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Kinetic Considerations for the Quantitative Assessment of Efflux Activity and Inhibition: Implications for Understanding and Predicting the Effects of Efflux Inhibition

Data up to Jan 2025

Published2006
Citations101
References32

Total Citations Per Year

Abstract

References (32)

Overcoming Multidrug Resistance in Cancer: An Update on the Clinical Strategy of Inhibiting P-Glycoprotein

2003 • 899 citations

Passive Permeability and P-Glycoprotein-Mediated Efflux Differentiate Central Nervous System (CNS) and Non-CNS Marketed Drugs

2002 • 590 citations

Transporters and drug therapy: Implications for drug disposition and disease

2005 • 497 citations

Increased Oral Bioavailability of Topotecan in Combination With the Breast Cancer Resistance Protein and P-Glycoprotein Inhibitor GF120918

2002 • 452 citations

Increased drug delivery to the brain by P-glycoprotein inhibition

2000 • 422 citations

Drug–drug interaction mediated by inhibition and induction of P-glycoprotein

2003 • 296 citations

In vitro substrate identification studies for p-glycoprotein-mediated transport: species difference and predictability of in vivo results.

2001 • 226 citations

Pharmacokinetic and Pharmacodynamic Implications of P‐glycoprotein Modulation

2001 • 219 citations

Variable modulation of opioid brain uptake by P-glycoprotein in mice

2003 • 211 citations

Interaction of Morphine, Fentanyl, Sufentanil, Alfentanil, and Loperamide with the Efflux Drug Transporter P-glycoprotein

2002 • 209 citations

Kinetics of drug-drug interactions

1973 • 202 citations

Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein.

2001 • 195 citations

Efflux transport systems for drugs at the blood–brain barrier and blood–cerebrospinal fluid barrier (Part 1)

2001 • 173 citations

Interaction of Cytochrome P450 3A Inhibitors with P-Glycoprotein

2002 • 137 citations

Transport Characteristics of Fexofenadine in the Caco-2 Cell Model

2004 • 129 citations

Rhodamine 123 requires carrier-mediated influx for its activity as a P-glycoprotein substrate in Caco-2 cells.

2003 • 128 citations

FUNCTIONAL ASSESSMENT OF MULTIPLE P-GLYCOPROTEIN (P-GP) PROBE SUBSTRATES: INFLUENCE OF CELL LINE AND MODULATOR CONCENTRATION ON P-GP ACTIVITY

2005 • 123 citations

The influence of the P-glycoprotein inhibitor zosuquidar trihydrochloride (LY335979) on the brain penetration of paclitaxel in mice

2003 • 91 citations

Utility of Mdr1-Gene Deficient Mice in Assessing the Impact of P-glycoprotein on Pharmacokinetics and Pharmacodynamics in Drug Discovery and Development

2003 • 81 citations

Efflux transport systems for drugs at the blood–brain barrier and blood–cerebrospinal fluid barrier (Part 2)

2001 • 74 citations

Modulation of P-glycoprotein Transport Activity in the Mouse Blood-Brain Barrier by Rifampin

2003 • 70 citations

Effect of mdr1a P-glycoprotein gene disruption, gender, and substrate concentration on brain uptake of selected compounds.

2001 • 68 citations

The Elementary Mass Action Rate Constants of P-gp Transport for a Confluent Monolayer of MDCKII-hMDR1 Cells

2004 • 64 citations

Compound profiling for P-glycoprotein at the blood-brain barrier using a microplate screening system.

2003 • 52 citations

Evaluation of the Permeation Characteristics of a Model Opioid Peptide, H-Tyr-d-Ala-Gly-Phe-d-Leu-OH (DADLE), and Its Cyclic Prodrugs across the Blood-Brain Barrier Using an In Situ Perfused Rat Brain Model

2002 • 50 citations

The Steady-State Michaelis–Menten Analysis of P-Glycoprotein Mediated Transport Through a Confluent Cell Monolayer Cannot Predict the Correct Michaelis Constant Km

2005 • 50 citations

Bias in Estimation of Transporter Kinetic Parameters from Overexpression Systems: Interplay of Transporter Expression Level and Substrate Affinity

2006 • 38 citations

Impact of P-Glycoprotein-Mediated Intestinal Efflux Kinetics on Oral Bioavailability of P-Glycoprotein Substrates

2004 • 31 citations

Implications of T-Cell P-Glycoprotein Activity During HIV-1 Infection and Its Therapy

2003 • 22 citations

Use of Loperamide as a Phenotypic Probe of mdr1a Status in CF-1 Mice

2004 • 20 citations

Many P-glycoprotein substrates do not inhibit the transport process across cell membranes

2003 • 19 citations

Tariquidar (TAR, XR-9576) selectively inhibits P-glycoprotein (P-gp) in t-lymphocytes compared to that in the blood-brain barrier (BBB)

2005 • 1 citations

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