Breast Cancer Resistance Protein: Mediating the Trans-placental Transfer of Glyburide across the Human Placenta

Gedeon, C.; Anger, G; Piquette-Miller, Micheline; Koren, Gideon

doi:10.1016/j.placenta.2007.08.004

Cited by 75 publications

(52 citation statements)

References 22 publications

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“…In vitro transport studies demonstrate that inhibitors of MRP1-3 and Pgp are ineffective in preventing glyburide transport across the placental membrane (Gedeon et al, 2008a,b). Instead, inhibition of BCRP disrupts glyburide efflux (Gedeon et al, 2008b). In support of this, glyburide concentrations are higher in Bcrp-null fetuses compared with wild type (Zhou et al, 2008b).…”

mentioning

confidence: 82%

Xenobiotic, Bile Acid, and Cholesterol Transporters: Function and Regulation

2010

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confidence: 82%

Xenobiotic, Bile Acid, and Cholesterol Transporters: Function and Regulation

2010

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“…administration of the antibiotic nitrofurantoin to pregnant mice leads to a 5-fold higher fetal concentration in ABCG2 2/2 mice versus wild-type mice . In humans, an ex vivo study employing human placental vesicles demonstrated that fetal-tomaternal concentration ratios of the gestational diabetes drug glyburide were increased 2-fold by coadministration of the ABCG2 inhibitor novobiocin (Gedeon et al, 2008).…”

Section: Localization and Physiologic Functionmentioning

confidence: 99%

Molecular Pharmacology of ABCG2 and Its Role in Chemoresistance

2013

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“…Among the ABC transporters, GLB has been identified as a substrate of the breast cancer resistance protein (BCRP, ABCG2) (3-7) and some multidrug resistance proteins (MRP1 and MRP3; ABCC1,3) (3,7). However, GLB transport by P-glycoprotein (P-gp, ABCB1, MDR1) remains controversial (3,(7)(8)(9). More recently, GLB has also been shown to be a substrate of the organic anion-transporting polypeptide (OATP, SLCO) family.…”

Section: Introductionmentioning

confidence: 99%

Effects of Selected OATP and/or ABC Transporter Inhibitors on the Brain and Whole-Body Distribution of Glyburide

Tournier

Saba

Cisternino

et al. 2013

AAPS J

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Abstract. Glyburide (glibenclamide, GLB) is a widely prescribed antidiabetic with potential beneficial effects in central nervous system injury and diseases. In vitro studies show that GLB is a substrate of organic anion transporting polypeptide (OATP) and ATP-binding cassette (ABC) transporter families, which may influence GLB distribution and pharmacokinetics in vivo. In the present study, we used [11 C] GLB positron emission tomography (PET) imaging to non-invasively observe the distribution of GLB at a non-saturating tracer dose in baboons. The role of OATP and P-glycoprotein (P-gp) in [11 C]GLB whole-body distribution, plasma kinetics, and metabolism was assessed using the OATP inhibitor rifampicin and the dual OATP/P-gp inhibitor cyclosporine. Finally, we used in situ brain perfusion in mice to pinpoint the effect of ABC transporters on GLB transport at the blood-brain barrier (BBB). PET revealed the critical role of OATP on liver [ 11 C]GLB uptake and its subsequent impact on [11 C]GLB metabolism and plasma clearance. OATP-mediated uptake also occurred in the myocardium and kidney parenchyma but not the brain. The inhibition of P-gp in addition to OATP did not further influence [11 C] GLB tissue and plasma kinetics. At the BBB, the inhibition of both P-gp and breast cancer resistance protein (BCRP) was necessary to demonstrate the role of ABC transporters in limiting GLB brain uptake. This study demonstrates that GLB distribution, metabolism, and elimination are greatly dependent on OATP activity, the first step in GLB hepatic clearance. Conversely, P-gp, BCRP, and probably multidrug resistance protein 4 work in synergy to limit GLB brain uptake.

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Breast Cancer Resistance Protein: Mediating the Trans-placental Transfer of Glyburide across the Human Placenta

Cited by 75 publications

References 22 publications

Xenobiotic, Bile Acid, and Cholesterol Transporters: Function and Regulation

Xenobiotic, Bile Acid, and Cholesterol Transporters: Function and Regulation

Molecular Pharmacology of ABCG2 and Its Role in Chemoresistance

Effects of Selected OATP and/or ABC Transporter Inhibitors on the Brain and Whole-Body Distribution of Glyburide

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