Title : Influence of P-glycoprotein on the disposition of fexofenadine and its enantiomers.

Pub. Date : 2017 Mar

PMID : 28090646






8 Functional Relationships(s)
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1 Influence of P-glycoprotein on the disposition of fexofenadine and its enantiomers. fexofenadine ATP binding cassette subfamily B member 1 Homo sapiens
2 Using fexofenadine as a model compound, we developed and validated HPLC-fluorescence methods to determine the effect of P-gp on the disposition of fexofenadine and its enantiomers. fexofenadine ATP binding cassette subfamily B member 1 Homo sapiens
3 Using fexofenadine as a model compound, we developed and validated HPLC-fluorescence methods to determine the effect of P-gp on the disposition of fexofenadine and its enantiomers. fexofenadine ATP binding cassette subfamily B member 1 Homo sapiens
4 KEY FINDINGS: This study demonstrates that P-gp prefers to transport (S)-fexofenadine, and P-gp deficiency causes the increase in both (R)-fexofenadine and (S)-fexofenadine in plasma. fexofenadine ATP binding cassette subfamily B member 1 Homo sapiens
5 KEY FINDINGS: This study demonstrates that P-gp prefers to transport (S)-fexofenadine, and P-gp deficiency causes the increase in both (R)-fexofenadine and (S)-fexofenadine in plasma. fexofenadine ATP binding cassette subfamily B member 1 Homo sapiens
6 Racemic fexofenadine, (R)-fexofenadine and (S)-fexofenadine were increased in ABCB1-1Delta Collies (118.7, 72.0 and 48.3 ng/ml) compared to wild-type Collies (25.0, 16.5 and 7.7 ng/ml) at 1 h postadministration. fexofenadine ATP binding cassette subfamily B member 1 Homo sapiens
7 Racemic fexofenadine, (R)-fexofenadine and (S)-fexofenadine were increased in ABCB1-1Delta Collies (118.7, 72.0 and 48.3 ng/ml) compared to wild-type Collies (25.0, 16.5 and 7.7 ng/ml) at 1 h postadministration. fexofenadine ATP binding cassette subfamily B member 1 Homo sapiens
8 The results demonstrate that the stereoselectivity of P-gp plays a key role in the disposition of fexofenadine enantiomers. fexofenadine ATP binding cassette subfamily B member 1 Homo sapiens