The change of pharmacokinetics of fexofenadine enantiomers through the single and simultaneous grapefruit juice ingestion

Akamine, Yumiko; Miura, Masatomo; Komori, Hisakazu; Tamai, Ikumi; Ieiri, Ichiro; Yasui‐Furukori, Norio; Uno, Tsukasa

doi:10.1016/j.dmpk.2015.06.005

Cited by 32 publications

(17 citation statements)

References 39 publications

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“…5,6 Grapefruit juice (GFJ) is a well-known strong inhibitor of OATP2B1. 5,7,8 GFJ reduced the marked OATP2B1-mediated uptake of estrone-3-sulfate induced by a simultaneous exposure; however, this is not a long-lasting mechanism. 9 Thus, OATP2B1 is functionally impaired through a competitive inhibition mechanism, leading to the lower bioavailabilities of several medications such as celiprolol, fexofenadine, and aliskiren.…”

Section: Introductionmentioning

confidence: 82%

“…9 Thus, OATP2B1 is functionally impaired through a competitive inhibition mechanism, leading to the lower bioavailabilities of several medications such as celiprolol, fexofenadine, and aliskiren. 5,7,8 Atorvastatin is an inhibitor of 3-hydroxy-3-methyl-glutaryl coenzyme A reductase and is widely used in the treatment of hypercholesterolemia. Atorvastatin has been identified as a good substrate for OATP2B1.…”

Section: Introductionmentioning

confidence: 99%

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Small-Dosing Clinical Study: Pharmacokinetic, Pharmacogenomic (SLCO2B1 and ABCG2), and Interaction (Atorvastatin and Grapefruit Juice) Profiles of 5 Probes for OATP2B1 and BCRP

Kashihara

Ieiri

Yoshikado³

et al. 2017

Journal of Pharmaceutical Sciences

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Section: Introductionmentioning

confidence: 82%

Section: Introductionmentioning

confidence: 99%

Small-Dosing Clinical Study: Pharmacokinetic, Pharmacogenomic (SLCO2B1 and ABCG2), and Interaction (Atorvastatin and Grapefruit Juice) Profiles of 5 Probes for OATP2B1 and BCRP

Kashihara

Ieiri

Yoshikado³

et al. 2017

Journal of Pharmaceutical Sciences

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“…In the case of intestinal uptake transporters (OATP1A2 and OATP2B1), curcumin shows an inhibition potential for OATP2B1 (Kusuhara et al, 2012;Zhou et al, 2017), which is considered to contribute to SASP and RSV uptake in the gut. However, significant reductions in oral AUC all and C max for FEX, TLN, and AL were not observed after curcumin administration (Table 5), although these compounds, as well as P-gp, were also known to be OATP1A2 and/or OATP2B1 substrates (Bailey, 2010;Tapaninen et al, 2011;Rebello et al, 2012;Akamine et al, 2015). These results implied that OATP1A2 and OATP2B1 inhibition after curcumin pretreatment was limited in monkeys or that the saturation of those transporters was observed under these study conditions.…”

Section: Downloaded Frommentioning

confidence: 94%

Curcumin as an In Vivo Selective Intestinal Breast Cancer Resistance Protein Inhibitor in Cynomolgus Monkeys

et al. 2018

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To estimate the clinical impact of pharmacokinetic modulation via breast cancer resistance protein (BCRP), in vivo approaches in nonclinical settings are desired in drug development. Clinical observation has identified curcumin as a promising candidate for in vivo selective BCRP inhibition, in addition to several well known inhibitors, such as lapatinib and pantoprazole. This study aimed to confirm the inhibitory efficacy of curcumin on gastrointestinal BCRP function in cynomolgus monkeys and to perform comparisons with lapatinib and pantoprazole. Oral area under the plasma concentration-time curve (AUC) and bioavailability of well known BCRP (sulfasalazine and rosuvastatin), P-glycoprotein (fexofenadine, aliskiren, and talinolol), and CYP3A (midazolam) substrates were investigated in the presence and absence of inhibitors. Oral exposures of sulfasalazine and rosuvastatin were markedly elevated by curcumin with minimal changes in systemic clearance, whereas pharmacokinetic alterations after fexofenadine, aliskiren, and talinolol oral exposure were limited. Curcumin increased oral midazolam exposure without affecting systemic clearance, presumably owing to partial inhibition of intestinal CYP3A. Lapatinib increased the oral AUC for sulfasalazine to a greater extent than curcumin did, whereas pantoprazole had a smaller effect. However, lapatinib also exerted significant effects on fexofenadine, failed to selectively discriminate between BCRP and P-glycoprotein inhibition, and had an effect on oral midazolam exposure comparable with that of curcumin. Thus, pharmacokinetic evaluation in monkeys demonstrated that pretreatment with curcumin as an in vivo selective BCRP inhibitor was more appropriate than pretreatment with lapatinib and pantoprazole for the assessment of the impact of BCRP on gastrointestinal absorption in nonrodent models.

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“…However, the effect of this SLCO2B1 nonsynonymous variant was not significant in the disposition or response for other substrates, e.g., montelukast . Several clinical studies have shown that apple juice or grapefruit juice can inhibit OATP2B1, and hence reduce absorption (reduce plasma AUC levels by >1.5‐fold) of several drugs that are substrates of OATP2B1, such as fexofenadine, atorvastatin, and celiprolol . More recently, a drug in early development, ronacaleret, unexpectedly reduced plasma levels of rosuvastatin, a substrate of OATP2B1, by 50%.…”

Section: Polymorphisms In Other Drug Transporters With Less Evidencementioning

confidence: 99%

Influence of Transporter Polymorphisms on Drug Disposition and Response: A Perspective From the International Transporter Consortium

Yee

Brackman

Ennis

et al. 2018

Clin Pharma and Therapeutics

108

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Advances in genomic technologies have led to a wealth of information identifying genetic polymorphisms in membrane transporters, specifically how these polymorphisms affect drug disposition and response. This review describes the current perspective of the International Transporter Consortium (ITC) on clinically important polymorphisms in membrane transporters. ITC suggests that, in addition to previously recommended polymorphisms in ABCG2 (BCRP) and SLCO1B1 (OATP1B1), polymorphisms in the emerging transporter, SLC22A1 (OCT1), be considered during drug development. Collectively, polymorphisms in these transporters are important determinants of interindividual differences in the levels, toxicities, and response to many drugs.

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The change of pharmacokinetics of fexofenadine enantiomers through the single and simultaneous grapefruit juice ingestion

Cited by 32 publications

References 39 publications

Small-Dosing Clinical Study: Pharmacokinetic, Pharmacogenomic (SLCO2B1 and ABCG2), and Interaction (Atorvastatin and Grapefruit Juice) Profiles of 5 Probes for OATP2B1 and BCRP

Small-Dosing Clinical Study: Pharmacokinetic, Pharmacogenomic (SLCO2B1 and ABCG2), and Interaction (Atorvastatin and Grapefruit Juice) Profiles of 5 Probes for OATP2B1 and BCRP

Curcumin as an In Vivo Selective Intestinal Breast Cancer Resistance Protein Inhibitor in Cynomolgus Monkeys

Influence of Transporter Polymorphisms on Drug Disposition and Response: A Perspective From the International Transporter Consortium

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