An inhibitory metabolite leads to dose- And time-dependent pharmacokinetics of (R)-N-{1-[3-(4-ethoxy-phenyl)-4-oxo-3,4-dihydro-pyrido[2,3-d]pyrimidin-2-yl] -ethyl}-N-pyridin-3-yl-methyl-2-(4-trifluoromethoxy-phenyl)-acetamide (AMG 487) in human subjects after multiple dosing

Drug Metabolism and Disposition

Volumn 37, Issue 3, 2009, Pages 502-513

  Tonn, George R ^a,b   Wong, Simon G ^a   Wong, Sylvia C ^a   Johnson, Michael G ^a   Ma, Ji ^a   Cho, Robert ^a   Floren, Leslie C ^a   Kersey, Kathryn ^a   Berry, Karen ^a   Marcus, Andrew P ^a   Wang, Xuemei ^a   Van Lengerich, Bettina ^a   Medina, Julio C ^a   Pearson, Paul G ^a   Wong, Bradley K ^a  

^a AMGEN INC   (United States)

^b ELAN PHARMACEUTICALS   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

AMG 487; CHEMOKINE RECEPTOR ANTAGONIST; CHEMOKINE RECEPTOR CXCR3; CYTOCHROME P450 1A2; CYTOCHROME P450 2C9; CYTOCHROME P450 2D6; CYTOCHROME P450 3A; CYTOCHROME P450 3A4; CYTOCHROME P450 3A5; N [1 [3 (4 ETHOXYPHENYL ) 4 OXO 3,4 DIHYDROPYRIDO[2,3 D]PYRIMIDIN 2 YL]ETHYL] N PYRIDIN 3 YLMETHYL 2 (4 TRIFLUOROMETHOXYPHENYL)ACETAMIDE; UNCLASSIFIED DRUG;

ADULT; AREA UNDER THE CURVE; ARTICLE; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; CROSSOVER PROCEDURE; DOSE TIME EFFECT RELATION; DOUBLE BLIND PROCEDURE; DRUG ACCUMULATION; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG DOSE COMPARISON; DRUG HALF LIFE; DRUG TRANSFORMATION; FIRST PASS EFFECT; HUMAN; HUMAN CELL; HUMAN EXPERIMENT; LIVER METABOLISM; LIVER MICROSOME METABOLISM; MALE; MAXIMUM PLASMA CONCENTRATION; NORMAL HUMAN; PRIORITY JOURNAL; RANDOMIZED CONTROLLED TRIAL;

ACETAMIDES; ADULT; AREA UNDER CURVE; CHROMATOGRAPHY, LIQUID; COHORT STUDIES; CYTOCHROME P-450 ENZYME SYSTEM; DRUG ADMINISTRATION SCHEDULE; HUMANS; MALE; PYRIMIDINONES; RECEPTORS, CXCR3; TANDEM MASS SPECTROMETRY;

EID: 61449202932     PISSN: 00909556     EISSN: 1521009X     Source Type: Journal    
DOI: 10.1124/dmd.108.021931     Document Type: Article

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