Prediction of nonlinear intestinal absorption of CYP3A4 and P-glycoprotein substrates from their in vitro Km values (Q95383469)

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24 May 2020

title

Prediction of nonlinear intestinal absorption of CYP3A4 and P-glycoprotein substrates from their in vitro Km values (English)

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24 May 2020

author name string

Tatsuhiko Tachibana

series ordinal

1

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24 May 2020

Motohiro Kato

series ordinal

2

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24 May 2020

Yuichi Sugiyama

series ordinal

3

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24 May 2020

publication date

13 September 2011

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24 May 2020

published in

Pharmaceutical Research

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24 May 2020

volume

29

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issue

3

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24 May 2020

page(s)

651-668

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Microdose pharmacokinetics of IDX899 and IDX989, candidate HIV-1 non-nucleoside reverse transcriptase inhibitors, following oral and intravenous administration in healthy male subjects

24 May 2020

cites work

1 reference

12 December 2020

The intestinal first-pass metabolism of substrates of CYP3A4 and P-glycoprotein-quantitative analysis based on information from the literature

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12 December 2020

Simulations of the nonlinear dose dependence for substrates of influx and efflux transporters in the human intestine

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The human intestinal cytochrome P450 "pie".

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Prediction of human blood-to-plasma drug concentration ratio

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Model analysis of the concentration-dependent permeability of P-gp substrates

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Itraconazole increases but grapefruit juice greatly decreases plasma concentrations of celiprolol

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12 December 2020

CYP3A4-transfected Caco-2 cells as a tool for understanding biochemical absorption barriers: studies with sirolimus and midazolam

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12 December 2020

The novel benzopyran class of selective cyclooxygenase-2 inhibitors. Part III: the three microdose candidates

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12 December 2020

Functional role of P-glycoprotein in limiting intestinal absorption of drugs: contribution of passive permeability to P-glycoprotein mediated efflux transport

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12 December 2020

Prediction of interindividual variability in pharmacokinetics for CYP3A4 substrates in humans

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12 December 2020

Approaches using molecular imaging technology -- use of PET in clinical microdose studies

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12 December 2020

Effect of P-glycoprotein expression levels on the concentration-dependent permeability of drugs to the cell membrane

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12 December 2020

In silico modeling of non-linear drug absorption for the P-gp substrate talinolol and of consequences for the resulting pharmacodynamic effect.

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12 December 2020

Predicting drug-drug interactions involving the inhibition of intestinal CYP3A4 and P-glycoprotein

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Early microdose drug studies in human volunteers can minimise animal testing: Proceedings of a workshop organised by Volunteers in Research and Testing

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Method for predicting the risk of drug-drug interactions involving inhibition of intestinal CYP3A4 and P-glycoprotein.

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12 December 2020

Effects of experimental setup on the apparent concentration dependency of active efflux transport in in vitro cell permeation experiments.

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12 December 2020

Prediction of human intestinal first-pass metabolism of 25 CYP3A substrates from in vitro clearance and permeability data.

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12 December 2020

Overlapping substrate specificities and tissue distribution of cytochrome P450 3A and P-glycoprotein: implications for drug delivery and activity in cancer chemotherapy.

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12 December 2020

Prediction of human clearance of twenty-nine drugs from hepatic microsomal intrinsic clearance data: An examination of in vitro half-life approach and nonspecific binding to microsomes.

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A pharmacokinetic evaluation of five H(1) antagonists after an oral and intravenous microdose to human subjects

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12 December 2020

Celiprolol. An updated review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in cardiovascular disease

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12 December 2020

Species difference in the effect of grapefruit juice on intestinal absorption of talinolol between human and rat.

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Nontraditional approaches to first-in-human studies to increase efficiency of drug development: will microdose studies make a significant impact?

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Early human studies of investigational agents: dose or microdose?

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Microdose study of a P-glycoprotein substrate, fexofenadine, using a non-radioisotope-labelled drug and LC/MS/MS.

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12 December 2020

Database analyses for the prediction of in vivo drug-drug interactions from in vitro data

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12 December 2020

Pharmacokinetics of fexofenadine: evaluation of a microdose and assessment of absolute oral bioavailability

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12 December 2020

Quantitative prediction of intestinal metabolism in humans from a simplified intestinal availability model and empirical scaling factor

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12 December 2020

Decrease in intracellular concentration causes the shift in Km value of efflux pump substrates.

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12 December 2020

Grapefruit juice substantially increases plasma concentrations of buspirone

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12 December 2020

Prediction of intestinal first-pass drug metabolism

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12 December 2020

'In silico' simulations to assess the 'in vivo' consequences of 'in vitro' metabolic drug-drug interactions

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12 December 2020

Single-dose pharmacokinetics of indinavir and the effect of food.

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12 December 2020

Involvement of influx and efflux transport systems in gastrointestinal absorption of celiprolol

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12 December 2020

Transporter database, TP-Search: a web-accessible comprehensive database for research in pharmacokinetics of drugs

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12 December 2020

Unmasking the dynamic interplay between efflux transporters and metabolic enzymes.

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12 December 2020

Microdose clinical trial: quantitative determination of fexofenadine in human plasma using liquid chromatography/electrospray ionization tandem mass spectrometry

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12 December 2020

A functional assay for quantitation of the apparent affinities of ligands of P-glycoprotein in Caco-2 cells

1 reference

12 December 2020

Prediction of in vivo nonlinear first-pass hepatic metabolism of YM796 from in vitro metabolic data

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12 December 2020

10.1007/S11095-011-0579-2

Identifiers

DOI

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24 May 2020

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