Catalog No.S3208 Synonyms: MDL 16455A
Molecular Weight(MW): 538.12
Fexofenadine inhibits histamine H1 receptor with IC50 of 246 nM.
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Choose Selective Histamine Receptor Inhibitors
|Description||Fexofenadine inhibits histamine H1 receptor with IC50 of 246 nM.|
Fexofenadine exhibits a potent and concentration-dependent anti-anaphylactic activity with an IC50 value of 95.5nM. Fexofenadine shows only a weak competitive antagonist behaviour for the 5-HT2A receptorsfrom rat caudal artery with pA2 of 5.2.  All four P-gp inhibitors has a strong, concentration-dependent effect on the Papp of fexofenadine in both directions in the Caco-2 cell model. The IC50 of verapamil is 8.44 mM on the P-gp-mediated secretion of Fexofenadine.  Fexofenadine causes a significant increase in the QT and Tp-e intervals and receives a significant TdP score at doses greater than 100 fold its free TPC in the rabbit left ventricular wedge preparation. 
|In vivo||Fexofenadine is excreted unchanged in the urine, bile, and gastrointestinal tract, indicating minimal metabolism in rats, making it an ideal probe to study transport processes. Coadministration of Fexofenadine with Ketoconazole increases the oral exposure of Fexofenadine by 187% in rats. In contrast, coadministration of Fexofenadine with orange juice or apple juice to rats decreases the oral exposure of Fexofenadine by 31% and 22%, respectively. Increasing the quantity of orange or apple juice administered further decreases the oral exposure of Fexofenadine, by 40% and 28%, respectively.  Biliary excretion clearance of Fexofenadine (17 ml/min/kg) accounts for almost 60% of the total body clearance (30 ml/min/kg) in mice. Knockout mice of Mdr1a/1b P-gp does not affect the biliary excretion clearance with regard to both plasma and liver concentrations, whereas the absence of P-gp causes a 6-fold increase in the plasma concentration and 3-fold higher brain-to-plasma concentration ratio after oral administration. |
|In vitro||DMSO||107 mg/mL (198.84 mM)|
|Ethanol||107 mg/mL (198.84 mM)|
|Water||2 mg/mL (3.71 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02908750||Not yet recruiting||Non Small Cell Lung Cancer||AstraZeneca|Quintiles, Inc.||January 2017||Phase 1|
|NCT03012763||Completed||Pharmacokinetics|Magnetic Resonance Imaging|Administration, Oral||University Medicine Greifswald||April 2016||Phase 1|
|NCT02391688||Completed||Drug Interaction||Jules Desmeules|University Hospital, Geneva||November 2014||Phase 1|
|NCT02157558||Completed||Drug Interactions||Lexicon Pharmaceuticals||July 2014||Phase 1|
|NCT02175485||Completed||Rhinitis Allergic||Sanofi||June 2014||Phase 4|
|NCT02551536||Completed||Allergic Rhinitis||Indira Gandhi Medical College||April 2014||Phase 4|
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