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Intestinal MDR transport proteins and P-450 enzymes as barriers to oral drug delivery.
Cytochrome P-450 3A4 (CYP3A4), the major phase I drug metabolizing enzyme in humans, and the multidrug efflux pump, MDR or P-glycoprotein (P-gp), are present at high levels in the villus tipExpand
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Prediction of Fluoroquinolone‐Induced Elevation in Serum Creatinine Levels: A Case of Drug–Endogenous Substance Interaction Involving the Inhibition of Renal Secretion
The aim of this study was to examine the mechanism underlying the elevation in serum creatinine levels caused by a novel des‐fluoro(6)‐quinolone antibacterial agent, DX‐619, in healthy subjects.Expand
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Variation of the ganglioside compositions of human milk, cow's milk and infant formulas.
The ganglioside compositions of human milk, cow's milk and infant formulas were compared. The results showed that there was a drastic change in the ganglioside composition from the colostrum to laterExpand
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Edoxaban Transport via P-Glycoprotein Is a Key Factor for the Drug’s Disposition
Edoxaban (the free base of DU-176b), an oral direct factor Xa inhibitor, is mainly excreted unchanged into urine and feces. Because active membrane transport processes such as active renal secretion,Expand
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Prediction of the human pharmacokinetics of troglitazone, a new and extensively metabolized antidiabetic agent, after oral administration, with an animal scale-up approach.
We have attempted to predict the human pharmacokinetics of troglitazone after oral administration based on animal data. Troglitazone is a new antidiabetic agent that exhibits a high-metabolicExpand
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A study to survey susceptible genetic factors responsible for troglitazone‐associated hepatotoxicity in Japanese patients with type 2 diabetes mellitus
Troglitazone is a 2,4‐thiazolidinedione antidiabetic agent with insulin‐sensitizing activities. This agent had been used efficiently in a large number of patients but was withdrawn from the market inExpand
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Human Pharmacokinetic Prediction of UDP-Glucuronosyltransferase Substrates with an Animal Scale-Up Approach
The aim of the current study was to evaluate the accuracy of allometric scaling methods for drugs metabolized by UDP-glucuronosyltransferases (UGTs), such as ketoprofen, imipramine, lorazepam,Expand
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Human Carboxymethylenebutenolidase as a Bioactivating Hydrolase of Olmesartan Medoxomil in Liver and Intestine
Olmesartan medoxomil (OM) is a prodrug type angiotensin II type 1 receptor antagonist widely prescribed as an antihypertensive agent. Herein, we describe the identification and characterization ofExpand
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Chronological changes in the ganglioside composition of human milk during lactation.
The normal chronological changes in the ganglioside composition of human milk during lactation were examined by means of a high-performance thin-layer chromatography (HPTLC) micro-method with 1 ml ofExpand
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Discovery of CS-0777: A Potent, Selective, and Orally Active S1P1 Agonist.
CS-0777 (3) is phosphorylated in vivo, and the phosphate of CS-0777 (CS-0777-P) (4) acts as a selective S1P receptor-1 (S1P1) modulator. We report herein the synthesis of CS-0777 and CS-0777-P,Expand
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