Species differences in metabolism of EPZ015666, an oxetane-containing protein arginine methyltransferase-5 (PRMT5) inhibitor

Xenobiotica

Volumn 46, Issue 3, 2016, Pages 268-277

  Rioux, Nathalie ^a   Duncan, Kenneth W ^a   Lantz, Ronald J ^b   Miao, Xiusheng ^b   Chan Penebre, Elayne ^a   Moyer, Mikel P ^a   Munchhof, Michael J ^a   Copeland, Robert A ^a   Chesworth, Richard ^a   Waters, Nigel J ^a  

^a EPIZYME INC   (United States)

^b IQVIA   (United States)

Author keywords

CYP2D15; CYP2D6; hepatocytes; interspecies scaling; metabolite identification

Indexed keywords

EPZ 015666; KETOCONAZOLE; METHYLTRANSFERASE INHIBITOR; PROTEIN ARGININE METHYLTRANSFERASE; PROTEIN ARGININE METHYLTRANSFERASE 5; PROTEIN ARGININE METHYLTRANSFERASE 5 INHIBITOR; QUINIDINE; UNCLASSIFIED DRUG; CYTOCHROME P450 2D6 INHIBITOR; CYTOCHROME P450 3A INHIBITOR; ENZYME INHIBITOR; ETHER DERIVATIVE; GSK3235025; ISOQUINOLINE DERIVATIVE; OXETANE; PYRIMIDINE DERIVATIVE;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTIPROLIFERATIVE ACTIVITY; AREA UNDER THE CURVE; ARTICLE; CONTROLLED STUDY; DEALKYLATION; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG DISPOSITION; DRUG HALF LIFE; DRUG METABOLISM; DRUG STABILITY; FEMALE; HUMAN; LIQUID CHROMATOGRAPHY; LIVER METABOLISM; LIVER MICROSOME; MALE; MANTLE CELL LYMPHOMA; MASS SPECTROMETRY; MAXIMUM PLASMA CONCENTRATION; MEAN RESIDENCE TIME; METABOLIC CLEARANCE; MOUSE; NONHUMAN; RAT; SINGLE DRUG DOSE; SPECIES DIFFERENCE; TIME TO MAXIMUM PLASMA CONCENTRATION; VOLUME OF DISTRIBUTION AT STEADY-STATE; ANIMAL; ANTAGONISTS AND INHIBITORS; DOG; LIVER CELL; METABOLISM; SPRAGUE DAWLEY RAT;

ANIMALS; CYTOCHROME P-450 CYP2D6 INHIBITORS; CYTOCHROME P-450 CYP3A INHIBITORS; DOGS; ENZYME INHIBITORS; ETHERS, CYCLIC; HEPATOCYTES; HUMANS; ISOQUINOLINES; KETOCONAZOLE; MALE; MICE; MICROSOMES, LIVER; PROTEIN-ARGININE N-METHYLTRANSFERASES; PYRIMIDINES; QUINIDINE; RATS; RATS, SPRAGUE-DAWLEY; SPECIES SPECIFICITY;

EID: 84956584406     PISSN: 00498254     EISSN: 13665928     Source Type: Journal    
DOI: 10.3109/00498254.2015.1072253     Document Type: Article

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