Title : Vectorial transport of fexofenadine across Caco-2 cells: involvement of apical uptake and basolateral efflux transporters.

Pub. Date : 2011 Oct 3

PMID : 21780830






4 Functional Relationships(s)
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1 Studies with cellular models expressing single transporters showed that OATP2B1 expression stimulated uptake of fexofenadine at pH 6.0. fexofenadine solute carrier organic anion transporter family member 2B1 Homo sapiens
2 Apical uptake of fexofenadine into Caco-2 cells was decreased by 45% by pretreatment with estrone 3-sulfate, an OATP inhibitor, at pH 6.0 but not at pH 7.4, indicating that OATP2B1 mediates apical uptake of fexofenadine into these cells. fexofenadine solute carrier organic anion transporter family member 2B1 Homo sapiens
3 Apical uptake of fexofenadine into Caco-2 cells was decreased by 45% by pretreatment with estrone 3-sulfate, an OATP inhibitor, at pH 6.0 but not at pH 7.4, indicating that OATP2B1 mediates apical uptake of fexofenadine into these cells. fexofenadine solute carrier organic anion transporter family member 2B1 Homo sapiens
4 The results provide a novel insight into a vectorial transport system mainly consisting of apical OATP2B1 and basolateral MRP3 that may play an important role in delivering hydrophilic anionic and zwitterionic drugs such as pravastatin and fexofenadine into systemic circulation upon oral administration. fexofenadine solute carrier organic anion transporter family member 2B1 Homo sapiens