The use of in vitro metabolic stability for rapid selection of compounds in early discovery based on their expected hepatic extraction ratios

Pharmaceutical Research

Volumn 19, Issue 11, 2002, Pages 1606-1610

  Lau, Y Y ^a   Krishna, G ^a   Yumibe, N P ^a,b   Grotz, D E ^a   Sapidou, E ^a   Norton, L ^a   Chu, I ^a   Chen, C ^a   Soares, A D ^a   Lin, C C ^a,c  

^a MERCK RESEARCH LABORATORIES   (United States)

^b ELI LILLY AND COMPANY   (United States)

^c Valeant Pharmaceuticals International   (United States)

Author keywords

Caco 2; Hepatic extraction ratio; In vitro in vivo correlation; Liver microsomes; Monkey; Rapid screening

Indexed keywords

4 [(4 BROMOPHENYL)(ETHOXYIMINO)METHYL] 1' [(2,4 DIMETHYL 3 PYRIDINYL)CARBONYL] 4' METHYL 1,4' BIPIPERIDINE; DRUG; ECOPIPAM; LONAFARNIB; N (3,5 DICHLORO 1 OXIDO 4 PYRIDINYL) 8 METHOXY 2 TRIFLUOROMETHYL 5 QUINOLINECARBOXAMIDE; SCH 201690; SCH 205831; SCH 206272; SCH 209119; SCH 210010; SCH 211334; SCH 211478; SCH 211784; SCH 211803; SCH 213949; SCH 214468; SCH 214472; SCH 217443; SCH 218829; SCH 220236; SCH 221000; SCH 224380; SCH 226374; SCH 350634; SCH 351867; SCH 352437; SCH 44643; SCH 68901; SCH 74909; SCH 79687; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; CELL STRAIN CACO 2; CORRELATION ANALYSIS; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG METABOLISM; DRUG SCREENING; DRUG STABILITY; FIRST PASS EFFECT; HEPATIC EXTRACTION RATIO; HUMAN; HUMAN CELL; IN VITRO STUDY; IN VIVO STUDY; LIVER METABOLISM; LIVER MICROSOME; MONKEY; NONHUMAN; PREDICTION; PRIORITY JOURNAL;

ANIMALS; CACO-2 CELLS; ENZYME STABILITY; FORECASTING; HUMANS; MACACA FASCICULARIS; METABOLIC CLEARANCE RATE; MICROSOMES, LIVER; PHARMACEUTICAL PREPARATIONS; TECHNOLOGY, PHARMACEUTICAL;

EID: 0036846773     PISSN: 07248741     EISSN: None     Source Type: Journal    
DOI: 10.1023/A:1020765025857     Document Type: Article

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