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Titolo:
Problems associated with in vitro assessment of drug inhibition of CYP3A4 and other P-450 enzymes and its impact on drug discovery
Autore:
Wienkers, LC;
Indirizzi:
Pharmacia Corp, Kalamazoo, MI 49007 USA Pharmacia Corp Kalamazoo MI USA 49007 macia Corp, Kalamazoo, MI 49007 USA
Titolo Testata:
JOURNAL OF PHARMACOLOGICAL AND TOXICOLOGICAL METHODS
fascicolo: 1, volume: 45, anno: 2001,
pagine: 79 - 84
SICI:
1056-8719(200101/02)45:1<79:PAWIVA>2.0.ZU;2-T
Fonte:
ISI
Lingua:
ENG
Soggetto:
HUMAN LIVER-MICROSOMES; IN-VITRO; CYTOCHROME-P450 3A4; WARFARIN-FLUCONAZOLE; NONSPECIFIC-BINDING; ACTIVE-SITE; METABOLISM; VIVO; COOPERATIVITY; ACTIVATION;
Keywords:
drug inhibition; high throughput; drug discovery; cytochrome P-450;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
42
Recensione:
Indirizzi per estratti:
Indirizzo: Wienkers, LC Pharmacia Corp, 301 Henrietta St,7265-300-319, Kalamazoo, MI 49007 USA Pharmacia Corp 301 Henrietta St,7265-300-319 Kalamazoo MI USA 49007
Citazione:
L.C. Wienkers, "Problems associated with in vitro assessment of drug inhibition of CYP3A4 and other P-450 enzymes and its impact on drug discovery", J PHARM TOX, 45(1), 2001, pp. 79-84

Abstract

The cytochromes P-450 recognize and metabolize a broad range of structurally diverse therapeutic agents. As a consequence, many clinically relevant drug-drug interactions (DDI) are associated with inhibition and/or inductionof a specific P-450 enzymes (in particular human cytochrome P-450 3A4, CYP3A4). In addition to inhibition and induction, CYP-mediated drug metabolismmay be enhanced upon coincubation with certain compounds. Moreover, some of these enzyme-based interactions appear to be substrate specific. In this presentation, several issues associated with the generation of accurate DDIinformation will be discussed. (C) 2001 Elsevier Science Inc. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 28/01/20 alle ore 15:21:17