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Titolo:
Does P-glycoprotein play a role in anticancer drug pharmacokinetics?
Autore:
Sparreboom, A; Nooter, K;
Indirizzi:
Rotterdam Canc Inst, Dept Med Oncol, Rotterdam, Netherlands Rotterdam CancInst Rotterdam Netherlands Oncol, Rotterdam, Netherlands Univ Rotterdam Hosp, Rotterdam, Netherlands Univ Rotterdam Hosp Rotterdam Netherlands Hosp, Rotterdam, Netherlands
Titolo Testata:
DRUG RESISTANCE UPDATES
fascicolo: 6, volume: 3, anno: 2000,
pagine: 357 - 363
SICI:
1368-7646(2000)3:6<357:DPPARI>2.0.ZU;2-K
Fonte:
ISI
Lingua:
ENG
Soggetto:
PHASE-I TRIAL; MULTIDRUG-RESISTANCE MODULATOR; PROTEIN GENE MRP1; CREMOPHOR EL; ALTERED PHARMACOKINETICS; CYTOCHROME-P450 3A4; CYCLOSPORINE-A; LUNG-CANCER; SDZ PSC-833; CELL-LINES;
Tipo documento:
Review
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
59
Recensione:
Indirizzi per estratti:
Indirizzo: Nooter, K Univ Rotterdam Hosp, Rotterdam Canc Inst, Groene Hilledijk 301, NL-3075 EARotterdam, Netherlands Univ Rotterdam Hosp Groene Hilledijk 301 Rotterdam Netherlands NL-3075 EA
Citazione:
A. Sparreboom e K. Nooter, "Does P-glycoprotein play a role in anticancer drug pharmacokinetics?", DRUG RESIST, 3(6), 2000, pp. 357-363

Abstract

The multidrug-resistance P-glycoprotein is a drug efflux transport proteinabundantly present in various types of human cancer. The protein is encoded by the MDRI gene and its function is sensitive to modulation by competitive inhibition. Clinical studies have indicated that inhibitors of P-glycoprotein function dramatically decrease the systemic clearance of anticancer agents, necessitating dose reduction. This dose reduction not only complicated the interpretation of toxicity and response data, but also presented a serious obstacle in the development and rational use of P-glycoprotein inhibitors. It is now evident that the pharmacokinetic interference between anticancer drugs and P-glycoprotein inhibitors is due primarily to competition for drug metabolizing enzymes. A wealth of recent experimental data shows that many of the previously rested P-glycoprotein inhibitors, including verapamil, cyclosporin A, and valspodar (SDZ PSC 833), are substrates and/or potent inhibitors of cytochrome P450 3A4 (CYP3A4). Future development and clinical use of potent P-glycoprotein modulators lacking high affinity for CYP3A4 should decrease the impact of these important drug interactions and will eventually result in improved therapeutic specificity and efficacy. (C) 2000 Harcourt Publishers Ltd.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 22/01/20 alle ore 06:24:14