The steady-state Michaelis-Menten analysis of P-glycoprotein mediated transport through a confluent cell monolayer cannot predict the correct Michaelis constant Km

Pharmaceutical Research

Volumn 22, Issue 10, 2005, Pages 1667-1677

  Bentz, Joe ^a   Thuy, Thanh Tran ^a,b   Polli, Joseph W ^c   Ayrton, Andrew ^d   Ellens, Harma ^b  

^a DREXEL UNIVERSITY   (United States)

^b Drug Metabolism and Pharmacokinetics   (United States)

^c Glaxo Wellcome   (United States)

^d Preclinical Drug Metabolism and Pharmacokinetics   (United Kingdom)

Author keywords

Elementary rate constants; Michaelis Menten; P gp; Pharmacokinetic extrapolation; Transcellular transport

Indexed keywords

AMPRENAVIR; ELACRIDAR; GLYCOPROTEIN P; LOPERAMIDE; QUINIDINE;

ACCURACY; ANIMAL CELL; ARTICLE; CALCULATION; COMPUTER SIMULATION; CONCENTRATION (PARAMETERS); CONTROLLED STUDY; CORRELATION ANALYSIS; DRUG PENETRATION; DRUG TRANSPORT; IN VITRO STUDY; IN VIVO STUDY; KINETICS; MASS ACTION; MEASUREMENT; MEMBRANE TRANSPORT; MICHAELIS CONSTANT; MICHAELIS MENTEN KINETICS; MICROSOME; MOLECULE; MONOLAYER CULTURE; NONHUMAN; PARAMETER; PREDICTION; PRIORITY JOURNAL; PROTEOLIPOSOME; RELIABILITY; STEADY STATE; TRANSPORT KINETICS;

ACRIDINES; ANIMALS; BIOLOGICAL TRANSPORT, ACTIVE; CARBAMATES; CELL LINE; CELL MEMBRANE PERMEABILITY; COMPUTER SIMULATION; DOGS; HUMANS; LOPERAMIDE; MODELS, BIOLOGICAL; P-GLYCOPROTEIN; PHARMACOKINETICS; QUINIDINE; REPRODUCIBILITY OF RESULTS; SULFONAMIDES; TETRAHYDROISOQUINOLINES;

EID: 25144511902     PISSN: 07248741     EISSN: 1573904X     Source Type: Journal    
DOI: 10.1007/s11095-005-6627-z     Document Type: Article

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