Pharmacokinetics of the active antifungal enantiomer, SCH 42427 (RR), and evaluation of its chiral inversion in animals following its oral administration and the oral administration of its racemate genaconazole (RR/SS)

Chirality

Volumn 14, Issue 5, 2002, Pages 436-441

  Kim, Hong ^a   Radwanski, Elaine ^a   Lovey, Raymond ^a   Lin, Chin Chung ^a   Nomeir, Amin A ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

Chiral HPLC analysis; Chiral inversion; Genaconazole; Pharmacokinetics; SCH 39304, SCH 42427; SCH 42426; Triazole antifungal agent

Indexed keywords

GENACONAZOLE; SCH 42426; SCH 42427; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ANTIFUNGAL ACTIVITY; AREA UNDER THE CURVE; ARTICLE; CHIRAL CHROMATOGRAPHY; CHIRALITY; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG HALF LIFE; DRUG STRUCTURE; ENANTIOMER; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; LIGHT ABSORPTION; MALE; MONKEY; NONHUMAN; PRIORITY JOURNAL; RACEMIC MIXTURE; RAT; STRUCTURE ACTIVITY RELATION; STRUCTURE ANALYSIS;

ADMINISTRATION, ORAL; ANIMALS; ANTIFUNGAL AGENTS; BIOLOGICAL AVAILABILITY; CHROMATOGRAPHY, HIGH PRESSURE LIQUID; MACACA FASCICULARIS; MALE; RATS; STEREOISOMERISM; TRIAZOLES;

EID: 0036249537     PISSN: 08990042     EISSN: None     Source Type: Journal    
DOI: 10.1002/chir.10114     Document Type: Article

References (17)

1. Problems in management of opportunistic fungal infections
2. Efficacy of SCH 39304 and fluconazole in a murine model of disseminated coccidiodomycosis
3. Treatment of murine coccidioidal meningitis with SCH 39304
4. Effects of incubation temperature, inoculum size and medium on agreement of macro- and microdilution broth susceptibility test results for yeasts
5. In vitro susceptibilities of yeasts to a new antifungal triazole, SCH 39304
6. Treatment of expe-rimental cryptococcal meningitis and disseminated candidiasis with SCH 39304
7. SCH 39304 in prevention and treatment of disseminated candidiasis in persistently granulocytopenic rabbits
8. Pharmacokinetics and tissue penetration of SCH 39304 in granulocytopenic and nongranulocytopenic rabbits
9. In vitro and in vivo activities of SCH 42427, the active enantiomer of the antifungal agent SCH 39304
10. Current regulatory (draft) guidance on chiral medicinal products: Canada, EEC, Japan, United States
11. Enantioselective aspects of drug action and disposition: Therapeutic pitfalls
12. Separation of drug enantiomers by HPLC using chiral stationary phases: Selective review
13. A chiral liquid chromatographic method for the determination of the enantiomers of the racemic triazole antifungal drug (SCH 39304) in human plasma
14. Comparative pharmacokinetics of SCH 39304 and fluconazole in mice, rabbits and c. monkeys
15. Treatment of murine pulmonary blastomycosis with SCH 39304, a new triazole antifungal agent
16. Pharmacokinetics and metabolism of genaconazole, a potent antifungal drug, in man