PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 24396144-11 2014 Inhibiting P-gp-mediated efflux by elacridar in in vitro experiments significantly decreased fexofenadine efflux from hepatocytes, resulting in an increase in apparent fexofenadine uptake. fexofenadine 93-105 phosphoglycolate phosphatase Homo sapiens 11-15 25020133-8 2014 Interestingly, the expression of iNOS and eNOS mRNA was increased in aortas of mice on high doses of cetirizine or fexofenadine. fexofenadine 115-127 nitric oxide synthase 3, endothelial cell Mus musculus 42-46 24549825-1 2014 PURPOSE: OATP2B1-mediated grapefruit juice (GFJ)-drug interactions are substrate-dependent; for example, GFJ ingestion significantly reduces bioavailability of fexofenadine, but not pravastatin. fexofenadine 160-172 solute carrier organic anion transporter family member 2B1 L homeolog Xenopus laevis 9-16 24549825-5 2014 RESULTS: OATP2B1-mediated uptake of pravastatin and fexofenadine exhibited biphasic saturation kinetics, indicating the presence of MBS on OATP2B1. fexofenadine 52-64 solute carrier organic anion transporter family member 2B1 L homeolog Xenopus laevis 9-16 24549825-5 2014 RESULTS: OATP2B1-mediated uptake of pravastatin and fexofenadine exhibited biphasic saturation kinetics, indicating the presence of MBS on OATP2B1. fexofenadine 52-64 solute carrier organic anion transporter family member 2B1 L homeolog Xenopus laevis 139-146 24549825-9 2014 These findings indicate that only fexofenadine is expected to interact with GFJ on OATP2B1 at therapeutic concentrations, in accordance with the clinical observations. fexofenadine 34-46 solute carrier organic anion transporter family member 2B1 L homeolog Xenopus laevis 83-90 24396144-11 2014 Inhibiting P-gp-mediated efflux by elacridar in in vitro experiments significantly decreased fexofenadine efflux from hepatocytes, resulting in an increase in apparent fexofenadine uptake. fexofenadine 168-180 phosphoglycolate phosphatase Homo sapiens 11-15 24138758-8 2013 Fexofenadine (a peripherally acting histamine H1 receptor antagonist) reduced MM activity in normal mice. fexofenadine 0-12 histamine receptor H1 Mus musculus 36-57 24782370-1 2014 OBJECTIVE: To establish a precolumn chiral derivatization method for determination of fexofenadine enantiomers, a chiral substrate of OATP1B1, in cellular model. fexofenadine 86-98 solute carrier organic anion transporter family member 1B1 Homo sapiens 134-141 24423593-2 2014 P-gp (fexofenadine) and CYP-specific substrates (caffeine for CYP1A2, bupropion for CYP2B6, flurbiprofen for CYP2C9, omeprazole for CYP2C19, dextromethorphan for CYP2D6 and midazolam for CYP3A4) and their metabolites were extracted from DBS (10 microl) using methanol. fexofenadine 6-18 ATP binding cassette subfamily B member 1 Homo sapiens 0-4 24040855-0 2013 The role of multidrug resistance-1 (MDR1) variants in response to fexofenadine among Jordanians. fexofenadine 66-78 ATP binding cassette subfamily B member 1 Homo sapiens 12-34 24040855-0 2013 The role of multidrug resistance-1 (MDR1) variants in response to fexofenadine among Jordanians. fexofenadine 66-78 ATP binding cassette subfamily B member 1 Homo sapiens 36-40 24040855-2 2013 The P-gp has wide substrate specificity for multiple medications, including the antiallergic drug fexofenadine. fexofenadine 98-110 ATP binding cassette subfamily B member 1 Homo sapiens 4-8 24040855-3 2013 In this study, we investigated the possible association between three common MDR1 gene polymorphisms (G2677T, C3435T, and C1236T), and the anti-allergic effect of fexofenadine among Jordanians. fexofenadine 163-175 ATP binding cassette subfamily B member 1 Homo sapiens 77-81 24040855-11 2013 CONCLUSIONS: The MDR1 gene polymorphism C1236T was associated with the anti-allergic effect of fexofenadine among male Jordanians. fexofenadine 95-107 ATP binding cassette subfamily B member 1 Homo sapiens 17-21 23369146-8 2013 The fentanyl-induced enhancement of the number of citric acid-induced coughs was abolished in mice that had been pretreated with moguisteine, a rapidly adapting receptor (RAR) antagonist or fexofenadine, a histamine H1 receptor antagonist. fexofenadine 190-202 histamine receptor H1 Mus musculus 206-227 23422332-7 2013 Fexofenadine was used as a P-gp phenotyping probe. fexofenadine 0-12 ATP binding cassette subfamily B member 1 Homo sapiens 27-31 23422332-15 2013 In the placebo phase, T1/2 of fexofenadine in ABCB1 3435T mutation allele carriers was longer compared to ABCB1 3435CC carriers (4.43+-1.44h vs. 2.54+-0.21h, p<0.05). fexofenadine 30-42 ATP binding cassette subfamily B member 1 Homo sapiens 46-51 21646440-2 2012 The purpose of this study was to determine the influence of Panax ginseng on CYP3A and P-gp function using the probe substrates midazolam and fexofenadine, respectively. fexofenadine 142-154 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 77-82 23115085-5 2013 Rifampicin inhibited the uptake of fexofenadine enantiomers by human hepatocytes via organic anion transporter (OAT) OATP1B3 and its basal-to-apical transport in Caco-2 cells, but not OAT3-mediated or multidrug and toxic compound extrusion 1 (MATE1)-mediated transport. fexofenadine 35-47 solute carrier organic anion transporter family member 1B3 Homo sapiens 117-124 23115085-5 2013 Rifampicin inhibited the uptake of fexofenadine enantiomers by human hepatocytes via organic anion transporter (OAT) OATP1B3 and its basal-to-apical transport in Caco-2 cells, but not OAT3-mediated or multidrug and toxic compound extrusion 1 (MATE1)-mediated transport. fexofenadine 35-47 solute carrier family 22 member 8 Homo sapiens 184-188 23115085-5 2013 Rifampicin inhibited the uptake of fexofenadine enantiomers by human hepatocytes via organic anion transporter (OAT) OATP1B3 and its basal-to-apical transport in Caco-2 cells, but not OAT3-mediated or multidrug and toxic compound extrusion 1 (MATE1)-mediated transport. fexofenadine 35-47 solute carrier family 47 member 1 Homo sapiens 243-248 23115085-8 2013 S-fexofenadine is a more potent human histamine H1 receptor antagonist than R-fexofenadine. fexofenadine 0-14 histamine receptor H1 Homo sapiens 38-59 23115085-9 2013 In conclusion, rifampicin has multiple interaction sites with fexofenadine, all of which contribute to increasing the area under the curve of fexofenadine when they are given simultaneously, to surpass the effect of the induction of P-glycoprotein elicited by multiple doses. fexofenadine 62-74 ATP binding cassette subfamily B member 1 Homo sapiens 233-247 23215684-7 2013 The difference in transporter-mediated R(+)-fexofenadine and S(-)-fexofenadine uptake was completely diminished under ATP-depleted conditions and in the presence of organic anion transporter peptide (OATP) inhibitors. fexofenadine 61-78 solute carrier organic anion transporter family member 1A2 Homo sapiens 165-198 23215684-7 2013 The difference in transporter-mediated R(+)-fexofenadine and S(-)-fexofenadine uptake was completely diminished under ATP-depleted conditions and in the presence of organic anion transporter peptide (OATP) inhibitors. fexofenadine 61-78 solute carrier organic anion transporter family member 1A2 Homo sapiens 200-204 22740401-7 2012 The binding pockets for two proposed inhibitors of the CD81-HCV interaction, namely, benzyl salicylate and fexofenadine, were shown to overlap the HCV and membrane interaction sites. fexofenadine 107-119 CD81 molecule Homo sapiens 55-59 22830293-0 2012 Enhancement of clara cell 10-kD protein (CC10) production from nasal epithelial cells by fexofenadine hydrochloride. fexofenadine 89-115 secretoglobin family 1A member 1 Homo sapiens 41-45 22830293-3 2012 In the present study, we examined the influence of a histamine H1 receptor antagonist, fexofenadine hydrochloride (FEX) on CC10 production in vitro and in vivo. fexofenadine 87-113 secretoglobin family 1A member 1 Homo sapiens 123-127 22830293-3 2012 In the present study, we examined the influence of a histamine H1 receptor antagonist, fexofenadine hydrochloride (FEX) on CC10 production in vitro and in vivo. fexofenadine 115-118 histamine receptor H1 Homo sapiens 53-74 22830293-3 2012 In the present study, we examined the influence of a histamine H1 receptor antagonist, fexofenadine hydrochloride (FEX) on CC10 production in vitro and in vivo. fexofenadine 115-118 secretoglobin family 1A member 1 Homo sapiens 123-127 21646440-2 2012 The purpose of this study was to determine the influence of Panax ginseng on CYP3A and P-gp function using the probe substrates midazolam and fexofenadine, respectively. fexofenadine 142-154 ATP binding cassette subfamily B member 1 Homo sapiens 87-91 22198458-4 2012 Multiple-dose ketoconazole coadministration reduced the P-gp activity as shown by fexofenadine oral challenge. fexofenadine 82-94 ATP binding cassette subfamily B member 1 Homo sapiens 56-60 21833762-4 2012 Permeability of FEX was determined at different donor concentrations, and the effect of SDS at two concentration levels (10 and 50 muM) on FEX permeability was evaluated. fexofenadine 139-142 latexin Homo sapiens 131-134 21950458-1 2012 AIM: This aim of this study was to characterize the impact of the P-glycoprotein (P-gp) inducer, carbamazepine, on fexofenadine enantiomer pharmacokinetics. fexofenadine 115-127 ATP binding cassette subfamily B member 1 Homo sapiens 66-80 21950458-1 2012 AIM: This aim of this study was to characterize the impact of the P-glycoprotein (P-gp) inducer, carbamazepine, on fexofenadine enantiomer pharmacokinetics. fexofenadine 115-127 ATP binding cassette subfamily B member 1 Homo sapiens 82-86 21950458-5 2012 The P-gp inducer showed a greater effect on the pharmacokinetic parameters of (S)-fexofenadine. fexofenadine 78-94 ATP binding cassette subfamily B member 1 Homo sapiens 4-8 22223343-7 2012 Mice given a histamine H1-receptor antagonist [fexofenadine (peripherally acting) or pyrilamine (peripherally and centrally acting)] or an irreversible HDC inhibitor (alpha-fluoromethylhistidine) displayed less PW endurance than control mice. fexofenadine 47-59 histamine receptor H1 Mus musculus 13-34 21280267-6 2011 OATP2B1-mediated uptake of fexofenadine and midazolam was evaluated with Xenopus laevis oocyte gene-expression system. fexofenadine 27-39 solute carrier organic anion transporter family member 2B1 L homeolog Xenopus laevis 0-7 21933692-5 2011 GRP(18-27)-induced scratching was inhibited by the mu-opioid receptor antagonist naltrexone hydrochloride, the BB(2) bombesin receptor antagonist RC-3095, the H(1) histamine receptor antagonists fexofenadine hydrochloride and chlorpheniramine maleate, and the PAR(2) proteinase-activated receptor antagonist FSLLRY-NH(2). fexofenadine 195-221 gastrin releasing peptide Mus musculus 0-3 21664903-3 2011 JNJ7777120 (10 and 30 mg/kg) reduced this scratching behavior and ameliorated the skin lesions in a dose-dependent manner, whereas the histamine H(1) receptor antagonist fexofenadine had no such effect and did not reduce the inflammation score, even though dexamethasone reduced the scratching bouts. fexofenadine 170-182 histamine receptor H1 Mus musculus 135-158 21780830-1 2011 Fexofenadine is a nonsedative antihistamine that exhibits good oral bioavailability despite its zwitterionic chemical structure and efflux by P-gp. fexofenadine 0-12 phosphoglycolate phosphatase Homo sapiens 142-146 21780830-5 2011 Studies with cellular models expressing single transporters showed that OATP2B1 expression stimulated uptake of fexofenadine at pH 6.0. fexofenadine 112-124 solute carrier organic anion transporter family member 2B1 Homo sapiens 72-79 21780830-6 2011 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 17-29 solute carrier organic anion transporter family member 1A2 Homo sapiens 112-116 21780830-6 2011 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 17-29 solute carrier organic anion transporter family member 2B1 Homo sapiens 173-180 21780830-6 2011 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 207-219 solute carrier organic anion transporter family member 2B1 Homo sapiens 173-180 21780830-11 2011 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 240-252 solute carrier organic anion transporter family member 2B1 Homo sapiens 98-105 21780830-11 2011 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 240-252 ATP binding cassette subfamily C member 3 Homo sapiens 122-126 21280267-13 2011 The uptake of fexofenadine by OATP2B1 cRNA-injected oocytes was significantly higher than that by water-injected oocytes. fexofenadine 14-26 solute carrier organic anion transporter family member 2B1 L homeolog Xenopus laevis 30-37 21280267-14 2011 Apple juice, but not midazolam, significantly decreased the uptake of fexofenadine by OATP2B1 cRNA-injected oocytes. fexofenadine 70-82 solute carrier organic anion transporter family member 2B1 L homeolog Xenopus laevis 86-93 21280267-15 2011 CONCLUSION: The results suggest that fexofenadine is a substrate of OATP2B1, and the transport function of OATP2B1 is subject to the genotype of SLCO2B1 c.1457C> T and apple juice. fexofenadine 37-49 solute carrier organic anion transporter family member 2B1 L homeolog Xenopus laevis 68-75 20869437-10 2010 Inhibition of Pgp by PSC-833 affected fexofenadine absorption only in distal segments resulting in AUC values comparable to the proximal data. fexofenadine 38-50 phosphoglycolate phosphatase Rattus norvegicus 14-17 20869437-12 2010 CONCLUSION: The study demonstrates that Pgp is responsible for a limitation of fexofenadine absorption from distal small intestine. fexofenadine 79-91 phosphoglycolate phosphatase Rattus norvegicus 40-43 20839930-2 2010 The area under the plasma concentration-time curve (AUC(0-24)) of S-fexofenadine, but not R-fexofenadine, was significantly lower in subjects with a SLCO2B1*1/*1 allele as compared to subjects with a *3 allele (p = 0.031). fexofenadine 66-80 solute carrier organic anion transporter family member 2B1 Homo sapiens 149-156 20797388-1 2010 OATP1A2 and OATP2B1 are uptake transporters of the human organic anion transporting polypeptide (OATP) family with a broad substrate spectrum including several endogenous compounds as well as drugs such as the antihistaminic drug fexofenadine and HMG-CoA reductase inhibitors. fexofenadine 230-242 solute carrier organic anion transporter family member 1A2 Homo sapiens 0-7 20797388-1 2010 OATP1A2 and OATP2B1 are uptake transporters of the human organic anion transporting polypeptide (OATP) family with a broad substrate spectrum including several endogenous compounds as well as drugs such as the antihistaminic drug fexofenadine and HMG-CoA reductase inhibitors. fexofenadine 230-242 solute carrier organic anion transporter family member 2B1 Homo sapiens 12-19 20797388-1 2010 OATP1A2 and OATP2B1 are uptake transporters of the human organic anion transporting polypeptide (OATP) family with a broad substrate spectrum including several endogenous compounds as well as drugs such as the antihistaminic drug fexofenadine and HMG-CoA reductase inhibitors. fexofenadine 230-242 solute carrier organic anion transporter family member 1A2 Homo sapiens 57-95 20797388-1 2010 OATP1A2 and OATP2B1 are uptake transporters of the human organic anion transporting polypeptide (OATP) family with a broad substrate spectrum including several endogenous compounds as well as drugs such as the antihistaminic drug fexofenadine and HMG-CoA reductase inhibitors. fexofenadine 230-242 solute carrier organic anion transporter family member 1A2 Homo sapiens 0-4 20797388-7 2010 Apigenin, kaempferol, and quercetin led to a concentration-dependent decrease of the OATP1A2-mediated fexofenadine transport with IC(50) values of 4.3muM, 12.0muM, and 12.6muM, respectively. fexofenadine 102-114 solute carrier organic anion transporter family member 1A2 Homo sapiens 85-92 21039758-2 2010 The discovery was based on an opposite to anticipated finding when assessing the possibility of grapefruit juice increasing oral fexofenadine bioavailability in humans through inhibition of intestinal MDR1-mediated efflux transport. fexofenadine 129-141 ATP binding cassette subfamily B member 1 Homo sapiens 201-205 20839930-4 2010 The pharmacokinetic properties of S-fexofenadine are affected by a single polymorphism of SLCO2B1 in combination with several polymorphisms of ABCB1 C1236T, C3435T, and ABCC2 C-24T. fexofenadine 34-48 solute carrier organic anion transporter family member 2B1 Homo sapiens 90-97 20839930-4 2010 The pharmacokinetic properties of S-fexofenadine are affected by a single polymorphism of SLCO2B1 in combination with several polymorphisms of ABCB1 C1236T, C3435T, and ABCC2 C-24T. fexofenadine 34-48 ATP binding cassette subfamily B member 1 Homo sapiens 143-148 20839930-4 2010 The pharmacokinetic properties of S-fexofenadine are affected by a single polymorphism of SLCO2B1 in combination with several polymorphisms of ABCB1 C1236T, C3435T, and ABCC2 C-24T. fexofenadine 34-48 ATP binding cassette subfamily C member 2 Homo sapiens 169-174 20839930-6 2010 These findings suggest that a combination of multiple transporters, including OATP, P-gp, and MRP2, reacts strongly to fexofenadine exposure in the small intestine and liver, resulting in different dispositions of both enantiomers. fexofenadine 119-131 solute carrier organic anion transporter family member 1A2 Homo sapiens 78-82 20839930-6 2010 These findings suggest that a combination of multiple transporters, including OATP, P-gp, and MRP2, reacts strongly to fexofenadine exposure in the small intestine and liver, resulting in different dispositions of both enantiomers. fexofenadine 119-131 ATP binding cassette subfamily B member 1 Homo sapiens 84-88 20839930-6 2010 These findings suggest that a combination of multiple transporters, including OATP, P-gp, and MRP2, reacts strongly to fexofenadine exposure in the small intestine and liver, resulting in different dispositions of both enantiomers. fexofenadine 119-131 ATP binding cassette subfamily C member 2 Homo sapiens 94-98 20863200-9 2010 This is consistent with a reduction in hepatic Oatp and/or P-gp for a high extraction ratio drug such as fexofenadine. fexofenadine 105-117 ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus 59-63 21188040-1 2010 Fexofenadine is a selective histamine H(1) receptor antagonist, used for relief of the symptoms of allergy. fexofenadine 0-12 histamine receptor H1 Homo sapiens 28-51 20306185-0 2010 Effect of metronidazole on the pharmacokinetics of fexofenadine, a P-glycoprotein substrate, in healthy male volunteers. fexofenadine 51-63 ATP binding cassette subfamily B member 1 Homo sapiens 67-81 20306185-3 2010 We have assessed the possible inhibitory effects of metronidazole on P-gp-mediated drug disposition in healthy subjects using fexofenadine as a P-gp substrate. fexofenadine 126-138 ATP binding cassette subfamily B member 1 Homo sapiens 144-148 20307657-2 2010 Fexofenadine was chosen to represent an unmetabolized transporter substrate (P-gP and OATP). fexofenadine 0-12 phosphoglycolate phosphatase Homo sapiens 77-81 20307657-2 2010 Fexofenadine was chosen to represent an unmetabolized transporter substrate (P-gP and OATP). fexofenadine 0-12 solute carrier organic anion transporter family member 1A2 Homo sapiens 86-90 20214407-4 2010 Digoxin, fexofenadine, talinolol and quinidine are commonly used probe drugs for P-gp phenotyping. fexofenadine 9-21 ATP binding cassette subfamily B member 1 Homo sapiens 81-85 19947891-3 2010 This article reviews the pharmacokinetic differences between fexofenadine enantiomers in humans and summarizes the previous reports that co-administration of P-glycoprotein inhibitors has altered the stereoselective pharmacokinetics of fexofenadine enantiomers. fexofenadine 61-73 ATP binding cassette subfamily B member 1 Homo sapiens 158-172 19947891-3 2010 This article reviews the pharmacokinetic differences between fexofenadine enantiomers in humans and summarizes the previous reports that co-administration of P-glycoprotein inhibitors has altered the stereoselective pharmacokinetics of fexofenadine enantiomers. fexofenadine 236-248 ATP binding cassette subfamily B member 1 Homo sapiens 158-172 19947891-7 2010 Co-administration of itraconazole and/or verapamil significantly increased the AUC(0 - 24) of both enantiomers; their influence on the P-glycoprotein-mediated transport of (S)-fexofenadine was greater than that of the (R)-enantiomer. fexofenadine 172-188 ATP binding cassette subfamily B member 1 Homo sapiens 135-149 19947891-8 2010 However, because t(max) and t(1/2) were constant in both studies, the fexofenadine stereoselective pharmacokinetics appears to be due to P-glycoprotein efflux activity in the small intestine, which suggests that P-glycoprotein probably possesses the chiral discriminatory abilities. fexofenadine 70-82 ATP binding cassette subfamily B member 1 Homo sapiens 137-151 19947891-8 2010 However, because t(max) and t(1/2) were constant in both studies, the fexofenadine stereoselective pharmacokinetics appears to be due to P-glycoprotein efflux activity in the small intestine, which suggests that P-glycoprotein probably possesses the chiral discriminatory abilities. fexofenadine 70-82 ATP binding cassette subfamily B member 1 Homo sapiens 212-226 19204737-8 2009 Coculture with fexofenadine(1 microM), an MDR1 substrate known to rescue misfolding in other membrane proteins, restored cell surface expression of MDR1 G2677T/C3435T and restored resistance to block HERG by ibutilide 200 nM (98.5+/-0.98% vs 42.3+/-2.2%, P<0.001). fexofenadine 15-27 ATP binding cassette subfamily B member 1 Homo sapiens 42-46 19652466-7 2009 Fexofenadine, a histamine H1 receptor antagonist, reduced scratching induced by histamine but not by substance P, whereas JNJ7777120, a histamine H4 receptor antagonist, significantly reduced both histamine- and substance P-induced scratching. fexofenadine 0-12 histamine receptor H1 Homo sapiens 16-37 19703347-1 2009 OBJECTIVES: This study examined the effects of St John"s wort (Hypericum perforatum) on the disposition of fexofenadine, a substrate of P-glycoprotein/organic anion transporting polypeptide, in the isolated perfused rat liver. fexofenadine 107-119 ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus 136-150 19785645-9 2009 SLCO1B1 polymorphism also affects the pharmacokinetics of many other, but not all (fluvastatin), statins and that of the antidiabetic drug repaglinide, the antihistamine fexofenadine and the endothelin A receptor antagonist atrasentan. fexofenadine 170-182 solute carrier organic anion transporter family member 1B1 Homo sapiens 0-7 19221726-0 2009 Short-term effect of quercetin on the pharmacokinetics of fexofenadine, a substrate of P-glycoprotein, in healthy volunteers. fexofenadine 58-70 ATP binding cassette subfamily B member 1 Homo sapiens 87-101 19221726-8 2009 CONCLUSION: The results of the present study showed that short-term use of quercetin elevated the plasma concentrations of fexofenadine, probably by the inhibition of P-gp-mediated efflux in humans. fexofenadine 123-135 ATP binding cassette subfamily B member 1 Homo sapiens 167-171 19204737-8 2009 Coculture with fexofenadine(1 microM), an MDR1 substrate known to rescue misfolding in other membrane proteins, restored cell surface expression of MDR1 G2677T/C3435T and restored resistance to block HERG by ibutilide 200 nM (98.5+/-0.98% vs 42.3+/-2.2%, P<0.001). fexofenadine 15-27 ATP binding cassette subfamily B member 1 Homo sapiens 148-152 19204737-8 2009 Coculture with fexofenadine(1 microM), an MDR1 substrate known to rescue misfolding in other membrane proteins, restored cell surface expression of MDR1 G2677T/C3435T and restored resistance to block HERG by ibutilide 200 nM (98.5+/-0.98% vs 42.3+/-2.2%, P<0.001). fexofenadine 15-27 potassium voltage-gated channel subfamily H member 2 Homo sapiens 200-204 19204737-9 2009 The non-synonymous MDR1 variant G2677 T (A893S) confers resistance to ibutilide block of I(Kr), which is mitigated by the C3435T polymorphism through reduced protein expression, an effect that can be restored by coculture with fexofenadine. fexofenadine 227-239 ATP binding cassette subfamily B member 1 Homo sapiens 19-23 19552748-9 2009 CONCLUSION: This study indicates that P-gp plays a key role in the stereoselectivity of fexofenadine pharmacokinetics, since the pharmacokinetics of fexofenadine enantiomers were altered by the P-gp inhibitor verapamil, and this effect was greater for S-fexofenadine compared with R-fexofenadine. fexofenadine 88-100 ATP binding cassette subfamily B member 1 Homo sapiens 38-42 19552748-9 2009 CONCLUSION: This study indicates that P-gp plays a key role in the stereoselectivity of fexofenadine pharmacokinetics, since the pharmacokinetics of fexofenadine enantiomers were altered by the P-gp inhibitor verapamil, and this effect was greater for S-fexofenadine compared with R-fexofenadine. fexofenadine 88-100 ATP binding cassette subfamily B member 1 Homo sapiens 194-198 19552748-0 2009 Enantioselective disposition of fexofenadine with the P-glycoprotein inhibitor verapamil. fexofenadine 32-44 ATP binding cassette subfamily B member 1 Homo sapiens 54-68 19552748-9 2009 CONCLUSION: This study indicates that P-gp plays a key role in the stereoselectivity of fexofenadine pharmacokinetics, since the pharmacokinetics of fexofenadine enantiomers were altered by the P-gp inhibitor verapamil, and this effect was greater for S-fexofenadine compared with R-fexofenadine. fexofenadine 149-161 ATP binding cassette subfamily B member 1 Homo sapiens 38-42 19552748-1 2009 AIMS: The aim was to compare possible effects of verapamil, as a P-glycoprotein (P-gp) inhibitor, on the pharmacokinetics of each fexofenadine enantiomer, as a P-gp substrate. fexofenadine 130-142 ATP binding cassette subfamily B member 1 Homo sapiens 65-79 19552748-9 2009 CONCLUSION: This study indicates that P-gp plays a key role in the stereoselectivity of fexofenadine pharmacokinetics, since the pharmacokinetics of fexofenadine enantiomers were altered by the P-gp inhibitor verapamil, and this effect was greater for S-fexofenadine compared with R-fexofenadine. fexofenadine 149-161 ATP binding cassette subfamily B member 1 Homo sapiens 194-198 19552748-1 2009 AIMS: The aim was to compare possible effects of verapamil, as a P-glycoprotein (P-gp) inhibitor, on the pharmacokinetics of each fexofenadine enantiomer, as a P-gp substrate. fexofenadine 130-142 ATP binding cassette subfamily B member 1 Homo sapiens 81-85 19552748-1 2009 AIMS: The aim was to compare possible effects of verapamil, as a P-glycoprotein (P-gp) inhibitor, on the pharmacokinetics of each fexofenadine enantiomer, as a P-gp substrate. fexofenadine 130-142 ATP binding cassette subfamily B member 1 Homo sapiens 160-164 19552748-9 2009 CONCLUSION: This study indicates that P-gp plays a key role in the stereoselectivity of fexofenadine pharmacokinetics, since the pharmacokinetics of fexofenadine enantiomers were altered by the P-gp inhibitor verapamil, and this effect was greater for S-fexofenadine compared with R-fexofenadine. fexofenadine 252-266 ATP binding cassette subfamily B member 1 Homo sapiens 38-42 19552748-9 2009 CONCLUSION: This study indicates that P-gp plays a key role in the stereoselectivity of fexofenadine pharmacokinetics, since the pharmacokinetics of fexofenadine enantiomers were altered by the P-gp inhibitor verapamil, and this effect was greater for S-fexofenadine compared with R-fexofenadine. fexofenadine 252-266 ATP binding cassette subfamily B member 1 Homo sapiens 194-198 19232844-4 2009 CYP3A4/5 and transporters were assessed using alfentanil and fexofenadine, respectively. fexofenadine 61-73 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-6 19114463-1 2009 P-glycoprotein (P-gp) plays an important role in determining net brain uptake of fexofenadine. fexofenadine 81-93 phosphoglycolate phosphatase Mus musculus 0-14 19114463-2 2009 Initial in vivo experiments with 24-h subcutaneous osmotic minipump administration demonstrated that fexofenadine brain penetration was 48-fold higher in mdr1a(-/-) mice than in mdr1a(+/+) mice. fexofenadine 101-113 ATP-binding cassette, sub-family B (MDR/TAP), member 1A Mus musculus 154-159 19114463-3 2009 In contrast, the P-gp efflux ratio at the blood-brain barrier (BBB) for fexofenadine was only approximately 4 using an in situ brain perfusion technique. fexofenadine 72-84 phosphoglycolate phosphatase Mus musculus 17-21 19114463-4 2009 Pharmacokinetic modeling based on the experimental results indicated that the apparent fexofenadine P-gp efflux ratio is time-dependent due to low passive permeability at the BBB. fexofenadine 87-99 phosphoglycolate phosphatase Mus musculus 100-104 19114463-9 2009 Taken together, these results indicate that the fexofenadine BBB P-gp efflux ratio has been underestimated previously due to the lack of complete equilibration of fexofenadine across the blood-brain interface under typical experimental paradigms. fexofenadine 48-60 phosphoglycolate phosphatase Mus musculus 65-69 19114463-1 2009 P-glycoprotein (P-gp) plays an important role in determining net brain uptake of fexofenadine. fexofenadine 81-93 phosphoglycolate phosphatase Mus musculus 16-20 19238656-8 2008 Acute and steady-state ritonavir increased the fexofenadine AUC(0-infinity) 2.8- and 1.4-fold, respectively, suggesting P-gp inhibition. fexofenadine 47-59 ATP binding cassette subfamily B member 1 Homo sapiens 120-124 19114463-9 2009 Taken together, these results indicate that the fexofenadine BBB P-gp efflux ratio has been underestimated previously due to the lack of complete equilibration of fexofenadine across the blood-brain interface under typical experimental paradigms. fexofenadine 163-175 phosphoglycolate phosphatase Mus musculus 65-69 19295235-4 2009 OBJECTIVE: We evaluated the variability of IL-16 and the effects of the antiallergic drugs fexofenadine (40 mg/kg/day) and ramatroban (30 mg/kg/day) on IL-16 in an OVA-sensitized BALB/c murine experimental allergic rhinitis model. fexofenadine 91-103 interleukin 16 Mus musculus 152-157 19295235-8 2009 Fexofenadine and ramatroban significantly inhibited the following OVA-induced allergic features when compared to the nontreated sensitized group: sneezing, nasal rubbing, eosinophil infiltration, IL-16 expressions in nasal tissue, and serum IL-16 level. fexofenadine 0-12 interleukin 16 Mus musculus 196-201 19295235-8 2009 Fexofenadine and ramatroban significantly inhibited the following OVA-induced allergic features when compared to the nontreated sensitized group: sneezing, nasal rubbing, eosinophil infiltration, IL-16 expressions in nasal tissue, and serum IL-16 level. fexofenadine 0-12 interleukin 16 Mus musculus 241-246 18572335-1 2008 It has been shown that fexofenadine, a selective non-sedating histamine H(1)-receptor antagonist, is a substrate for P-glycoprotein (P-gp) and an organic anion transporting peptide (OATP). fexofenadine 23-35 histamine receptor H 1 Rattus norvegicus 62-85 18572335-1 2008 It has been shown that fexofenadine, a selective non-sedating histamine H(1)-receptor antagonist, is a substrate for P-glycoprotein (P-gp) and an organic anion transporting peptide (OATP). fexofenadine 23-35 ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus 117-131 18572335-1 2008 It has been shown that fexofenadine, a selective non-sedating histamine H(1)-receptor antagonist, is a substrate for P-glycoprotein (P-gp) and an organic anion transporting peptide (OATP). fexofenadine 23-35 ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus 133-137 18572335-10 2008 Low absorption of fexofenadine in rats is attributed to potent secretory transport mediated by P-gp. fexofenadine 18-30 ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus 95-99 18511651-8 2008 ABCB1 3435 C/T carriers showed increased basal P-gp activity in CD4+ and CD8+ T cells, increased R123-induced efflux activity in CD4+ T cell, and decreased fexofenadine AUC. fexofenadine 156-168 ATP binding cassette subfamily B member 1 Homo sapiens 0-5 18294330-3 2008 WHAT THIS STUDY ADDS: This study indicates that the stereoselective pharmacokinetics of fexofenadine are due to P-gp-mediated transport and its stereoselectivity is altered by itraconazole, a an inhibitor of P-gp. fexofenadine 88-100 ATP binding cassette subfamily B member 1 Homo sapiens 112-116 18570599-2 2008 We evaluated whether a genetic polymorphism of multi-drug resistance 1 gene (MDR1) could produce variations in pharmacokinetic and pharmacodynamic parameters of fexofenadine. fexofenadine 161-173 ATP binding cassette subfamily B member 1 Homo sapiens 47-70 18570599-2 2008 We evaluated whether a genetic polymorphism of multi-drug resistance 1 gene (MDR1) could produce variations in pharmacokinetic and pharmacodynamic parameters of fexofenadine. fexofenadine 161-173 ATP binding cassette subfamily B member 1 Homo sapiens 77-81 18294330-3 2008 WHAT THIS STUDY ADDS: This study indicates that the stereoselective pharmacokinetics of fexofenadine are due to P-gp-mediated transport and its stereoselectivity is altered by itraconazole, a an inhibitor of P-gp. fexofenadine 88-100 ATP binding cassette subfamily B member 1 Homo sapiens 208-212 18294330-4 2008 AIMS: The aim of this study was to determine the inhibitory effect of itraconazole, a P-glycoprotein (P-gp) inhibitor, on the stereoselective pharmacokinetics of fexofenadine. fexofenadine 162-174 ATP binding cassette subfamily B member 1 Homo sapiens 86-100 18294330-4 2008 AIMS: The aim of this study was to determine the inhibitory effect of itraconazole, a P-glycoprotein (P-gp) inhibitor, on the stereoselective pharmacokinetics of fexofenadine. fexofenadine 162-174 ATP binding cassette subfamily B member 1 Homo sapiens 102-106 18294330-11 2008 CONCLUSIONS: This study indicates that the stereoselective pharmacokinetics of fexofenadine are due to P-gp-mediated transport and its stereoselectivity is altered by itraconazole, a P-gp inhibitor. fexofenadine 79-91 ATP binding cassette subfamily B member 1 Homo sapiens 103-107 18294330-11 2008 CONCLUSIONS: This study indicates that the stereoselective pharmacokinetics of fexofenadine are due to P-gp-mediated transport and its stereoselectivity is altered by itraconazole, a P-gp inhibitor. fexofenadine 79-91 ATP binding cassette subfamily B member 1 Homo sapiens 183-187 18276836-0 2008 Impact of basolateral multidrug resistance-associated protein (Mrp) 3 and Mrp4 on the hepatobiliary disposition of fexofenadine in perfused mouse livers. fexofenadine 115-127 ATP-binding cassette, sub-family C (CFTR/MRP), member 3 Mus musculus 22-69 18276836-0 2008 Impact of basolateral multidrug resistance-associated protein (Mrp) 3 and Mrp4 on the hepatobiliary disposition of fexofenadine in perfused mouse livers. fexofenadine 115-127 ATP-binding cassette, sub-family C (CFTR/MRP), member 4 Mus musculus 74-78 18276836-8 2008 In Abcc2(-/-)/Abcc3(-/-) double-knockout mice, fexofenadine biliary excretion was impaired, but perfusate recovery was similar to that in wild-type mice and more than 2-fold higher than that in Abcc3(-/-) mice, presumably due to compensatory basolateral transport mechanism(s). fexofenadine 47-59 ATP-binding cassette, sub-family C (CFTR/MRP), member 2 Mus musculus 3-8 18276836-4 2008 Recently, we showed that in mice fexofenadine is excreted into bile primarily by multidrug resistance-associated protein (Mrp) 2 (Abcc2). fexofenadine 33-45 ATP-binding cassette, sub-family C (CFTR/MRP), member 2 Mus musculus 81-128 18299336-7 2008 This result suggests that P-gp limits the intestinal absorption of fexofenadine in dogs. fexofenadine 67-79 PGP Canis lupus familiaris 26-30 18276836-4 2008 Recently, we showed that in mice fexofenadine is excreted into bile primarily by multidrug resistance-associated protein (Mrp) 2 (Abcc2). fexofenadine 33-45 ATP-binding cassette, sub-family C (CFTR/MRP), member 2 Mus musculus 130-135 18276836-5 2008 In the present study, the roles of Mrp3 (Abcc3) and Mrp4 (Abcc4) in the hepatobiliary disposition of fexofenadine were examined in knockout mice using in situ liver perfusion. fexofenadine 101-113 ATP-binding cassette, sub-family C (CFTR/MRP), member 3 Mus musculus 35-39 18276836-5 2008 In the present study, the roles of Mrp3 (Abcc3) and Mrp4 (Abcc4) in the hepatobiliary disposition of fexofenadine were examined in knockout mice using in situ liver perfusion. fexofenadine 101-113 ATP-binding cassette, sub-family C (CFTR/MRP), member 4 Mus musculus 52-56 18276836-5 2008 In the present study, the roles of Mrp3 (Abcc3) and Mrp4 (Abcc4) in the hepatobiliary disposition of fexofenadine were examined in knockout mice using in situ liver perfusion. fexofenadine 101-113 ATP-binding cassette, sub-family C (CFTR/MRP), member 4 Mus musculus 58-63 18276836-6 2008 Compared with that in wild-type mice, basolateral excretion of fexofenadine was impaired, resulting in a approximately 50% decrease in perfusate recovery in Abcc3(-/-) mice; in contrast, fexofenadine hepatobiliary disposition was unaltered in Abcc4(-/-) mice. fexofenadine 63-75 ATP-binding cassette, sub-family C (CFTR/MRP), member 3 Mus musculus 157-162 18276836-6 2008 Compared with that in wild-type mice, basolateral excretion of fexofenadine was impaired, resulting in a approximately 50% decrease in perfusate recovery in Abcc3(-/-) mice; in contrast, fexofenadine hepatobiliary disposition was unaltered in Abcc4(-/-) mice. fexofenadine 63-75 ATP-binding cassette, sub-family C (CFTR/MRP), member 4 Mus musculus 243-248 18276836-7 2008 As expected, in Abcc2(-/-) mice, fexofenadine was redirected from the canalicular to the basolateral membrane for excretion. fexofenadine 33-45 ATP-binding cassette, sub-family C (CFTR/MRP), member 2 Mus musculus 16-21 17910814-1 2007 The aim of this study was to examine the effect of fexofenadine hydrochloride (FEX), a histamine H1-receptor antagonist, on nitric oxide (NO) production in-vitro and in-vivo. fexofenadine 51-77 histamine receptor H1 Mus musculus 87-108 18180276-6 2008 Vectorial basal-to-apical transport of FEX was observed in double transfectants expressing OATP1B1/multidrug resistance-associated protein 2 (MRP2) and OATP1B3/MRP2, suggesting that OATP1B1 as well as OATP1B3 is involved in the hepatic uptake of FEX and that MRP2 can recognize FEX as a substrate. fexofenadine 39-42 ATP binding cassette subfamily C member 2 Homo sapiens 91-140 18180276-6 2008 Vectorial basal-to-apical transport of FEX was observed in double transfectants expressing OATP1B1/multidrug resistance-associated protein 2 (MRP2) and OATP1B3/MRP2, suggesting that OATP1B1 as well as OATP1B3 is involved in the hepatic uptake of FEX and that MRP2 can recognize FEX as a substrate. fexofenadine 39-42 ATP binding cassette subfamily C member 2 Homo sapiens 142-146 18180276-6 2008 Vectorial basal-to-apical transport of FEX was observed in double transfectants expressing OATP1B1/multidrug resistance-associated protein 2 (MRP2) and OATP1B3/MRP2, suggesting that OATP1B1 as well as OATP1B3 is involved in the hepatic uptake of FEX and that MRP2 can recognize FEX as a substrate. fexofenadine 39-42 solute carrier organic anion transporter family member 1B3 Homo sapiens 152-159 18180276-6 2008 Vectorial basal-to-apical transport of FEX was observed in double transfectants expressing OATP1B1/multidrug resistance-associated protein 2 (MRP2) and OATP1B3/MRP2, suggesting that OATP1B1 as well as OATP1B3 is involved in the hepatic uptake of FEX and that MRP2 can recognize FEX as a substrate. fexofenadine 39-42 ATP binding cassette subfamily C member 2 Homo sapiens 160-164 18180276-6 2008 Vectorial basal-to-apical transport of FEX was observed in double transfectants expressing OATP1B1/multidrug resistance-associated protein 2 (MRP2) and OATP1B3/MRP2, suggesting that OATP1B1 as well as OATP1B3 is involved in the hepatic uptake of FEX and that MRP2 can recognize FEX as a substrate. fexofenadine 39-42 solute carrier organic anion transporter family member 1B1 Homo sapiens 91-98 18180276-6 2008 Vectorial basal-to-apical transport of FEX was observed in double transfectants expressing OATP1B1/multidrug resistance-associated protein 2 (MRP2) and OATP1B3/MRP2, suggesting that OATP1B1 as well as OATP1B3 is involved in the hepatic uptake of FEX and that MRP2 can recognize FEX as a substrate. fexofenadine 39-42 solute carrier organic anion transporter family member 1B3 Homo sapiens 201-208 18180276-6 2008 Vectorial basal-to-apical transport of FEX was observed in double transfectants expressing OATP1B1/multidrug resistance-associated protein 2 (MRP2) and OATP1B3/MRP2, suggesting that OATP1B1 as well as OATP1B3 is involved in the hepatic uptake of FEX and that MRP2 can recognize FEX as a substrate. fexofenadine 39-42 ATP binding cassette subfamily C member 2 Homo sapiens 160-164 18180276-7 2008 The inhibitory effects of compounds on FEX uptake in OATP1B3-expressing HEK293 cells were investigated, and the maximal degree of increase in plasma AUC of FEX by drug interaction in clinical situations was estimated. fexofenadine 39-42 solute carrier organic anion transporter family member 1B3 Homo sapiens 53-60 17951087-3 2008 The number of citric-acid-induced coughs in sensitized guinea pigs was dose-dependently and significantly reduced to the level in non-sensitized guinea pigs when animals were pretreated with fexofenadine, a selective histamine H1 receptor antagonist, 60min before citric acid inhalation. fexofenadine 191-203 histamine H1 receptor Cavia porcellus 217-238 17913796-0 2008 Multidrug resistance-associated protein 2 is primarily responsible for the biliary excretion of fexofenadine in mice. fexofenadine 96-108 ATP-binding cassette, sub-family C (CFTR/MRP), member 2 Mus musculus 0-41 17913796-1 2008 Previous studies implicated P-glycoprotein (P-gp) as the major transport protein responsible for the biliary excretion of fexofenadine (FEX). fexofenadine 122-134 phosphoglycolate phosphatase Mus musculus 28-42 17913796-1 2008 Previous studies implicated P-glycoprotein (P-gp) as the major transport protein responsible for the biliary excretion of fexofenadine (FEX). fexofenadine 122-134 phosphoglycolate phosphatase Mus musculus 44-48 17913796-1 2008 Previous studies implicated P-glycoprotein (P-gp) as the major transport protein responsible for the biliary excretion of fexofenadine (FEX). fexofenadine 136-139 phosphoglycolate phosphatase Mus musculus 28-42 17913796-1 2008 Previous studies implicated P-glycoprotein (P-gp) as the major transport protein responsible for the biliary excretion of fexofenadine (FEX). fexofenadine 136-139 phosphoglycolate phosphatase Mus musculus 44-48 17910814-1 2007 The aim of this study was to examine the effect of fexofenadine hydrochloride (FEX), a histamine H1-receptor antagonist, on nitric oxide (NO) production in-vitro and in-vivo. fexofenadine 79-82 histamine receptor H1 Mus musculus 87-108 17215845-8 2007 However, among OATP transporters, only OATP1A2 was capable of fexofenadine uptake when assessed in vitro. fexofenadine 62-74 solute carrier organic anion transporter family member 1A2 Homo sapiens 39-46 17230498-1 2007 Fexofenadine, a substrate of P-glycoprotein and an organic anion transporter polypeptide, is commonly used to assess P-glycoprotein activity in vivo. fexofenadine 0-12 ATP binding cassette subfamily B member 1 Homo sapiens 29-43 17230498-1 2007 Fexofenadine, a substrate of P-glycoprotein and an organic anion transporter polypeptide, is commonly used to assess P-glycoprotein activity in vivo. fexofenadine 0-12 ATP binding cassette subfamily B member 1 Homo sapiens 117-131 17230498-8 2007 On the other hand, the stereoselective metabolism of fexofenadine using recombinant CYP3A4 was investigated; however, fexofenadine enantiomers were not metabolized by CYP3A4. fexofenadine 53-65 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 84-90 17230498-8 2007 On the other hand, the stereoselective metabolism of fexofenadine using recombinant CYP3A4 was investigated; however, fexofenadine enantiomers were not metabolized by CYP3A4. fexofenadine 118-130 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 84-90 17230498-9 2007 Fexofenadine is transported by both P-glycoprotein and OATP and is not metabolized by intestinal CYP3A. fexofenadine 0-12 ATP binding cassette subfamily B member 1 Homo sapiens 36-50 17230498-9 2007 Fexofenadine is transported by both P-glycoprotein and OATP and is not metabolized by intestinal CYP3A. fexofenadine 0-12 solute carrier organic anion transporter family member 1A2 Homo sapiens 55-59 17230498-10 2007 Our findings suggest that the affinity of P-glycoprotein for S(-)-fexofenadine is greater than its affinity for the R(+)-enantiomer. fexofenadine 62-78 ATP binding cassette subfamily B member 1 Homo sapiens 42-56 17215845-12 2007 OATP1A2 is likely the key intestinal uptake transporter for fexofenadine absorption whose inhibition results in the grapefruit juice effect. fexofenadine 60-72 solute carrier organic anion transporter family member 1A2 Homo sapiens 0-7 17133778-1 2006 Fexofenadine, a histamine H1-receptor antagonist, is approved for the treatment of pruritus associated with atopic dermatitis. fexofenadine 0-12 histamine receptor H1 Mus musculus 16-37 17767395-1 2007 Fexofenadine, an active metabolite of the second-generation histamine H1 receptor antagonist (antihistamine) terfenadine, does not have the disadvantage of QT prolongation. fexofenadine 0-12 histamine receptor H1 Homo sapiens 60-81 17080426-6 2007 However, the symmetric transport of fexofenadine.HCl in this NHBE cell monolayers study seems to be due to the low expression of P-gp transporter and/or to its saturation with high concentration of fexofenadine.HCl. fexofenadine 36-48 phosphoglycolate phosphatase Homo sapiens 129-133 17323859-5 2007 RESULTS: RT-PCR revealed that IL-12-induced expression of IFN-gamma was partially suppressed by loratadine and fexofenadine and that all 4 agents tested inhibited IL-4-induced expression of IL-5. fexofenadine 111-123 interferon gamma Homo sapiens 58-67 17323859-6 2007 ELISA demonstrated that IL-12-induced IFN-gamma production was significantly suppressed by cetirizine and fexofenadine and IL-4-induced IL-5 production was downregulated by three agents with the exception of cetirizine. fexofenadine 106-118 interferon gamma Homo sapiens 38-47 16935279-3 2006 This histamine-induced increase in the number of citric acid-induced coughs was dose dependently and significantly reduced when animals were pretreated with fexofenadine, a histamine H1 receptor antagonist. fexofenadine 157-169 histamine H1 receptor Cavia porcellus 173-194 17133778-4 2006 Compared with group N, group S mice showed significantly greater scratching frequency, and plasma histamine and eotaxin concentrations; these three variables were significantly lower in group S + F(0-10) than in group S. Scratching frequency increased when fexofenadine was discontinued. fexofenadine 257-269 chemokine (C-C motif) ligand 11 Mus musculus 112-119 16964701-3 2006 Between them, polymorphisms of MDR1 gene coding trans-membrane transport glicoprotein P-gp have been reported to affect the outcome of therapy, and was studied for different drugs-digoxin, fexofenadine, etoposid, vincristine, vinblastine, athracyclines and taxans. fexofenadine 189-201 ATP binding cassette subfamily B member 1 Homo sapiens 31-35 16767419-3 2006 One hypothesis suggests that this is due to fexofenadine producing an increase in dopamine levels by blocking the dopamine transporter. fexofenadine 44-56 solute carrier family 6 member 3 Homo sapiens 114-134 16767419-4 2006 OBJECTIVE: In this study, it was investigated whether a high dose of fexofenadine blocks the dopamine transporter in the striatum. fexofenadine 69-81 solute carrier family 6 member 3 Homo sapiens 93-113 16850393-6 2006 Fexofenadine is a substrate for Pgp, Oatp1, Oatp2, and Oatp3. fexofenadine 0-12 phosphoglycolate phosphatase Rattus norvegicus 32-35 16850393-6 2006 Fexofenadine is a substrate for Pgp, Oatp1, Oatp2, and Oatp3. fexofenadine 0-12 solute carrier organic anion transporter family, member 1a1 Rattus norvegicus 37-42 16850393-6 2006 Fexofenadine is a substrate for Pgp, Oatp1, Oatp2, and Oatp3. fexofenadine 0-12 solute carrier organic anion transporter family, member 1a4 Rattus norvegicus 44-49 16850393-6 2006 Fexofenadine is a substrate for Pgp, Oatp1, Oatp2, and Oatp3. fexofenadine 0-12 solute carrier organic anion transporter family, member 1A5 Rattus norvegicus 55-60 16850393-7 2006 BA appears to preferentially inhibit Oatp3 over Pgp in the intestine, leading to the decreased oral absorption of fexofenadine. fexofenadine 114-126 solute carrier organic anion transporter family, member 1A5 Rattus norvegicus 37-42 16850393-7 2006 BA appears to preferentially inhibit Oatp3 over Pgp in the intestine, leading to the decreased oral absorption of fexofenadine. fexofenadine 114-126 phosphoglycolate phosphatase Rattus norvegicus 48-51 16946558-6 2006 Furthermore, uptake of fexofenadine by Xenopus oocytes expressing rat oatp3 was significantly greater than that by water-injected oocytes, and the affinity of oatp3 for fexofenadine (Km) was about 60 microM, which is comparable with the value obtained by the Ussing chamber method using rat intestinal tissues. fexofenadine 23-35 solute carrier organic anion transporter family, member 1A5 Rattus norvegicus 70-75 16946558-6 2006 Furthermore, uptake of fexofenadine by Xenopus oocytes expressing rat oatp3 was significantly greater than that by water-injected oocytes, and the affinity of oatp3 for fexofenadine (Km) was about 60 microM, which is comparable with the value obtained by the Ussing chamber method using rat intestinal tissues. fexofenadine 23-35 solute carrier organic anion transporter family, member 1A5 Rattus norvegicus 159-164 16946558-6 2006 Furthermore, uptake of fexofenadine by Xenopus oocytes expressing rat oatp3 was significantly greater than that by water-injected oocytes, and the affinity of oatp3 for fexofenadine (Km) was about 60 microM, which is comparable with the value obtained by the Ussing chamber method using rat intestinal tissues. fexofenadine 169-181 solute carrier organic anion transporter family, member 1A5 Rattus norvegicus 159-164 16946558-7 2006 These results indicate that oatp3 plays a role as an influx transporter in the intestinal absorption of fexofenadine in rats. fexofenadine 104-116 solute carrier organic anion transporter family, member 1A5 Rattus norvegicus 28-33 16174671-10 2006 P1 and P3 latency were affected by Treatment x Workload and Treatment respectively and indicated faster attentional and information processing latencies following fexofenadine treatment. fexofenadine 163-175 crystallin gamma F, pseudogene Homo sapiens 0-9 16964701-3 2006 Between them, polymorphisms of MDR1 gene coding trans-membrane transport glicoprotein P-gp have been reported to affect the outcome of therapy, and was studied for different drugs-digoxin, fexofenadine, etoposid, vincristine, vinblastine, athracyclines and taxans. fexofenadine 189-201 phosphoglycolate phosphatase Homo sapiens 86-90 16455804-0 2006 Inhibition of oat3-mediated renal uptake as a mechanism for drug-drug interaction between fexofenadine and probenecid. fexofenadine 90-102 solute carrier family 22 member 8 Homo sapiens 14-18 16625658-10 2006 To further study the utility of ABT, the antihistamine fexofenadine (Fex), which is not significantly metabolized and is a substrate for the uptake and efflux transporters, OATP and P-gp, was tested in rat. fexofenadine 55-67 phosphoglycolate phosphatase Rattus norvegicus 182-186 16625658-10 2006 To further study the utility of ABT, the antihistamine fexofenadine (Fex), which is not significantly metabolized and is a substrate for the uptake and efflux transporters, OATP and P-gp, was tested in rat. fexofenadine 69-72 phosphoglycolate phosphatase Rattus norvegicus 182-186 16455807-11 2006 Such intestinal absorption property of bepotastine is distinctly different from the low membrane-permeable P-gp substrate fexofenadine. fexofenadine 122-134 phosphoglycolate phosphatase Mus musculus 107-111 16455804-4 2006 The uptake of fexofenadine was determined in HEK293 cells expressing human organic anion transporter 1 (OAT1/SLC22A6), OAT2 (SLC22A7), OAT3 (SLC22A8), and organic cation transporter 2 (OCT2/SLC22A2). fexofenadine 14-26 solute carrier family 22 member 6 Homo sapiens 75-102 16455804-4 2006 The uptake of fexofenadine was determined in HEK293 cells expressing human organic anion transporter 1 (OAT1/SLC22A6), OAT2 (SLC22A7), OAT3 (SLC22A8), and organic cation transporter 2 (OCT2/SLC22A2). fexofenadine 14-26 solute carrier family 22 member 2 Homo sapiens 185-189 16455804-4 2006 The uptake of fexofenadine was determined in HEK293 cells expressing human organic anion transporter 1 (OAT1/SLC22A6), OAT2 (SLC22A7), OAT3 (SLC22A8), and organic cation transporter 2 (OCT2/SLC22A2). fexofenadine 14-26 solute carrier family 22 member 2 Homo sapiens 190-197 16455804-5 2006 Only hOAT3-HEK showed a significantly greater accumulation of fexofenadine than that in vector-HEK, which was saturable with K(m) and V(max) values of 70.2 microM and 120 pmol/min/mg protein, respectively. fexofenadine 62-74 solute carrier family 22 member 8 Homo sapiens 5-10 16455804-4 2006 The uptake of fexofenadine was determined in HEK293 cells expressing human organic anion transporter 1 (OAT1/SLC22A6), OAT2 (SLC22A7), OAT3 (SLC22A8), and organic cation transporter 2 (OCT2/SLC22A2). fexofenadine 14-26 solute carrier family 22 member 6 Homo sapiens 104-108 16455804-6 2006 Inhibition potency of probenecid for the uptake of fexofenadine was compared between hOAT3 and organic anion-transporting peptide 1B3 (hOATP1B3), a transporter responsible for the hepatic uptake of fexofenadine (Drug Metab Dispos 33:1477-1481, 2005). fexofenadine 198-210 solute carrier family 22 member 8 Homo sapiens 85-133 16455804-6 2006 Inhibition potency of probenecid for the uptake of fexofenadine was compared between hOAT3 and organic anion-transporting peptide 1B3 (hOATP1B3), a transporter responsible for the hepatic uptake of fexofenadine (Drug Metab Dispos 33:1477-1481, 2005). fexofenadine 198-210 solute carrier organic anion transporter family member 1B3 Homo sapiens 135-143 16455804-4 2006 The uptake of fexofenadine was determined in HEK293 cells expressing human organic anion transporter 1 (OAT1/SLC22A6), OAT2 (SLC22A7), OAT3 (SLC22A8), and organic cation transporter 2 (OCT2/SLC22A2). fexofenadine 14-26 solute carrier family 22 member 6 Homo sapiens 109-116 16455804-9 2006 These results suggest that the renal drug-drug interaction between fexofenadine and probenecid is probably explained by an inhibition of the renal uptake of fexofenadine via hOAT3, at least in part. fexofenadine 67-79 solute carrier family 22 member 8 Homo sapiens 174-179 16455804-4 2006 The uptake of fexofenadine was determined in HEK293 cells expressing human organic anion transporter 1 (OAT1/SLC22A6), OAT2 (SLC22A7), OAT3 (SLC22A8), and organic cation transporter 2 (OCT2/SLC22A2). fexofenadine 14-26 solute carrier family 22 member 7 Homo sapiens 119-123 16455804-9 2006 These results suggest that the renal drug-drug interaction between fexofenadine and probenecid is probably explained by an inhibition of the renal uptake of fexofenadine via hOAT3, at least in part. fexofenadine 157-169 solute carrier family 22 member 8 Homo sapiens 174-179 16455804-4 2006 The uptake of fexofenadine was determined in HEK293 cells expressing human organic anion transporter 1 (OAT1/SLC22A6), OAT2 (SLC22A7), OAT3 (SLC22A8), and organic cation transporter 2 (OCT2/SLC22A2). fexofenadine 14-26 solute carrier family 22 member 7 Homo sapiens 125-132 16455804-4 2006 The uptake of fexofenadine was determined in HEK293 cells expressing human organic anion transporter 1 (OAT1/SLC22A6), OAT2 (SLC22A7), OAT3 (SLC22A8), and organic cation transporter 2 (OCT2/SLC22A2). fexofenadine 14-26 solute carrier family 22 member 8 Homo sapiens 135-139 16455804-4 2006 The uptake of fexofenadine was determined in HEK293 cells expressing human organic anion transporter 1 (OAT1/SLC22A6), OAT2 (SLC22A7), OAT3 (SLC22A8), and organic cation transporter 2 (OCT2/SLC22A2). fexofenadine 14-26 solute carrier family 22 member 8 Homo sapiens 141-148 16455804-4 2006 The uptake of fexofenadine was determined in HEK293 cells expressing human organic anion transporter 1 (OAT1/SLC22A6), OAT2 (SLC22A7), OAT3 (SLC22A8), and organic cation transporter 2 (OCT2/SLC22A2). fexofenadine 14-26 solute carrier family 22 member 2 Homo sapiens 155-183 16270723-0 2005 The effect of fexofenadine on expression of intercellular adhesion molecule 1 and induction of apoptosis on peripheral eosinophils. fexofenadine 14-26 intercellular adhesion molecule 1 Homo sapiens 44-77 17016062-6 2006 RESULTS: High concentrations of FEX (10(-3) mol/l) significantly inhibited arachidonic acid-mediated ovine COX-1 activity, but low concentrations had no effect. fexofenadine 32-35 mitochondrially encoded cytochrome c oxidase I Homo sapiens 107-112 17016062-8 2006 The inhibition of COX-2 activity by FEX was similar to that seen with the selective COX-2 inhibitor, DuP-679. fexofenadine 36-39 mitochondrially encoded cytochrome c oxidase II Homo sapiens 18-23 17016062-11 2006 CONCLUSION: FEX showed selective arachidonic acid-mediated COX-2 inhibitory enzyme activity, which differed markedly from the COX inhibitory enzyme activity of LOR. fexofenadine 12-15 mitochondrially encoded cytochrome c oxidase II Homo sapiens 59-64 17016062-12 2006 This selective COX-2 inhibitor activity by FEX may contribute to its anti-inflammatory properties in relieving nasal congestion in allergic rhinitis. fexofenadine 43-46 mitochondrially encoded cytochrome c oxidase II Homo sapiens 15-20 16014768-0 2005 Contribution of OATP (organic anion-transporting polypeptide) family transporters to the hepatic uptake of fexofenadine in humans. fexofenadine 107-119 solute carrier organic anion transporter family member 1A2 Homo sapiens 16-20 16014768-0 2005 Contribution of OATP (organic anion-transporting polypeptide) family transporters to the hepatic uptake of fexofenadine in humans. fexofenadine 107-119 solute carrier organic anion transporter family member 1A2 Homo sapiens 22-60 16014768-12 2005 In conclusion, this is, to our knowledge, the first demonstration that OATP1B3 is thought to be a major transporter involved in hepatic uptake of FEX in humans. fexofenadine 146-149 solute carrier organic anion transporter family member 1B3 Homo sapiens 71-78 17016062-0 2006 New evidence of H1-receptor independent COX-2 inhibition by fexofenadine HCl in vitro. fexofenadine 60-76 mitochondrially encoded cytochrome c oxidase II Homo sapiens 40-45 17016062-3 2006 METHODS: The effects of two antihistamines, FEX and loratadine (LOR), were investigated on cyclooxygenase (COX)-1 and -2 enzymes in vitro. fexofenadine 44-47 prostaglandin-endoperoxide synthase 1 Homo sapiens 91-120 16572735-0 2005 The efficacy and safety of 30 mg fexofenadine HCl bid in pediatric patients with allergic rhinitis. fexofenadine 33-49 BH3 interacting domain death agonist Homo sapiens 50-53 16572735-13 2005 Fexofenadine 30 mg bid is effective in reducing the total symptom score of allergic rhinitis including blocked nose and is generally well tolerated. fexofenadine 0-12 BH3 interacting domain death agonist Homo sapiens 19-22 16361727-6 2005 In contrast, cetiridine and fexofenadine unexpectedly increased the substance P level. fexofenadine 28-40 tachykinin precursor 1 Homo sapiens 68-79 16270723-3 2005 To assess the possible anti-inflammatory activity of fexofenadine, a selective H1-receptor antagonist, we evaluated its capacity to modulate the expression of adhesion molecules leukocyte function-associated antigen (LFA) 1 and intracellular adhesion molecule (ICAM) 1 on eosinophil surface and to induce apoptosis of eosinophils. fexofenadine 53-65 integrin subunit alpha L Homo sapiens 178-223 16270723-3 2005 To assess the possible anti-inflammatory activity of fexofenadine, a selective H1-receptor antagonist, we evaluated its capacity to modulate the expression of adhesion molecules leukocyte function-associated antigen (LFA) 1 and intracellular adhesion molecule (ICAM) 1 on eosinophil surface and to induce apoptosis of eosinophils. fexofenadine 53-65 intercellular adhesion molecule 1 Homo sapiens 228-268 16270723-5 2005 To evaluate apoptosis of eosinophils, cells stimulated with interleukin-5, in the presence of different concentrations of fexofenadine, have been incubated with a phosphatidylserine-binding protein (annexin V) fluorescein isothiocyanate conjugated and then analyzed by flow cytometry. fexofenadine 122-134 interleukin 5 Homo sapiens 60-73 16270723-7 2005 In this study, fexofenadine did not cause any significant changes in the expression of LFA-1 but was shown to be able to inhibit the expression of ICAM-1 at concentrations between 10(-3) and 10(-4) M. Moreover, concentrations of fexofenadine from 10(-3) to 6 x 10(-4) M induced a significant increment in the percentage of apoptotic cells. fexofenadine 15-27 intercellular adhesion molecule 1 Homo sapiens 147-153 16270723-7 2005 In this study, fexofenadine did not cause any significant changes in the expression of LFA-1 but was shown to be able to inhibit the expression of ICAM-1 at concentrations between 10(-3) and 10(-4) M. Moreover, concentrations of fexofenadine from 10(-3) to 6 x 10(-4) M induced a significant increment in the percentage of apoptotic cells. fexofenadine 229-241 intercellular adhesion molecule 1 Homo sapiens 147-153 16270723-8 2005 Our findings indicate the possibility of obtaining relevant anti-inflammatory pharmacologic effects, other than antihistamine activity, by fexofenadine, such as inhibition of ICAM-1 expression and induction of eosinophil apoptosis. fexofenadine 139-151 intercellular adhesion molecule 1 Homo sapiens 175-181 15842561-0 2005 Fexofenadine pharmacokinetics are associated with a polymorphism of the SLCO1B1 gene (encoding OATP1B1). fexofenadine 0-12 solute carrier organic anion transporter family member 1B1 Homo sapiens 72-79 15821041-0 2005 P-glycoprotein plays a major role in the efflux of fexofenadine in the small intestine and blood-brain barrier, but only a limited role in its biliary excretion. fexofenadine 51-63 phosphoglycolate phosphatase Mus musculus 0-14 15821041-6 2005 In addition, the steady-state brain-to-plasma concentration ratio of fexofenadine was approximately 3-fold higher in Mdr1a/1b P-gp knockout mice than in wild-type mice. fexofenadine 69-81 ATP-binding cassette, sub-family B (MDR/TAP), member 1A Mus musculus 117-122 15821041-6 2005 In addition, the steady-state brain-to-plasma concentration ratio of fexofenadine was approximately 3-fold higher in Mdr1a/1b P-gp knockout mice than in wild-type mice. fexofenadine 69-81 phosphoglycolate phosphatase Mus musculus 126-130 15821041-9 2005 These results suggest that the biliary excretion of fexofenadine is mediated by unknown transporters distinct from P-gp, Mrp2, and Bcrp. fexofenadine 52-64 ATP-binding cassette, sub-family C (CFTR/MRP), member 2 Mus musculus 121-125 15842561-0 2005 Fexofenadine pharmacokinetics are associated with a polymorphism of the SLCO1B1 gene (encoding OATP1B1). fexofenadine 0-12 solute carrier organic anion transporter family member 1B1 Homo sapiens 95-102 15601808-5 2005 Fexofenadine is a P-gp probe but not a CYP3A substrate. fexofenadine 0-12 phosphoglycolate phosphatase Homo sapiens 18-22 15570603-1 2005 Fexofenadine has been identified as a substrate for both the efflux transporter, P-glycoprotein (P-gp), as well as the influx transporter, organic anion transporting polypeptide (OATP). fexofenadine 0-12 ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus 81-95 15570603-1 2005 Fexofenadine has been identified as a substrate for both the efflux transporter, P-glycoprotein (P-gp), as well as the influx transporter, organic anion transporting polypeptide (OATP). fexofenadine 0-12 ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus 97-101 15570603-1 2005 Fexofenadine has been identified as a substrate for both the efflux transporter, P-glycoprotein (P-gp), as well as the influx transporter, organic anion transporting polypeptide (OATP). fexofenadine 0-12 solute carrier organic anion transporter family member 1A2 Homo sapiens 179-183 15570603-2 2005 Clinical studies in humans showed that fruit juices reduced the oral bioavailability of fexofenadine by preferentially inhibiting OATP over P-gp. fexofenadine 88-100 solute carrier organic anion transporter family member 1A2 Homo sapiens 130-134 15570603-2 2005 Clinical studies in humans showed that fruit juices reduced the oral bioavailability of fexofenadine by preferentially inhibiting OATP over P-gp. fexofenadine 88-100 phosphoglycolate phosphatase Homo sapiens 140-144 15570603-5 2005 Coadministration of fexofenadine with ketoconazole, a P-gp inhibitor, increased the oral exposure of fexofenadine by 187%. fexofenadine 20-32 ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus 54-58 15570603-5 2005 Coadministration of fexofenadine with ketoconazole, a P-gp inhibitor, increased the oral exposure of fexofenadine by 187%. fexofenadine 101-113 ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus 54-58 15601808-6 2005 This investigation tested the hypothesis that alfentanil and fexofenadine could be administered in combination to probe first-pass CYP3A and P-gp activities in humans. fexofenadine 61-73 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 131-136 15601808-6 2005 This investigation tested the hypothesis that alfentanil and fexofenadine could be administered in combination to probe first-pass CYP3A and P-gp activities in humans. fexofenadine 61-73 phosphoglycolate phosphatase Homo sapiens 141-145 15601808-17 2005 Alfentanil and fexofenadine in combination appear to be a useful probe for evaluating both first-pass CYP3A and P-gp activities in humans. fexofenadine 15-27 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 102-107 15601808-17 2005 Alfentanil and fexofenadine in combination appear to be a useful probe for evaluating both first-pass CYP3A and P-gp activities in humans. fexofenadine 15-27 phosphoglycolate phosphatase Homo sapiens 112-116 15663564-4 2004 OBJECTIVE: We evaluated whether fexofenadine hydrochloride (FEX), the carboxylic acid metabolite of terfenadine with selective H(1)-receptor antagonist activity, could inhibit MMP production from nasal fibroblasts (NFs) in response to TNF-alpha stimulation in vitro. fexofenadine 32-58 tumor necrosis factor Homo sapiens 235-244 15663564-4 2004 OBJECTIVE: We evaluated whether fexofenadine hydrochloride (FEX), the carboxylic acid metabolite of terfenadine with selective H(1)-receptor antagonist activity, could inhibit MMP production from nasal fibroblasts (NFs) in response to TNF-alpha stimulation in vitro. fexofenadine 60-63 tumor necrosis factor Homo sapiens 235-244 15663564-12 2004 FEX also inhibited MMP mRNA expression and NF-kappa B activation in PF and MF after TNF-alpha stimulation. fexofenadine 0-3 nuclear factor kappa B subunit 1 Homo sapiens 43-53 15663564-12 2004 FEX also inhibited MMP mRNA expression and NF-kappa B activation in PF and MF after TNF-alpha stimulation. fexofenadine 0-3 tumor necrosis factor Homo sapiens 84-93 15037214-12 2004 In CBF1 mice injected with serum from NC/Nga mice with high IgE levels, the decrease in rectal temperature was suppressed by single administration of fexofenadine HCl (10 and 20 mg/kg; p<0.01 and p<0.001, respectively). fexofenadine 150-166 recombination signal binding protein for immunoglobulin kappa J region Mus musculus 3-7 15331914-6 2004 In contrast, acrivastine and fexofenadine had low brain-to-plasma ratios of 0.072 +/- 0.014 and 0.018 + 0.002, consistent with low passive membrane permeability for both compounds (16.2 and 66 nm/s, respectively) and Pgp efflux. fexofenadine 29-41 ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus 217-220 15359574-7 2004 All four P-gp inhibitors had a strong, concentration-dependent effect on the Papp of fexofenadine in both directions, with GF 120918 being the most specific among them. fexofenadine 85-97 ATP binding cassette subfamily B member 1 Homo sapiens 9-13 15359574-8 2004 The IC50 of verapamil was 8.44 microM on the P-gp-mediated secretion of fexofenadine. fexofenadine 72-84 ATP binding cassette subfamily B member 1 Homo sapiens 45-49 15359574-10 2004 CONCLUSIONS: This study clearly indicates that P-gp was the main transport protein of fexofenadine in the Caco-2 model. fexofenadine 86-98 ATP binding cassette subfamily B member 1 Homo sapiens 47-51 14976396-0 2004 Suppressive activity of fexofenadine hydrochloride on thymus- and activation-regulated chemokine production from human peripheral blood leukocytes in response to antigenic stimulation in vitro. fexofenadine 24-50 C-C motif chemokine ligand 17 Homo sapiens 54-96 14976396-3 2004 The aim of this study is to examine the influence of fexofenadine hydrochloride (FEX), an H1-receptor antagonist, on TARC production from human peripheral blood leukocytes (PBL) using an in vitro cell culture technique. fexofenadine 53-79 C-C motif chemokine ligand 17 Homo sapiens 117-121 14976396-3 2004 The aim of this study is to examine the influence of fexofenadine hydrochloride (FEX), an H1-receptor antagonist, on TARC production from human peripheral blood leukocytes (PBL) using an in vitro cell culture technique. fexofenadine 81-84 C-C motif chemokine ligand 17 Homo sapiens 117-121 15536457-0 2004 A variant 2677A allele of the MDR1 gene affects fexofenadine disposition. fexofenadine 48-60 ATP binding cassette subfamily B member 1 Homo sapiens 30-34 15536457-3 2004 This study was performed to clarify the effects of major MDR1 gene polymorphisms, including a variant A allele in exon 21, on fexofenadine pharmacokinetics. fexofenadine 126-138 ATP binding cassette subfamily B member 1 Homo sapiens 57-61 15536457-5 2004 A single oral dose of 180 mg fexofenadine hydrochloride was administered to 33 healthy Korean male volunteers, who were divided into 6 groups based on the MDR1 genotype for the G2677T/A polymorphism in exon 21 and the C3435T polymorphism in exon 26. fexofenadine 29-55 ATP binding cassette subfamily B member 1 Homo sapiens 155-159 15352500-0 2004 A novel membrane sensor for histamine H1-receptor antagonist "fexofenadine". fexofenadine 62-74 histamine receptor H1 Homo sapiens 28-49 15312146-11 2004 Fexofenadine is a P-glycoprotein (P-gp) substrate and P-gp is certainly involved both in the poor brain penetration by the compound and, at least partially, in a number of observed drug interactions. fexofenadine 0-12 ATP binding cassette subfamily B member 1 Homo sapiens 18-32 15312146-11 2004 Fexofenadine is a P-glycoprotein (P-gp) substrate and P-gp is certainly involved both in the poor brain penetration by the compound and, at least partially, in a number of observed drug interactions. fexofenadine 0-12 ATP binding cassette subfamily B member 1 Homo sapiens 34-38 15125696-0 2004 Fexofenadine does not affect omeprazole pharmacokinetics: both are putative P-glycoprotein substrates. fexofenadine 0-12 ATP binding cassette subfamily B member 1 Homo sapiens 76-90 15125696-2 2004 Several studies have shown P-glycoprotein is involved in the absorption and excretion of fexofenadine. fexofenadine 89-101 ATP binding cassette subfamily B member 1 Homo sapiens 27-41 15125696-8 2004 In addition, the effect of fexofenadine on P-glycoprotein function was examined by flow cytometry using rhodamine 123 and CD56-positive lymphocytes. fexofenadine 27-39 ATP binding cassette subfamily B member 1 Homo sapiens 43-57 15180356-7 2004 Fexofenadine significantly inhibited IL6 (p < 0.004) and TNFalpha (p < 0.004) levels in comparison with placebo. fexofenadine 0-12 interleukin 6 Homo sapiens 37-40 15180356-7 2004 Fexofenadine significantly inhibited IL6 (p < 0.004) and TNFalpha (p < 0.004) levels in comparison with placebo. fexofenadine 0-12 tumor necrosis factor Homo sapiens 60-68 15180356-9 2004 Fexofenadine reduces TNFalpha and IL6 levels only. fexofenadine 0-12 tumor necrosis factor Homo sapiens 21-29 15180356-9 2004 Fexofenadine reduces TNFalpha and IL6 levels only. fexofenadine 0-12 interleukin 6 Homo sapiens 34-37 15217301-6 2004 With regard to the variability, polymorphisms of the MDR1 gene have recently been reported to be associated with alterations in disposition kinetics and interaction profiles of clinically useful drugs, including digoxin, fexofenadine, ciclosporin and talinolol. fexofenadine 221-233 ATP binding cassette subfamily B member 1 Homo sapiens 53-57 14610227-5 2004 Dehydroepiandrosterone-sulfate, estrone-3-sulfate, and fexofenadine were transported by OATP-B at both neutral and acidic pH, whereas estradiol-17beta-glucuronide, acetic acid, and lactic acid were not transported at all. fexofenadine 55-67 solute carrier organic anion transporter family member 2B1 Homo sapiens 88-94 15460210-1 2004 The influence of fexofenadine hydrochloride (FEX; CAS 138452-21-8) on the production of eosinophil chemoattractants, RANTES and eotaxin, from nasal polyp fibroblasts (NPFs) was examined in vitro. fexofenadine 45-48 C-C motif chemokine ligand 5 Homo sapiens 117-123 14530792-7 2003 In addition, fexofenadine has proven anti-inflammatory activity and has been shown to inhibit a number of mediators at clinically relevant concentrations, including in vitro inhibition of ICAM-1 expression on conjunctival and nasal epithelial cells. fexofenadine 13-25 intercellular adhesion molecule 1 Homo sapiens 188-194 14586383-11 2003 However, verapamil increased the apparent absorption rate constant into the systemic circulation and the area under the plasma concentration-time curve for fexofenadine from 0.0030 +/- 0.0012 min(-1) to 0.0255 +/- 0.0103 min(-1) (P <.001) and from 161 +/- 181 ng/mL x min to 664 +/- 537 ng/mL x min (P <.01), respectively. fexofenadine 156-168 MAX-like protein X Mus musculus 266-270 14586383-11 2003 However, verapamil increased the apparent absorption rate constant into the systemic circulation and the area under the plasma concentration-time curve for fexofenadine from 0.0030 +/- 0.0012 min(-1) to 0.0255 +/- 0.0103 min(-1) (P <.001) and from 161 +/- 181 ng/mL x min to 664 +/- 537 ng/mL x min (P <.01), respectively. fexofenadine 156-168 MAX-like protein X Mus musculus 293-297 14586383-14 2003 The most plausible mechanism is either decreased organic anion transporting polypeptide-mediated sinusoidal uptake or P-glycoprotein-mediated canalicular secretion of fexofenadine, or both. fexofenadine 167-179 ATP binding cassette subfamily B member 1 Homo sapiens 118-132 12575922-11 2002 After treatment with fexofenadine, there was a significant decrease in the expression of ELAM-1 (p= 0.02), VCAM-1 (p= 0.04) and tryptase (p= 0.04), whereas no relevant change was observed for the other parameters examined. fexofenadine 21-33 selectin E Homo sapiens 89-95 12411421-5 2002 In the present study the ability of fexofenadine to block the K897T HERG channel variant was investigated. fexofenadine 36-48 potassium voltage-gated channel subfamily H member 2 Homo sapiens 68-72 12575922-11 2002 After treatment with fexofenadine, there was a significant decrease in the expression of ELAM-1 (p= 0.02), VCAM-1 (p= 0.04) and tryptase (p= 0.04), whereas no relevant change was observed for the other parameters examined. fexofenadine 21-33 vascular cell adhesion molecule 1 Homo sapiens 107-113 11703220-5 2001 RESULTS: The total symptom score was reduced by fexofenadine (both dosages) at V2 (P=0.007), whereas placebo did not modify it. fexofenadine 48-60 nibrin Homo sapiens 76-81 12070109-5 2002 We tested terfenadine carboxylate (fexofenadine) and terfenadine, structurally similar drugs with markedly different affinities for HERG block, for rescue of trafficking-defective LQT2 mutations. fexofenadine 10-33 potassium voltage-gated channel subfamily H member 2 Homo sapiens 180-184 11994059-0 2002 MDR1 gene polymorphisms and disposition of the P-glycoprotein substrate fexofenadine. fexofenadine 72-84 ATP binding cassette subfamily B member 1 Homo sapiens 0-4 11994059-0 2002 MDR1 gene polymorphisms and disposition of the P-glycoprotein substrate fexofenadine. fexofenadine 72-84 ATP binding cassette subfamily B member 1 Homo sapiens 47-61 11823753-0 2002 Fruit juices inhibit organic anion transporting polypeptide-mediated drug uptake to decrease the oral availability of fexofenadine. fexofenadine 118-130 solute carrier organic anion transporter family member 1A2 Homo sapiens 21-59 11823753-3 2002 OATP-mediated fexofenadine uptake was measured in a transfected cell line. fexofenadine 14-26 solute carrier organic anion transporter family member 1A2 Homo sapiens 0-4 12087344-4 2002 Fexofenadine, 60 mg, was administered orally before administration of St John"s wort, with a single dose of St John"s wort (900 mg), and after 2 weeks of treatment with St John"s wort (300 mg 3 times a day) to determine P-glycoprotein activity. fexofenadine 0-12 ATP binding cassette subfamily B member 1 Homo sapiens 220-234 12134950-3 2002 Rhodamine123, fexofenadine and saquinavir were used as P-gp substrates. fexofenadine 14-26 phosphoglycolate phosphatase Rattus norvegicus 55-59 11503014-7 2001 In humans, MDR1*1 and MDR1*2 variants were associated with differences in fexofenadine levels, consistent with the in vitro data, with the area under the plasma level-time curve being almost 40% greater in the *1/*1 genotype compared with the *2/*2 and the *1/*2 heterozygotes having an intermediate value, suggesting enhanced in vivo P-glycoprotein activity among subjects with the MDR1*2 allele. fexofenadine 74-86 ATP binding cassette subfamily B member 1 Homo sapiens 11-15 11503014-7 2001 In humans, MDR1*1 and MDR1*2 variants were associated with differences in fexofenadine levels, consistent with the in vitro data, with the area under the plasma level-time curve being almost 40% greater in the *1/*1 genotype compared with the *2/*2 and the *1/*2 heterozygotes having an intermediate value, suggesting enhanced in vivo P-glycoprotein activity among subjects with the MDR1*2 allele. fexofenadine 74-86 ATP binding cassette subfamily B member 1 Homo sapiens 22-26 11503014-7 2001 In humans, MDR1*1 and MDR1*2 variants were associated with differences in fexofenadine levels, consistent with the in vitro data, with the area under the plasma level-time curve being almost 40% greater in the *1/*1 genotype compared with the *2/*2 and the *1/*2 heterozygotes having an intermediate value, suggesting enhanced in vivo P-glycoprotein activity among subjects with the MDR1*2 allele. fexofenadine 74-86 ATP binding cassette subfamily B member 1 Homo sapiens 22-26 11238657-6 2001 Histamine-induced beta-glucuronidase and IL-6 release and [Ca(2+)](i) elevation were inhibited by the selective H(1) antagonist fexofenadine (10(-7)-10(-4) M), but not by the H(2) antagonist ranitidine. fexofenadine 128-140 interleukin 6 Homo sapiens 41-45 11238657-6 2001 Histamine-induced beta-glucuronidase and IL-6 release and [Ca(2+)](i) elevation were inhibited by the selective H(1) antagonist fexofenadine (10(-7)-10(-4) M), but not by the H(2) antagonist ranitidine. fexofenadine 128-140 glucuronidase beta Homo sapiens 18-36 11257421-6 2001 In P-gp-deficient mice, DPDPE uptake was saturable (K(m) approximately 24 mM), and was inhibited by dexverapamil and the Oatp2 substrates digoxin, estradiol-17beta-glucuronide and fexofenadine. fexofenadine 180-192 solute carrier organic anion transporter family, member 1a4 Mus musculus 121-126 11238657-7 2001 Inhibition of histamine-induced beta-glucuronidase and IL-6 release by fexofenadine was concentration dependent and displayed the characteristics of a competitive antagonism (K(d) = 89 nM). fexofenadine 71-83 glucuronidase beta Homo sapiens 32-50 11238657-7 2001 Inhibition of histamine-induced beta-glucuronidase and IL-6 release by fexofenadine was concentration dependent and displayed the characteristics of a competitive antagonism (K(d) = 89 nM). fexofenadine 71-83 interleukin 6 Homo sapiens 55-59 11240975-7 2001 The amount of azacyclonol, a CYP3A4 mediated metabolite of fexofenadine, eliminated renally increased on average 2-fold after rifampin dosing; however, this pathway accounted for less than 0.5% of the dose. fexofenadine 59-71 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 29-35 10444235-6 1999 In fact, other molecules such as cetirizine, loratadine, acrivastine, and fexofenadine seem to lack both cardiotoxic potential and HERG-blocking ability at therapeutically relevant concentrations. fexofenadine 74-86 potassium voltage-gated channel subfamily H member 2 Homo sapiens 131-135 10730552-1 2000 UNLABELLED: Fexofenadine, the active metabolite of terfenadine, is a selective histamine H1 receptor antagonist that does not cross the blood brain barrier and appears to display some anti-inflammatory properties. fexofenadine 12-24 histamine receptor H1 Homo sapiens 79-100 10421612-0 1999 OATP and P-glycoprotein transporters mediate the cellular uptake and excretion of fexofenadine. fexofenadine 82-94 solute carrier organic anion transporter family member 1A2 Homo sapiens 0-4 10421612-0 1999 OATP and P-glycoprotein transporters mediate the cellular uptake and excretion of fexofenadine. fexofenadine 82-94 ATP binding cassette subfamily B member 1 Homo sapiens 9-23 10421612-3 1999 Utilizing a recombinant vaccinia expression system, members of the organic anion transporting polypeptide family, such as the human organic anion transporting polypeptide (OATP) and rat organic anion transporting polypeptides 1 and 2 (Oatp1 and Oatp2), were found to mediate [(14)C]fexofenadine cellular uptake. fexofenadine 282-294 solute carrier organic anion transporter family member 1A2 Homo sapiens 67-105 10421612-7 1999 administration of [(14)C]fexofenadine to mice lacking mdr1a-encoded P-gp resulted in 5- and 9-fold increases in the drug"s plasma and brain levels, respectively, compared with wild-type mice. fexofenadine 25-37 phosphoglycolate phosphatase Mus musculus 68-72 10421612-9 1999 Because OATP transporters and P-gp colocalize in organs of importance to drug disposition such as the liver, their activity provides an explanation for the heretofore unknown mechanism(s) responsible for fexofenadine"s disposition and suggests potentially similar roles in the disposition of other xenobiotics. fexofenadine 204-216 solute carrier organic anion transporter family member 1A2 Homo sapiens 8-12 10421612-9 1999 Because OATP transporters and P-gp colocalize in organs of importance to drug disposition such as the liver, their activity provides an explanation for the heretofore unknown mechanism(s) responsible for fexofenadine"s disposition and suggests potentially similar roles in the disposition of other xenobiotics. fexofenadine 204-216 ATP binding cassette subfamily B member 1 Homo sapiens 30-34 10496299-12 1999 Troglitazone may enhance the activities of cytochrome P450 (CYP) 3A and/or transporter(s) thereby reducing the plasma concentrations of terfenadine, cyclosporin, atorvastatin and fexofenadine. fexofenadine 179-191 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 43-67 10384858-7 1999 Fexofenadine, eliminated largely unchanged in the faeces and urine, has a terminal t1/2 beta of approximately 14 hours and duration of action of 24 hours, making it suitable for once or twice daily administration. fexofenadine 0-12 interleukin 1 receptor like 1 Homo sapiens 83-92 9892033-0 1998 Terfenadine and fexofenadine reduce in vitro ICAM-1 expression on human continuous cell lines. fexofenadine 16-28 intercellular adhesion molecule 1 Homo sapiens 45-51 9892033-3 1998 OBJECTIVE: The aim of the study was to evaluate the effect exerted by terfenadine and fexofenadine on adhesion molecules expression (CD54/ICAM-1 and CD29) of a human continuously cultured conjunctival epithelial cell line (WK) and a fibroblast cell line (HEL). fexofenadine 86-98 intercellular adhesion molecule 1 Homo sapiens 133-137 9892033-6 1998 RESULTS: Terfenadine and fexofenadine significantly reduced ICAM-1 basal expression on WK cells at the concentration of 1 microg/mL and 50 microg/mL, respectively. fexofenadine 25-37 intercellular adhesion molecule 1 Homo sapiens 60-66 9892033-7 1998 In addition, both terfenadine and fexofenadine were able to decrease soluble ICAM-1 levels in IFN gamma-stimulated WK cells. fexofenadine 34-46 intercellular adhesion molecule 1 Homo sapiens 77-83 9892033-7 1998 In addition, both terfenadine and fexofenadine were able to decrease soluble ICAM-1 levels in IFN gamma-stimulated WK cells. fexofenadine 34-46 interferon gamma Homo sapiens 94-103 9892033-8 1998 On HEL fibroblasts, fexofenadine only was able to inhibit ICAM-1 upregulation induced by IFN gamma. fexofenadine 20-32 intercellular adhesion molecule 1 Homo sapiens 58-64 9892033-8 1998 On HEL fibroblasts, fexofenadine only was able to inhibit ICAM-1 upregulation induced by IFN gamma. fexofenadine 20-32 interferon gamma Homo sapiens 89-98 9892033-9 1998 Concerning the release of fibroblast products, we observed a dose-dependent decrease of spontaneous IL6 release only in the presence of fexofenadine. fexofenadine 136-148 interleukin 6 Homo sapiens 100-103 9892033-10 1998 CONCLUSION: This study shows that terfenadine and fexofenadine exert a biologic effect directly on epithelial cells and fibroblasts reducing ICAM-1 expression and partially reducing soluble ICAM-1 release. fexofenadine 50-62 intercellular adhesion molecule 1 Homo sapiens 141-147 9892033-10 1998 CONCLUSION: This study shows that terfenadine and fexofenadine exert a biologic effect directly on epithelial cells and fibroblasts reducing ICAM-1 expression and partially reducing soluble ICAM-1 release. fexofenadine 50-62 intercellular adhesion molecule 1 Homo sapiens 190-196 9506246-1 1998 The nonsedating histamine H1 receptor antagonist fexofenadine is the active metabolite of terfenadine. fexofenadine 49-61 histamine receptor H1 Homo sapiens 16-37 9525460-7 1998 The eosinophil-induced release of IL-8, GM-CSF, and sICAM-1 from the HNEC was significantly attenuated by treatment with fexofenadine. fexofenadine 121-133 C-X-C motif chemokine ligand 8 Homo sapiens 34-38 9525460-7 1998 The eosinophil-induced release of IL-8, GM-CSF, and sICAM-1 from the HNEC was significantly attenuated by treatment with fexofenadine. fexofenadine 121-133 colony stimulating factor 2 Homo sapiens 40-46 33825113-1 2021 PURPOSE: Fexofenadine is a well-identified in vivo probe substrate of P-glycoprotein (P-gp) and/or organic anion transporting polypeptide (OATP). fexofenadine 9-21 ATP binding cassette subfamily B member 1 Homo sapiens 70-84 33825113-1 2021 PURPOSE: Fexofenadine is a well-identified in vivo probe substrate of P-glycoprotein (P-gp) and/or organic anion transporting polypeptide (OATP). fexofenadine 9-21 ATP binding cassette subfamily B member 1 Homo sapiens 86-90 33825113-1 2021 PURPOSE: Fexofenadine is a well-identified in vivo probe substrate of P-glycoprotein (P-gp) and/or organic anion transporting polypeptide (OATP). fexofenadine 9-21 solute carrier organic anion transporter family member 1A2 Homo sapiens 99-137 33825113-1 2021 PURPOSE: Fexofenadine is a well-identified in vivo probe substrate of P-glycoprotein (P-gp) and/or organic anion transporting polypeptide (OATP). fexofenadine 9-21 solute carrier organic anion transporter family member 1A2 Homo sapiens 139-143 33825113-2 2021 This work aimed to investigate the transplacental pharmacokinetics of fexofenadine enantiomers with and without the selective P-gp inhibitor fluoxetine. fexofenadine 70-82 ATP binding cassette subfamily B member 1 Homo sapiens 126-130 33825113-10 2021 CONCLUSIONS: Our study showed a low extent, slow rate of non-enantioselective placental transfer of fexofenadine enantiomers, indicating a limited fetal fexofenadine exposure mediated by placental P-gp and/or OATP2B1. fexofenadine 100-112 solute carrier organic anion transporter family member 2B1 Homo sapiens 209-216 28712300-14 2017 As proof of concept, incorporating OATP2B1 and P-gp markedly improved the EOC and predicted Cmax and Tmax for fexofenadine. fexofenadine 110-122 solute carrier organic anion transporter family member 2B1 Homo sapiens 35-42 28712300-14 2017 As proof of concept, incorporating OATP2B1 and P-gp markedly improved the EOC and predicted Cmax and Tmax for fexofenadine. fexofenadine 110-122 phosphoglycolate phosphatase Homo sapiens 47-51 35403732-6 2022 Administration of fexofenadine, a histamine H1 receptor antagonist, suppressed tumor growth in HFD-fed mice by reducing the number of myeloid-derived suppressor cells and suppressing IL6/STAT3 signaling. fexofenadine 18-30 histamine receptor H1 Mus musculus 34-55 34917820-3 2021 This study aimed to evaluate the effect of fexofenadine and fluticasone propionate on the gene expression levels of Interferon regulatory factor 4 (IRF4), B cell-activating transcription factor-like (BATF), and SPI1 gene-encoded protein (PU.1), essential transcription factors for Th9 cell differentiation, in AR patients. fexofenadine 43-55 interferon regulatory factor 4 Homo sapiens 116-146 34917820-3 2021 This study aimed to evaluate the effect of fexofenadine and fluticasone propionate on the gene expression levels of Interferon regulatory factor 4 (IRF4), B cell-activating transcription factor-like (BATF), and SPI1 gene-encoded protein (PU.1), essential transcription factors for Th9 cell differentiation, in AR patients. fexofenadine 43-55 interferon regulatory factor 4 Homo sapiens 148-152 34917820-3 2021 This study aimed to evaluate the effect of fexofenadine and fluticasone propionate on the gene expression levels of Interferon regulatory factor 4 (IRF4), B cell-activating transcription factor-like (BATF), and SPI1 gene-encoded protein (PU.1), essential transcription factors for Th9 cell differentiation, in AR patients. fexofenadine 43-55 basic leucine zipper ATF-like transcription factor Homo sapiens 155-198 34917820-3 2021 This study aimed to evaluate the effect of fexofenadine and fluticasone propionate on the gene expression levels of Interferon regulatory factor 4 (IRF4), B cell-activating transcription factor-like (BATF), and SPI1 gene-encoded protein (PU.1), essential transcription factors for Th9 cell differentiation, in AR patients. fexofenadine 43-55 basic leucine zipper ATF-like transcription factor Homo sapiens 200-204 34917820-3 2021 This study aimed to evaluate the effect of fexofenadine and fluticasone propionate on the gene expression levels of Interferon regulatory factor 4 (IRF4), B cell-activating transcription factor-like (BATF), and SPI1 gene-encoded protein (PU.1), essential transcription factors for Th9 cell differentiation, in AR patients. fexofenadine 43-55 Spi-1 proto-oncogene Homo sapiens 211-215 34917820-3 2021 This study aimed to evaluate the effect of fexofenadine and fluticasone propionate on the gene expression levels of Interferon regulatory factor 4 (IRF4), B cell-activating transcription factor-like (BATF), and SPI1 gene-encoded protein (PU.1), essential transcription factors for Th9 cell differentiation, in AR patients. fexofenadine 43-55 Spi-1 proto-oncogene Homo sapiens 238-242 34917820-7 2021 Overall, our results showed that after one month of treatment with fexofenadine and fluticasone propionate, the expression levels of IRF4 and BATF genes in AR patients decreased, which may be due to this treatment regimen. fexofenadine 67-79 interferon regulatory factor 4 Homo sapiens 133-137 34917820-7 2021 Overall, our results showed that after one month of treatment with fexofenadine and fluticasone propionate, the expression levels of IRF4 and BATF genes in AR patients decreased, which may be due to this treatment regimen. fexofenadine 67-79 basic leucine zipper ATF-like transcription factor Homo sapiens 142-146 34504840-0 2021 Fexofenadine Protects Against Intervertebral Disc Degeneration Through TNF Signaling. fexofenadine 0-12 tumor necrosis factor Rattus norvegicus 71-74 34826148-0 2022 Addition of oral Fexofenadine to topical therapy leads to a significantly greater reduction in the serum IL-31 levels in mild to moderate pediatric atopic dermatitis. fexofenadine 17-29 interleukin 31 Homo sapiens 105-110 34826148-6 2022 However, the serum IL-31 (ng/ml) decreased significantly from baseline in the fexofenadine group after 8 weeks of treatment. fexofenadine 78-90 interleukin 31 Homo sapiens 19-24 34826148-7 2022 CONCLUSIONS: Although we could not conclusively confirm the clinical efficacy of adding oral fexofenadine to topical treatment in AD, serological evaluation indicates that fexofenadine treatment can lead to significant lowering of serum IL-31 levels in AD patients. fexofenadine 93-105 interleukin 31 Homo sapiens 237-242 34826148-7 2022 CONCLUSIONS: Although we could not conclusively confirm the clinical efficacy of adding oral fexofenadine to topical treatment in AD, serological evaluation indicates that fexofenadine treatment can lead to significant lowering of serum IL-31 levels in AD patients. fexofenadine 172-184 interleukin 31 Homo sapiens 237-242 34681815-0 2021 Cytosolic Phospholipase A2 Is Required for Fexofenadine"s Therapeutic Effects against Inflammatory Bowel Disease in Mice. fexofenadine 43-55 phospholipase A2, group IVA (cytosolic, calcium-dependent) Mus musculus 0-26 34681815-3 2021 We recently identified fexofenadine, a well-known antagonist of histamine H1 receptor, as a novel inhibitor of TNFalpha signaling. fexofenadine 23-35 histamine receptor H1 Mus musculus 64-85 34681815-3 2021 We recently identified fexofenadine, a well-known antagonist of histamine H1 receptor, as a novel inhibitor of TNFalpha signaling. fexofenadine 23-35 tumor necrosis factor Mus musculus 111-119 34681815-4 2021 Additionally, cytosolic phospholipase A2 (cPLA2) was isolated as a binding target of fexofenadine, and fexofenadine-mediated anti-TNF activity relied on cPLA2 in vitro. fexofenadine 85-97 phospholipase A2, group IVA (cytosolic, calcium-dependent) Mus musculus 14-40 34681815-4 2021 Additionally, cytosolic phospholipase A2 (cPLA2) was isolated as a binding target of fexofenadine, and fexofenadine-mediated anti-TNF activity relied on cPLA2 in vitro. fexofenadine 85-97 phospholipase A2, group IVA (cytosolic, calcium-dependent) Mus musculus 42-47 34681815-4 2021 Additionally, cytosolic phospholipase A2 (cPLA2) was isolated as a binding target of fexofenadine, and fexofenadine-mediated anti-TNF activity relied on cPLA2 in vitro. fexofenadine 103-115 phospholipase A2, group IVA (cytosolic, calcium-dependent) Mus musculus 14-40 34681815-4 2021 Additionally, cytosolic phospholipase A2 (cPLA2) was isolated as a binding target of fexofenadine, and fexofenadine-mediated anti-TNF activity relied on cPLA2 in vitro. fexofenadine 103-115 phospholipase A2, group IVA (cytosolic, calcium-dependent) Mus musculus 42-47 34681815-4 2021 Additionally, cytosolic phospholipase A2 (cPLA2) was isolated as a binding target of fexofenadine, and fexofenadine-mediated anti-TNF activity relied on cPLA2 in vitro. fexofenadine 103-115 tumor necrosis factor Mus musculus 130-133 34681815-4 2021 Additionally, cytosolic phospholipase A2 (cPLA2) was isolated as a binding target of fexofenadine, and fexofenadine-mediated anti-TNF activity relied on cPLA2 in vitro. fexofenadine 103-115 phospholipase A2, group IVA (cytosolic, calcium-dependent) Mus musculus 153-158 34681815-5 2021 The objective of this study is to determine whether fexofenadine is therapeutic against chemically-induced murine IBD model and whether cPLA2 and/or histamine H1 receptor is important for fexofenadine"s anti-inflammatory activity in vivo by leveraging various genetically modified mice and chemically induced murine IBD models. fexofenadine 188-200 phospholipase A2, group IVA (cytosolic, calcium-dependent) Mus musculus 136-141 34681815-5 2021 The objective of this study is to determine whether fexofenadine is therapeutic against chemically-induced murine IBD model and whether cPLA2 and/or histamine H1 receptor is important for fexofenadine"s anti-inflammatory activity in vivo by leveraging various genetically modified mice and chemically induced murine IBD models. fexofenadine 188-200 histamine receptor H1 Mus musculus 149-170 34681815-6 2021 Both dextran sulfate sodium- and 2, 4, 6-trinitrobenzene sulfonic acid-induced murine IBD models revealed that orally delivered fexofenadine was therapeutic against IBD, evidenced by mitigated clinical symptoms, decreased secretions of the proinflammatory cytokine IL-6 and IL-1beta, lowered intestinal inflammation, and reduced p-p65 and p-IkBalpha. fexofenadine 128-140 interleukin 6 Mus musculus 265-269 34681815-6 2021 Both dextran sulfate sodium- and 2, 4, 6-trinitrobenzene sulfonic acid-induced murine IBD models revealed that orally delivered fexofenadine was therapeutic against IBD, evidenced by mitigated clinical symptoms, decreased secretions of the proinflammatory cytokine IL-6 and IL-1beta, lowered intestinal inflammation, and reduced p-p65 and p-IkBalpha. fexofenadine 128-140 interleukin 1 alpha Mus musculus 274-282 34681815-6 2021 Both dextran sulfate sodium- and 2, 4, 6-trinitrobenzene sulfonic acid-induced murine IBD models revealed that orally delivered fexofenadine was therapeutic against IBD, evidenced by mitigated clinical symptoms, decreased secretions of the proinflammatory cytokine IL-6 and IL-1beta, lowered intestinal inflammation, and reduced p-p65 and p-IkBalpha. fexofenadine 128-140 v-rel reticuloendotheliosis viral oncogene homolog A (avian) Mus musculus 331-334 34681815-7 2021 Intriguingly, Fexofenadine-mediated protective effects against IBD were lost in cPLA2 deficient mice but not in histamine H1 receptor-deficient mice. fexofenadine 14-26 phospholipase A2, group IVA (cytosolic, calcium-dependent) Mus musculus 80-85 34681815-8 2021 Collectively, these findings demonstrate the therapeutic effects of over-the-counter drug Fexofenadine in treating DSS-induced IBD murine and provide first in vivo evidence showing that cPLA2 is required for fexofenadine"s therapeutic effects in murine IBD model and probably other inflammatory and autoimmune diseases as well. fexofenadine 208-220 phospholipase A2, group IVA (cytosolic, calcium-dependent) Mus musculus 186-191 35403732-6 2022 Administration of fexofenadine, a histamine H1 receptor antagonist, suppressed tumor growth in HFD-fed mice by reducing the number of myeloid-derived suppressor cells and suppressing IL6/STAT3 signaling. fexofenadine 18-30 interleukin 6 Mus musculus 183-186 35403732-6 2022 Administration of fexofenadine, a histamine H1 receptor antagonist, suppressed tumor growth in HFD-fed mice by reducing the number of myeloid-derived suppressor cells and suppressing IL6/STAT3 signaling. fexofenadine 18-30 signal transducer and activator of transcription 3 Mus musculus 187-192 33372901-2 2020 Pgp activity was analyzed in a transwell system by the transport of its substrate, fexofenadine. fexofenadine 83-95 ATP binding cassette subfamily B member 1 Homo sapiens 0-3 35455642-7 2022 CYP3A and P-gp phenotypic activities were assessed by the metabolic ratio of midazolam and AUC0-6h of fexofenadine, respectively. fexofenadine 102-114 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-5 35455642-7 2022 CYP3A and P-gp phenotypic activities were assessed by the metabolic ratio of midazolam and AUC0-6h of fexofenadine, respectively. fexofenadine 102-114 phosphoglycolate phosphatase Homo sapiens 10-14 33256506-0 2021 Effects of Breviscapine and C3435T MDR1 gene polymorphism on the pharmacokinetics of fexofenadine, a P-glycoprotein substrate, in healthy volunteers. fexofenadine 85-97 ATP binding cassette subfamily B member 1 Homo sapiens 35-39 33256506-0 2021 Effects of Breviscapine and C3435T MDR1 gene polymorphism on the pharmacokinetics of fexofenadine, a P-glycoprotein substrate, in healthy volunteers. fexofenadine 85-97 ATP binding cassette subfamily B member 1 Homo sapiens 101-115 33256506-4 2021 The aim of this study was to evaluate the effect of BRE on the pharmacokinetics of fexofenadine, a P-gp probe substrate and its associations with the MDR1 C3435T genetic polymorphism in healthy volunteers. fexofenadine 83-95 ATP binding cassette subfamily B member 1 Homo sapiens 99-103 33256506-4 2021 The aim of this study was to evaluate the effect of BRE on the pharmacokinetics of fexofenadine, a P-gp probe substrate and its associations with the MDR1 C3435T genetic polymorphism in healthy volunteers. fexofenadine 83-95 ATP binding cassette subfamily B member 1 Homo sapiens 150-154 33832418-5 2021 The transport of the P-gp substrate fexofenadine was evaluated in a special Transwell system. fexofenadine 36-48 ATP binding cassette subfamily B member 1 Homo sapiens 21-25 35230114-3 2022 Inhibitory potency was assessed by examining the uptake of (3H)estrone 3-sulfate and (3H)fexofenadine into HEK293 cells expressing OATP1A2 or OATP2B1. fexofenadine 89-101 solute carrier organic anion transporter family member 1A2 Homo sapiens 131-138 32571913-6 2020 40, a common azo dye excipient and a potent inhibitor of OATP2B1, decreased the plasma level of the OATP2B1 substrate fexofenadine, suggesting that FD&C Red No. fexofenadine 118-130 solute carrier organic anion transporter family member 2B1 Homo sapiens 57-64 32571913-6 2020 40, a common azo dye excipient and a potent inhibitor of OATP2B1, decreased the plasma level of the OATP2B1 substrate fexofenadine, suggesting that FD&C Red No. fexofenadine 118-130 solute carrier organic anion transporter family member 2B1 Homo sapiens 100-107 32557079-2 2020 Fexofenadine, an in vivo P-gp probe, is an antihistamine drug for seasonal allergic rhinitis and chronic urticaria treatment during pregnancy and it is available as a racemic mixture. fexofenadine 0-12 ATP binding cassette subfamily B member 1 Homo sapiens 25-29 32557079-10 2020 CONCLUSIONS: A single oral dose of 40 mg fluoxetine inhibited the intestinal P-gp mediated transport of S-(-)-fexofenadine to a greater extent than R-(+)-fexofenadine in parturient women. fexofenadine 104-122 ATP binding cassette subfamily B member 1 Homo sapiens 77-81 30652318-5 2019 In contrast, atorvastatin, bosentan, etoposide, fexofenadine, fluvastatin, glibenclamide and simeprevir were broadly transported by recombinant monkey OATP1B1, OATP1B3 and OATP2B1. fexofenadine 48-60 solute carrier organic anion transporter family member 1B1 Homo sapiens 151-158 32078103-8 2020 The absorption of oral verapamil, diltiazem and tacrolimus was not influenced by elacridar pre-treatment, and the increase in the AUC0-t of fexofenadine was approximately 3-fold when co-administered with each substrate; the minimal effect of elacridar was attributable to the limited contribution of P-gp but not to their self-inhibition against the transporter. fexofenadine 140-152 ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus 300-304 32115554-3 2020 In the present study, we designed a prodrug of fexofenadine (FXD) as a model parent drug that is resistant to hCE2 but hydrolyzed by hCE1, utilizing the differences in catalytic characteristics of hCE1 and hCE2. fexofenadine 47-59 carboxylesterase 2 Homo sapiens 110-114 32115554-3 2020 In the present study, we designed a prodrug of fexofenadine (FXD) as a model parent drug that is resistant to hCE2 but hydrolyzed by hCE1, utilizing the differences in catalytic characteristics of hCE1 and hCE2. fexofenadine 47-59 carboxylesterase 1 Homo sapiens 133-137 32115554-3 2020 In the present study, we designed a prodrug of fexofenadine (FXD) as a model parent drug that is resistant to hCE2 but hydrolyzed by hCE1, utilizing the differences in catalytic characteristics of hCE1 and hCE2. fexofenadine 47-59 carboxylesterase 1 Homo sapiens 197-201 32115554-3 2020 In the present study, we designed a prodrug of fexofenadine (FXD) as a model parent drug that is resistant to hCE2 but hydrolyzed by hCE1, utilizing the differences in catalytic characteristics of hCE1 and hCE2. fexofenadine 47-59 carboxylesterase 2 Homo sapiens 206-210 31581637-4 2019 As part of a study evaluating potential drug-drug interactions between probe drugs of the Geneva cocktail, the present paper focuses on the impact of cytochromes (CYP) probe drugs on the disposition of fexofenadine, a P-gp test drug. fexofenadine 202-214 peptidylprolyl isomerase G Homo sapiens 163-166 31581637-4 2019 As part of a study evaluating potential drug-drug interactions between probe drugs of the Geneva cocktail, the present paper focuses on the impact of cytochromes (CYP) probe drugs on the disposition of fexofenadine, a P-gp test drug. fexofenadine 202-214 ATP binding cassette subfamily B member 1 Homo sapiens 218-222 31183371-8 2019 Conclusions: Our study revealed for the first time that second-generation antihistamines, including cetirizine, fexofenadine, azelastine, and terfenadine, exert suppressive effects on lymphocyte Kv1.3-channels. fexofenadine 112-124 potassium voltage-gated channel, shaker-related subfamily, member 3 Mus musculus 195-200 31317804-3 2020 Buspirone and fexofenadine, probe substrates of CYP3A and P-glycoprotein (P-gp), respectively, were orally co-administered to rats with bergamottin (2.5 mg/kg) or orally administered 2 h after bergamottin pre-treatment. fexofenadine 14-26 cytochrome P450, family 3, subfamily a, polypeptide 62 Rattus norvegicus 48-53 31317804-3 2020 Buspirone and fexofenadine, probe substrates of CYP3A and P-glycoprotein (P-gp), respectively, were orally co-administered to rats with bergamottin (2.5 mg/kg) or orally administered 2 h after bergamottin pre-treatment. fexofenadine 14-26 ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus 58-72 31317804-3 2020 Buspirone and fexofenadine, probe substrates of CYP3A and P-glycoprotein (P-gp), respectively, were orally co-administered to rats with bergamottin (2.5 mg/kg) or orally administered 2 h after bergamottin pre-treatment. fexofenadine 14-26 ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus 74-78 31746415-12 2020 In 293-OATP1A2 cells, the uptake of FEX without OATP1A2 inhibitor naringenin (100 microg/ml) was 2.8-fold higher compared with that in the presence of naringenin, and the uptake of fentanyl without naringenin was 7.3-fold higher compared with that in the presence of naringenin (100 microg/ml). fexofenadine 36-39 solute carrier organic anion transporter family member 1A2 Homo sapiens 7-14 31302596-0 2019 Fexofenadine inhibits TNF signaling through targeting to cytosolic phospholipase A2 and is therapeutic against inflammatory arthritis. fexofenadine 0-12 tumor necrosis factor Mus musculus 22-25 31302596-0 2019 Fexofenadine inhibits TNF signaling through targeting to cytosolic phospholipase A2 and is therapeutic against inflammatory arthritis. fexofenadine 0-12 phospholipase A2, group IVA (cytosolic, calcium-dependent) Mus musculus 57-83 31302596-3 2019 METHODS: In vitro and in vivo screening of an Food and Drug Administration (FDA)-approved drug library; in vitro and in vivo assays for examining the blockade of TNF actions by fexofenadine: assays for defining the anti-inflammatory activity of fexofenadine using TNF-alpha transgenic (TNF-tg) mice and collagen-induced arthritis in DBA/1 mice. fexofenadine 177-189 tumor necrosis factor Mus musculus 162-165 31302596-4 2019 Identification and characterisation of the binding of fexofenadine to cytosolic phospholipase A2 (cPLA2) using drug affinity responsive target stability assay, proteomics, cellular thermal shift assay, information field dynamics and molecular dynamics; various assays for examining fexofenadine inhibition of cPLA2 as well as the dependence of fexofenadine"s anti-TNF activity on cPLA2. fexofenadine 54-66 phospholipase A2, group IVA (cytosolic, calcium-dependent) Mus musculus 70-96 31302596-4 2019 Identification and characterisation of the binding of fexofenadine to cytosolic phospholipase A2 (cPLA2) using drug affinity responsive target stability assay, proteomics, cellular thermal shift assay, information field dynamics and molecular dynamics; various assays for examining fexofenadine inhibition of cPLA2 as well as the dependence of fexofenadine"s anti-TNF activity on cPLA2. fexofenadine 54-66 phospholipase A2, group IVA (cytosolic, calcium-dependent) Mus musculus 98-103 31302596-4 2019 Identification and characterisation of the binding of fexofenadine to cytosolic phospholipase A2 (cPLA2) using drug affinity responsive target stability assay, proteomics, cellular thermal shift assay, information field dynamics and molecular dynamics; various assays for examining fexofenadine inhibition of cPLA2 as well as the dependence of fexofenadine"s anti-TNF activity on cPLA2. fexofenadine 54-66 phospholipase A2, group IVA (cytosolic, calcium-dependent) Mus musculus 309-314 31302596-4 2019 Identification and characterisation of the binding of fexofenadine to cytosolic phospholipase A2 (cPLA2) using drug affinity responsive target stability assay, proteomics, cellular thermal shift assay, information field dynamics and molecular dynamics; various assays for examining fexofenadine inhibition of cPLA2 as well as the dependence of fexofenadine"s anti-TNF activity on cPLA2. fexofenadine 54-66 tumor necrosis factor Mus musculus 364-367 31302596-4 2019 Identification and characterisation of the binding of fexofenadine to cytosolic phospholipase A2 (cPLA2) using drug affinity responsive target stability assay, proteomics, cellular thermal shift assay, information field dynamics and molecular dynamics; various assays for examining fexofenadine inhibition of cPLA2 as well as the dependence of fexofenadine"s anti-TNF activity on cPLA2. fexofenadine 54-66 phospholipase A2, group IVA (cytosolic, calcium-dependent) Mus musculus 309-314 31302596-4 2019 Identification and characterisation of the binding of fexofenadine to cytosolic phospholipase A2 (cPLA2) using drug affinity responsive target stability assay, proteomics, cellular thermal shift assay, information field dynamics and molecular dynamics; various assays for examining fexofenadine inhibition of cPLA2 as well as the dependence of fexofenadine"s anti-TNF activity on cPLA2. fexofenadine 282-294 phospholipase A2, group IVA (cytosolic, calcium-dependent) Mus musculus 70-96 31302596-4 2019 Identification and characterisation of the binding of fexofenadine to cytosolic phospholipase A2 (cPLA2) using drug affinity responsive target stability assay, proteomics, cellular thermal shift assay, information field dynamics and molecular dynamics; various assays for examining fexofenadine inhibition of cPLA2 as well as the dependence of fexofenadine"s anti-TNF activity on cPLA2. fexofenadine 282-294 phospholipase A2, group IVA (cytosolic, calcium-dependent) Mus musculus 98-103 31302596-4 2019 Identification and characterisation of the binding of fexofenadine to cytosolic phospholipase A2 (cPLA2) using drug affinity responsive target stability assay, proteomics, cellular thermal shift assay, information field dynamics and molecular dynamics; various assays for examining fexofenadine inhibition of cPLA2 as well as the dependence of fexofenadine"s anti-TNF activity on cPLA2. fexofenadine 282-294 phospholipase A2, group IVA (cytosolic, calcium-dependent) Mus musculus 70-96 31302596-4 2019 Identification and characterisation of the binding of fexofenadine to cytosolic phospholipase A2 (cPLA2) using drug affinity responsive target stability assay, proteomics, cellular thermal shift assay, information field dynamics and molecular dynamics; various assays for examining fexofenadine inhibition of cPLA2 as well as the dependence of fexofenadine"s anti-TNF activity on cPLA2. fexofenadine 282-294 phospholipase A2, group IVA (cytosolic, calcium-dependent) Mus musculus 98-103 31302596-5 2019 RESULTS: Serial screenings of a library composed of FDA-approved drugs led to the identification of fexofenadine as an inhibitor of TNF-alpha signalling. fexofenadine 100-112 tumor necrosis factor Mus musculus 132-141 31302596-7 2019 cPLA2 was isolated as a novel target of fexofenadine. fexofenadine 40-52 phospholipase A2, group IVA (cytosolic, calcium-dependent) Mus musculus 0-5 31302596-8 2019 Fexofenadine blocked TNF-stimulated cPLA2 activity and arachidonic acid production through binding to catalytic domain 2 of cPLA2 and inhibition of its phosphorylation on Ser-505. fexofenadine 0-12 tumor necrosis factor Mus musculus 21-24 31302596-8 2019 Fexofenadine blocked TNF-stimulated cPLA2 activity and arachidonic acid production through binding to catalytic domain 2 of cPLA2 and inhibition of its phosphorylation on Ser-505. fexofenadine 0-12 phospholipase A2, group IVA (cytosolic, calcium-dependent) Mus musculus 36-41 31302596-8 2019 Fexofenadine blocked TNF-stimulated cPLA2 activity and arachidonic acid production through binding to catalytic domain 2 of cPLA2 and inhibition of its phosphorylation on Ser-505. fexofenadine 0-12 phospholipase A2, group IVA (cytosolic, calcium-dependent) Mus musculus 124-129 31302596-9 2019 Further, deletion of cPLA2 abolished fexofenadine"s anti-TNF activity. fexofenadine 37-49 phospholipase A2, group IVA (cytosolic, calcium-dependent) Mus musculus 21-26 31302596-9 2019 Further, deletion of cPLA2 abolished fexofenadine"s anti-TNF activity. fexofenadine 37-49 tumor necrosis factor Mus musculus 57-60 31302596-10 2019 CONCLUSION: Collectively, these findings not only provide new insights into the understanding of fexofenadine action and underlying mechanisms but also provide new therapeutic interventions for various TNF-alpha and cPLA2-associated pathologies and conditions, particularly inflammatory rheumatic diseases. fexofenadine 97-109 tumor necrosis factor Mus musculus 202-211 31302596-10 2019 CONCLUSION: Collectively, these findings not only provide new insights into the understanding of fexofenadine action and underlying mechanisms but also provide new therapeutic interventions for various TNF-alpha and cPLA2-associated pathologies and conditions, particularly inflammatory rheumatic diseases. fexofenadine 97-109 phospholipase A2, group IVA (cytosolic, calcium-dependent) Mus musculus 216-221 30875094-0 2019 Modulation of Fexofenadine Pharmacokinetics by Osimertinib in Patients With Advanced EGFR-Mutated Non-Small Cell Lung Cancer. fexofenadine 14-26 epidermal growth factor receptor Homo sapiens 85-89 30953868-10 2019 CONCLUSIONS: This study shows that fexofenadine (FXF - antihistamine drug) and osthole exhibit selective COX-2 enzyme inhibitory activity. fexofenadine 35-47 mitochondrially encoded cytochrome c oxidase II Homo sapiens 105-110 30652318-5 2019 In contrast, atorvastatin, bosentan, etoposide, fexofenadine, fluvastatin, glibenclamide and simeprevir were broadly transported by recombinant monkey OATP1B1, OATP1B3 and OATP2B1. fexofenadine 48-60 solute carrier organic anion transporter family member 1B3 Homo sapiens 160-167 30652318-5 2019 In contrast, atorvastatin, bosentan, etoposide, fexofenadine, fluvastatin, glibenclamide and simeprevir were broadly transported by recombinant monkey OATP1B1, OATP1B3 and OATP2B1. fexofenadine 48-60 solute carrier organic anion transporter family member 2B1 Homo sapiens 172-179 30280663-2 2019 This guidance has indicated that digoxin, dabigatran etexilate and fexofenadine are P-gp substrate drugs and has defined P-gp inhibitors as those that increase the AUC of digoxin by 1.25-fold in clinical DDI studies. fexofenadine 67-79 ATP binding cassette subfamily B member 1 Homo sapiens 84-88 30280663-2 2019 This guidance has indicated that digoxin, dabigatran etexilate and fexofenadine are P-gp substrate drugs and has defined P-gp inhibitors as those that increase the AUC of digoxin by 1.25-fold in clinical DDI studies. fexofenadine 67-79 ATP binding cassette subfamily B member 1 Homo sapiens 121-125 30742585-0 2019 Effect of the Fexofenadine on the expression of HRH-1 and HRH-4 receptor in Peripheral Blood Mononuclear Cell isolated from children with diagnosed allergy - in vitro study Short communication. fexofenadine 14-26 histamine receptor H1 Homo sapiens 48-53 30280663-4 2019 OBJECTIVE: Since there are no detailed manuscripts that summarizes P-gp interactions unrelated to CYP metabolism, this article reviews the effects of potent P-gp inhibitors and P-gp inducers on the pharmacokinetics of P-gp substrate drugs, including digoxin, talinolol, dabigatran etexilate, and fexofenadine in human studies. fexofenadine 296-308 ATP binding cassette subfamily B member 1 Homo sapiens 157-161 30280663-4 2019 OBJECTIVE: Since there are no detailed manuscripts that summarizes P-gp interactions unrelated to CYP metabolism, this article reviews the effects of potent P-gp inhibitors and P-gp inducers on the pharmacokinetics of P-gp substrate drugs, including digoxin, talinolol, dabigatran etexilate, and fexofenadine in human studies. fexofenadine 296-308 ATP binding cassette subfamily B member 1 Homo sapiens 157-161 30280663-4 2019 OBJECTIVE: Since there are no detailed manuscripts that summarizes P-gp interactions unrelated to CYP metabolism, this article reviews the effects of potent P-gp inhibitors and P-gp inducers on the pharmacokinetics of P-gp substrate drugs, including digoxin, talinolol, dabigatran etexilate, and fexofenadine in human studies. fexofenadine 296-308 ATP binding cassette subfamily B member 1 Homo sapiens 157-161 27864798-8 2017 One study using a midazolam probe found weak CYP3A induction and another using a fexofenadine probe found weak P-gp inhibition. fexofenadine 81-93 phosphoglycolate phosphatase Homo sapiens 111-115 30020547-1 2018 Thirty-two Collies were used to determine the impact of ABCB1 genotype and phenotype on the plasma pharmacokinetics of fexofenadine"s (Fex) R- and S-enantiomers after bolus Fex administration, as human P-gp exhibits stereoselectivity. fexofenadine 119-131 ATP binding cassette subfamily B member 1 Homo sapiens 56-61 30009812-11 2018 These results indicate that both blood brain barrier penetrating (chlorpheniramine) and poorly penetrating (fexofenadine) histamine H1 receptor antagonists could improve the neuropathic pain sign, but only the blood brain barrier penetrating histamine H2 receptor antagonist (ranitidine) could produce anti-allodynic effects in the TNT model of neuropathic pain in rats. fexofenadine 108-120 histamine receptor H 1 Rattus norvegicus 122-143 29635947-5 2018 Expert opinion: Differences in pharmacokinetics between fexofenadine enantiomers were caused by organic anion transporting polypeptide (OATP) 2B1, with a minor contribution from P-glycoprotein (P-gp). fexofenadine 56-68 solute carrier organic anion transporter family member 2B1 Homo sapiens 96-145 29635947-7 2018 P-gp inducers, carbamazepine, and inhibitors such as itraconazole and verapamil show greater effects on the pharmacokinetics of (S)-fexofenadine. fexofenadine 128-144 ATP binding cassette subfamily B member 1 Homo sapiens 0-4 29635947-8 2018 Apple juice and grape fruit juice, OATP2B1 inhibitors, significantly decrease the exposure of both fexofenadine enantiomers, particularly the (S)-enantiomer, but do not change the t1/2. fexofenadine 99-111 solute carrier organic anion transporter family member 2B1 Homo sapiens 35-42 29635947-9 2018 Rifampicin significantly increases plasma concentrations of both enantiomers through inhibition of OATP1B3, whereas enantioselectivity of fexofenadine uptake by OATP1B3-expressing cells has not been observed. fexofenadine 138-150 solute carrier organic anion transporter family member 1B3 Homo sapiens 161-168 29635947-10 2018 Combinations of multiple transporters such as OATP2B1 and P-gp facilitate enantioselective disposition of fexofenadine. fexofenadine 106-118 solute carrier organic anion transporter family member 2B1 Homo sapiens 46-53 29635947-10 2018 Combinations of multiple transporters such as OATP2B1 and P-gp facilitate enantioselective disposition of fexofenadine. fexofenadine 106-118 ATP binding cassette subfamily B member 1 Homo sapiens 58-62 29378195-8 2018 Treatment of HepG2 cells with other H1 receptor antagonists including fexofenadine, cetirizine, and diphenhydramine increased apo A-I levels in a dose-dependent manner while treatment with H2 receptor antagonists including cimetidine, famotidine, and ranitidine had no effect. fexofenadine 70-82 apolipoprotein A1 Homo sapiens 126-133 27109454-0 2017 Binding of fexofenadine hydrochloride to bovine serum albumin: structural considerations by spectroscopic techniques and molecular docking. fexofenadine 11-37 albumin Homo sapiens 48-61 28544909-0 2017 Can human allergy drug fexofenadine, an antagonist of histamine (H1) receptor, be used to treat dog and cat? fexofenadine 23-35 histamine receptor H1 Homo sapiens 54-77 28521025-5 2017 Then we explored pharmacological rescue strategies on As2O3-induced LQTS, and found that 4 therapeutic agents exert rescue efficacy via 3 different pathways: fexofenadine and astemizole facilitate hERG trafficking via promotion of channel-chaperone formation after As2O3 incubation; ranolazine slows hERG degradation in the presence of As2O3; and resveratrol shows significant attenuation on calcium current increase triggered by As2O3. fexofenadine 158-170 ETS transcription factor ERG Homo sapiens 197-201 28521025-5 2017 Then we explored pharmacological rescue strategies on As2O3-induced LQTS, and found that 4 therapeutic agents exert rescue efficacy via 3 different pathways: fexofenadine and astemizole facilitate hERG trafficking via promotion of channel-chaperone formation after As2O3 incubation; ranolazine slows hERG degradation in the presence of As2O3; and resveratrol shows significant attenuation on calcium current increase triggered by As2O3. fexofenadine 158-170 ETS transcription factor ERG Homo sapiens 300-304 28102715-0 2017 Capsaicin pretreatment enhanced the bioavailability of fexofenadine in rats by P-glycoprotein modulation: in vitro, in situ and in vivo evaluation. fexofenadine 55-67 ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus 79-93 28102715-2 2017 Therefore, purpose of this study was to evaluate the effect of capsaicin on intestinal absorption and bioavailability of fexofenadine, a P-gp substrate in rats. fexofenadine 121-133 ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus 137-141 28102715-9 2017 CONCLUSIONS: Capsaicin pretreatment significantly enhanced the intestinal absorption and bioavailability of fexofenadine in rats likely by inhibition of P-gp mediated cellular efflux, suggesting that the combined use of capsaicin with P-gp substrates may require close monitoring for potential drug interactions. fexofenadine 108-120 ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus 153-157 28102715-9 2017 CONCLUSIONS: Capsaicin pretreatment significantly enhanced the intestinal absorption and bioavailability of fexofenadine in rats likely by inhibition of P-gp mediated cellular efflux, suggesting that the combined use of capsaicin with P-gp substrates may require close monitoring for potential drug interactions. fexofenadine 108-120 ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus 235-239 28188296-1 2017 The aim of this study was to determine the effects of garlic and ginkgo herbal extracts on the pharmacokinetics of the P-glycoprotein (P-gp)/organic anion-transporting polypeptides (Oatps) substrate fexofenadine. fexofenadine 199-211 phosphoglycolate phosphatase Rattus norvegicus 135-139 28301431-5 2017 In addition, oral fexofenadine was used as an in vivo probe for P-gp activity. fexofenadine 18-30 ATP binding cassette subfamily B member 1 Homo sapiens 64-68 27109454-1 2017 The binding interaction of peripheral H1 receptor antagonist drug, fexofenadine hydrochloride to bovine serum albumin (BSA) is investigated by fluorescence spectroscopy in combination with UV-absorption spectroscopy under physiological conditions. fexofenadine 67-93 albumin Homo sapiens 104-117 28040476-7 2017 The mutation of Asp2.50 (Asp73) to asparagine abrogated NaCl-induced reductions in affinities for histamine and d-chlorpheniramine, but not NaCl-induced increases in the affinity for fexofenadine. fexofenadine 183-195 beta-secretase 1 Homo sapiens 16-20 27981349-0 2017 The influence of piperine on the pharmacokinetics of fexofenadine, a P-glycoprotein substrate, in healthy volunteers. fexofenadine 53-65 ATP binding cassette subfamily B member 1 Homo sapiens 69-83 27981349-2 2017 The aim of this study was to evaluate the effect of PIP on the pharmacokinetics of fexofenadine (FEX), a P-gp substrate, in healthy volunteers. fexofenadine 83-95 ATP binding cassette subfamily B member 1 Homo sapiens 105-109 27981349-2 2017 The aim of this study was to evaluate the effect of PIP on the pharmacokinetics of fexofenadine (FEX), a P-gp substrate, in healthy volunteers. fexofenadine 97-100 ATP binding cassette subfamily B member 1 Homo sapiens 105-109 27843000-0 2017 Changes in gene expression induced by histamine, fexofenadine and osthole: Expression of histamine H1 receptor, COX-2, NF-kappaB, CCR1, chemokine CCL5/RANTES and interleukin-1beta in PBMC allergic and non-allergic patients. fexofenadine 49-61 histamine receptor H1 Homo sapiens 89-110 27074034-5 2016 Subjects were randomly assigned to take either a combined H1R and H2R antagonist (fexofenadine and ranitidine) or a control placebo. fexofenadine 82-94 histamine receptor H2 Homo sapiens 66-69 28090646-0 2017 Influence of P-glycoprotein on the disposition of fexofenadine and its enantiomers. fexofenadine 50-62 ATP binding cassette subfamily B member 1 Homo sapiens 13-27 28090646-3 2017 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 6-18 ATP binding cassette subfamily B member 1 Homo sapiens 120-124 28090646-3 2017 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 147-159 ATP binding cassette subfamily B member 1 Homo sapiens 120-124 28090646-8 2017 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 69-85 ATP binding cassette subfamily B member 1 Homo sapiens 43-47 28090646-8 2017 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 156-172 ATP binding cassette subfamily B member 1 Homo sapiens 43-47 28090646-9 2017 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 8-20 ATP binding cassette subfamily B member 1 Homo sapiens 78-83 28090646-9 2017 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 43-59 ATP binding cassette subfamily B member 1 Homo sapiens 78-83 28090646-10 2017 The results demonstrate that the stereoselectivity of P-gp plays a key role in the disposition of fexofenadine enantiomers. fexofenadine 98-110 ATP binding cassette subfamily B member 1 Homo sapiens 54-58 27023466-5 2016 One hundred twenty milligrams fexofenadine, an OATP1A2 substrate, was taken in 1 day before the first folic acid intake, and again on the ninth day of 1,25(OH)2D3 intake. fexofenadine 30-42 solute carrier organic anion transporter family member 1A2 Homo sapiens 47-54 26798172-0 2015 Does Ethnic Variability Exist in the Systemic Exposures of OATP1A2 Substrates-Fexofenadine in Taiwanese? fexofenadine 78-90 solute carrier organic anion transporter family member 1A2 Homo sapiens 59-66 26922536-8 2016 CONCLUSIONS: RSV significantly enhanced the exposure of FEX in rats likely by the inhibition of P-glycoprotein (P-gp) mediated efflux during the intestinal absorption, suggesting that there is a potential pharmacokinetic interaction between RSV and FEX. fexofenadine 56-59 ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus 96-110 26922536-8 2016 CONCLUSIONS: RSV significantly enhanced the exposure of FEX in rats likely by the inhibition of P-glycoprotein (P-gp) mediated efflux during the intestinal absorption, suggesting that there is a potential pharmacokinetic interaction between RSV and FEX. fexofenadine 56-59 ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus 112-116 26922536-8 2016 CONCLUSIONS: RSV significantly enhanced the exposure of FEX in rats likely by the inhibition of P-glycoprotein (P-gp) mediated efflux during the intestinal absorption, suggesting that there is a potential pharmacokinetic interaction between RSV and FEX. fexofenadine 249-252 ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus 112-116 26474764-4 2016 However, the above hypothesis was refuted by another published human pharmacokinetic study of fexofenadine formulated with chitosan formulation - in this work it was unambiguously shown that chitosan helped in enhanced absorption of fexofenadine which is a well-known Pgp substrate. fexofenadine 94-106 phosphoglycolate phosphatase Homo sapiens 268-271 26474764-4 2016 However, the above hypothesis was refuted by another published human pharmacokinetic study of fexofenadine formulated with chitosan formulation - in this work it was unambiguously shown that chitosan helped in enhanced absorption of fexofenadine which is a well-known Pgp substrate. fexofenadine 233-245 phosphoglycolate phosphatase Homo sapiens 268-271 26467209-0 2016 Prediction of area under the curve for a p-glycoprotein, a CYP3A4 and a CYP2C9 substrate using a single time point strategy: assessment using fexofenadine, itraconazole and losartan and metabolites. fexofenadine 142-154 ATP binding cassette subfamily B member 1 Homo sapiens 41-55 25953731-0 2015 Design of Fexofenadine Prodrugs Based on Tissue-Specific Esterase Activity and Their Dissimilar Recognition by P-Glycoprotein. fexofenadine 10-22 ATP binding cassette subfamily B member 1 Homo sapiens 111-125 25908246-8 2015 OATP1A2-mediated uptake of zolmitriptan, rosuvastatin, and fexofenadine across monolayers increased with increasing OATP1A2 protein expression. fexofenadine 59-71 solute carrier organic anion transporter family member 1A2 Homo sapiens 0-7 26204515-5 2015 Although fexofenadine-treated mice had decreased antigen-specific IgE levels as well as lower splenocyte IL-5 and IFNgamma production, they exhibited a greater than fourfold rise in eosinophil numbers at the tissue site where adult L. sigmodontis worms reside. fexofenadine 9-21 interleukin 5 Mus musculus 105-109 25908246-8 2015 OATP1A2-mediated uptake of zolmitriptan, rosuvastatin, and fexofenadine across monolayers increased with increasing OATP1A2 protein expression. fexofenadine 59-71 solute carrier organic anion transporter family member 1A2 Homo sapiens 116-123 25908246-9 2015 OATP1A2 counteracted P-gp efflux for cosubstrates zolmitriptan and fexofenadine. fexofenadine 67-79 solute carrier organic anion transporter family member 1A2 Homo sapiens 0-7 25908246-9 2015 OATP1A2 counteracted P-gp efflux for cosubstrates zolmitriptan and fexofenadine. fexofenadine 67-79 ATP binding cassette subfamily B member 1 Homo sapiens 21-25 25263393-2 2015 Simultaneous administration of single- or multiple-dose rifampicin 600 mg significantly increases the concentrations of fexofenadine enantiomers by inhibiting OATP transporters. fexofenadine 120-132 solute carrier organic anion transporter family member 1A2 Homo sapiens 159-163 25159828-4 2015 Fexofenadine (FEX), a P-gp/OATP substrate, can be considered a suitable probe. fexofenadine 0-12 phosphoglycolate phosphatase Homo sapiens 22-26 25159828-4 2015 Fexofenadine (FEX), a P-gp/OATP substrate, can be considered a suitable probe. fexofenadine 0-12 solute carrier organic anion transporter family member 1A2 Homo sapiens 27-31 25159828-4 2015 Fexofenadine (FEX), a P-gp/OATP substrate, can be considered a suitable probe. fexofenadine 14-17 phosphoglycolate phosphatase Homo sapiens 22-26 25159828-4 2015 Fexofenadine (FEX), a P-gp/OATP substrate, can be considered a suitable probe. fexofenadine 14-17 solute carrier organic anion transporter family member 1A2 Homo sapiens 27-31 25538104-8 2015 Fexofenadine significantly inhibited the upregulated expression of IL-8 in HCT116 and COLO205 cells stimulated with TNF-alpha. fexofenadine 0-12 C-X-C motif chemokine ligand 8 Homo sapiens 67-71 25538104-8 2015 Fexofenadine significantly inhibited the upregulated expression of IL-8 in HCT116 and COLO205 cells stimulated with TNF-alpha. fexofenadine 0-12 tumor necrosis factor Homo sapiens 116-125 25538104-11 2015 In addition, the induction of ER stress markers caspase-12 and p-eukaryotic initiation factor 2 (eIF2)-alpha was significantly suppressed by the pretreatment of fexofenadine. fexofenadine 161-173 caspase 12 Mus musculus 48-58 25538104-11 2015 In addition, the induction of ER stress markers caspase-12 and p-eukaryotic initiation factor 2 (eIF2)-alpha was significantly suppressed by the pretreatment of fexofenadine. fexofenadine 161-173 eukaryotic translation initiation factor 2A Mus musculus 97-108 25538104-14 2015 Finally, fexofenadine significantly reduced the severity of colitis and the immunoreactivity of caspase-12 and p-eIF2-alpha in IL-10(-/-) mice as compared with controls. fexofenadine 9-21 caspase 12 Mus musculus 96-106 25538104-14 2015 Finally, fexofenadine significantly reduced the severity of colitis and the immunoreactivity of caspase-12 and p-eIF2-alpha in IL-10(-/-) mice as compared with controls. fexofenadine 9-21 interleukin 10 Mus musculus 127-132 25712660-3 2015 Hence, the present study was performed to investigate the effect of diosmin on the intestinal absorption and pharmacokinetics of fexofenadine, a P-gp substrate in rats. fexofenadine 129-141 ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus 145-149 25712660-9 2015 CONCLUSIONS: Diosmin significantly enhanced the oral bioavailability of fexofenadine by the inhibition of P-gp mediated drug efflux during the intestinal absorption. fexofenadine 72-84 ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus 106-110 25263393-10 2015 Therefore, the interactive mechanism of multidose rifampicin may occur through a combination of OATP and P-gp transporters, thereby altering the pharmacokinetics of fexofenadine enantiomers. fexofenadine 165-177 solute carrier organic anion transporter family member 1A2 Homo sapiens 96-100 25263393-10 2015 Therefore, the interactive mechanism of multidose rifampicin may occur through a combination of OATP and P-gp transporters, thereby altering the pharmacokinetics of fexofenadine enantiomers. fexofenadine 165-177 ATP binding cassette subfamily B member 1 Homo sapiens 105-109 25501360-13 2014 Fexofenadine, levocetirizine, desloratadine, olopatadine, loratadine, and mequitazine all had a PIR for subjective ratings of 0, but the upper limits of the 95% CIs were all in excess of 1, although fexofenadine (PIR = 2.57) was the lowest. fexofenadine 0-12 ring finger protein 144B Homo sapiens 213-220 25759055-7 2015 The findings suggested that a combination of multiple transporters involving organic anion transporting polypeptide (OATP) 2B1, P-glycoprotein (P-gp), and multidrug resistance-associated protein 2 (MRP2) react to stereoselective fexofenadine exposure. fexofenadine 229-241 solute carrier organic anion transporter family member 2B1 Homo sapiens 77-126 25759055-7 2015 The findings suggested that a combination of multiple transporters involving organic anion transporting polypeptide (OATP) 2B1, P-glycoprotein (P-gp), and multidrug resistance-associated protein 2 (MRP2) react to stereoselective fexofenadine exposure. fexofenadine 229-241 ATP binding cassette subfamily B member 1 Homo sapiens 128-142 25759055-7 2015 The findings suggested that a combination of multiple transporters involving organic anion transporting polypeptide (OATP) 2B1, P-glycoprotein (P-gp), and multidrug resistance-associated protein 2 (MRP2) react to stereoselective fexofenadine exposure. fexofenadine 229-241 ATP binding cassette subfamily B member 1 Homo sapiens 144-148 25759055-7 2015 The findings suggested that a combination of multiple transporters involving organic anion transporting polypeptide (OATP) 2B1, P-glycoprotein (P-gp), and multidrug resistance-associated protein 2 (MRP2) react to stereoselective fexofenadine exposure. fexofenadine 229-241 ATP binding cassette subfamily C member 2 Homo sapiens 155-196 25759055-7 2015 The findings suggested that a combination of multiple transporters involving organic anion transporting polypeptide (OATP) 2B1, P-glycoprotein (P-gp), and multidrug resistance-associated protein 2 (MRP2) react to stereoselective fexofenadine exposure. fexofenadine 229-241 ATP binding cassette subfamily C member 2 Homo sapiens 198-202 25759055-9 2015 Coadministration of P-gp inducer/inhibitors significantly altered the pharmacokinetics of fexofenadine enantiomers. fexofenadine 90-102 ATP binding cassette subfamily B member 1 Homo sapiens 20-24 25759055-11 2015 Moreover, in in vitro studies, the uptake of both fexofenadine enantiomers into OATP2B1 cRNA-injected oocytes was significantly higher than that into water-injected oocytes, and this effect was greater for (R)-fexofenadine. fexofenadine 50-62 solute carrier organic anion transporter family member 2B1 Homo sapiens 80-87 25759055-12 2015 Taken together, these studies indicated that multiple transporters including P-gp, OATPs, and MRP2 play important roles in fexofenadine enantiomer pharmacokinetics. fexofenadine 123-135 ATP binding cassette subfamily B member 1 Homo sapiens 77-81 25759055-12 2015 Taken together, these studies indicated that multiple transporters including P-gp, OATPs, and MRP2 play important roles in fexofenadine enantiomer pharmacokinetics. fexofenadine 123-135 ATP binding cassette subfamily C member 2 Homo sapiens 94-98 25759055-13 2015 Furthermore, OATP2B1 is a key determinant of the stereoselective pharmacokinetics of fexofenadine, and drug transporters may have chiral discrimination ability. fexofenadine 85-97 solute carrier organic anion transporter family member 2B1 Homo sapiens 13-20