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Titolo:
ARE THE MAJOR EFFECTS OF P-GLYCOPROTEIN MODULATORS DUE TO ALTERED PHARMACOKINETICS OF ANTICANCER DRUGS
Autore:
RELLING MV;
Indirizzi:
ST JUDE CHILDRENS HOSP,DEPT PHARMACEUT,332 N LAUDERDALE ST MEMPHIS TN38105 UNIV TENNESSEE,DEPT CLIN PHARM MEMPHIS TN 00000 UNIV TENNESSEE,DEPT PHARMACEUT SCI MEMPHIS TN 00000
Titolo Testata:
Therapeutic drug monitoring
fascicolo: 4, volume: 18, anno: 1996,
pagine: 350 - 356
SICI:
0163-4356(1996)18:4<350:ATMEOP>2.0.ZU;2-X
Fonte:
ISI
Lingua:
ENG
Soggetto:
HUMAN LIVER-MICROSOMES; PHASE-I TRIAL; MULTIDRUG-RESISTANCE; CYTOCHROME-P450 3A4; CLINICAL-TRIALS; BREAST-CANCER; CYCLOSPORINE; METABOLISM; IDENTIFICATION; CHEMOTHERAPY;
Keywords:
P-GLYCOPROTEIN; ANTICANCER DRUGS; PHARMACOKINETICS;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
38
Recensione:
Indirizzi per estratti:
Citazione:
M.V. Relling, "ARE THE MAJOR EFFECTS OF P-GLYCOPROTEIN MODULATORS DUE TO ALTERED PHARMACOKINETICS OF ANTICANCER DRUGS", Therapeutic drug monitoring, 18(4), 1996, pp. 350-356

Abstract

Agents (modulators) that reverse the in vitro resistance of tumor cells to anticancer drugs that are substrates for P-glycoprotein (Pgp, the product of the MDR1 gene) have been given to patients concurrently with anticancer drugs in an attempt to improve therapeutic response. The vast majority of investigations into these drugs indicate that Pgp modulators decrease the systemic clearance of anticancer drugs, thus potentially nonselectively increasing exposure to normal and malignant cells and thereby potentially increasing the severity and/or incidence of adverse effects associated with the anticancer therapy. Mechanisms by which Pgp modulators could alter the pharmacokinetics of the anticancer agent include competition for cytochrome P450 intestinal or livermetabolism, inhibition of Pgp-mediated biliary excretion or intestinal transport, or inhibition of renal elimination. It is suggested that administration of Pgp modulators is unlikely to improve the therapeutic index for anticancer drugs unless agents that lack significant pharmacokinetic interactions are found. Moreover, it will likely be required that there be some cancer-tissue selectivity for modulators in orderto avoid collaterally increasing the sensitivity of normal Pgp-expressing tissues to the anticancer drug.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 22/01/20 alle ore 12:27:22