inhibitor), MK 571 (an MRP inhibitor), Ko143 (a BCRP inhibitor) and DIDS (an OATP inhibitor). Additionally, membrane preparation experiments demonstrated the interaction of bazedoxifene with P-gp, MRP2 and BCRP. CHO experiments did not show any interactions of bazedoxifene with OATP1B1 or OATP1B3; therefore, bazedoxifene may be a substrate of other OATP isoform(s). The comprehensive in vitro study indicates a strong involvement of Pgp, MRP, BCRP and OATP in bazedoxifene disposition.Source: European journal of drug metabolism and phamacokinetics. - ISSN 0378-7966 (Vol. 41, iss. 3, 2016, str. 251-257)Type of material - article, component partPublish date - 2016Language - englishCOBISS.SI-ID - 3814513
Author
Trdan Lušin, Tina |
Mrhar, Aleš |
Stieger, Bruno |
Kristl, Albin |
Berginc, Katja, 1980- |
Trontelj, Jurij
Topics
Farmakokinetika |
bazedoxifene |
efflux transporters |
uptake transporters
source: European journal of drug metabolism and phamacokinetics. - ISSN 0378-7966 (Vol. 41, iss. 3, 2016, str. 251-257)
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Database name | Field | Year |
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Links to authors' personal bibliographies | Links to information on researchers in the SICRIS system |
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Trdan Lušin, Tina | 30817 |
Mrhar, Aleš | 06086 |
Stieger, Bruno | |
Kristl, Albin | 11122 |
Berginc, Katja, 1980- | 25492 |
Trontelj, Jurij | 23420 |
Source: Personal bibliographies
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