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Titolo:
Fluorouracil and the new oral fluorinated pyrimidines
Autore:
Kuhn, JG;
Indirizzi:
Univ Texas, Hlth Sci Ctr, Dept Pharmacol Pharmacotherapy, San Antonio, TX 78284 USA Univ Texas San Antonio TX USA 78284 acotherapy, San Antonio, TX 78284 USA Univ Texas, Coll Pharm, Austin, TX 78712 USA Univ Texas Austin TX USA 78712 iv Texas, Coll Pharm, Austin, TX 78712 USA
Titolo Testata:
ANNALS OF PHARMACOTHERAPY
fascicolo: 2, volume: 35, anno: 2001,
pagine: 217 - 227
SICI:
1060-0280(200102)35:2<217:FATNOF>2.0.ZU;2-3
Fonte:
ISI
Lingua:
ENG
Soggetto:
DIHYDROPYRIMIDINE DEHYDROGENASE-DEFICIENCY; SEVERE 5-FLUOROURACIL TOXICITY; PHASE-I; CLINICAL-PHARMACOLOGY; COLORECTAL-CARCINOMA; ANTITUMOR-ACTIVITY; THYMIDINE PHOSPHORYLASE; 5-ETHYNYLURACIL 776C85; FAMILIAL PYRIMIDINEMIA; BIOCHEMICAL BASIS;
Keywords:
BOF-A2; capecitabine; dihydropyrimidine dehydrogenase; DpD; fluorouracil; fluorinated pyrimidines; fluoropyrimidines; eniluracil; 5-ethynyluracil; uracil-tegafur; uracil-ftorafur;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Clinical Medicine
Citazioni:
81
Recensione:
Indirizzi per estratti:
Indirizzo: Kuhn, JG Univ Texas, Hlth Sci Ctr, Dept Pharmacol Pharmacotherapy, 7703 Floyd Curl Dr, San Antonio, TX 78284 USA Univ Texas 7703 Floyd Curl Dr San Antonio TX USA 78284 78284 USA
Citazione:
J.G. Kuhn, "Fluorouracil and the new oral fluorinated pyrimidines", ANN PHARMAC, 35(2), 2001, pp. 217-227

Abstract

OBJECTIVE: To briefly review the biotransformation and bioavailability of fluorouracil (5-FU); discuss the effects of dihydropyrimidine dehydrogenase(DpD) on the efficacy and toxicity profiles of 5-FU; and review a new class of drugs known collectively as the oral fluorinated pyrimidines, which inhibit or circumvent DpD activity and, when administered with 5-FU, alter its pharmacokinetic and pharmacodynamic properties. DATA SOURCES: A MEDLINE literature search was conducted (1966-March 1999),using the search terms fluoropyrimidines, fluorouracil, 5-FU, fluorinated pyrimidines, capecitabine, eniluracil, uracil-tegafur, uracil-ftorafur, UR;S1, BMS-247616, and BOf-A2. Reference lists, bibliographies of pertinent articles, and abstracts from the American Society of Clinical Oncology and the San Antonio Breast Cancer Symposium annual meetings were also identifiedand reviewed. Both preclinical and clinical literature were reviewed and analyzed. DATA SYNTHESIS: The new oral fluorinated pyrimidines appear to produce antitumor activity equivalent or superior to that of intravenously administered 5-FU by achieving higher intratumoral 5-FU concentrations or sustained 5-FU exposure. These agents are generally associated with manageable and non-life-threatening toxicities. The oral route of administration facilitates ease of administration and may reduce total healthcare costs associated with5-FU-sensitive tumors. More Studies are needed to assess the therapeutic and economic benefits of the oral fluorinated pyrimidines. CONCLUSIONS: The bioavailability, efficacy, and toxicity of 5-FU depend onits catabolic rate-limiting enzyme, DpD. The new oral fluorinated pyrimidines inhibit or circumvent DpD activity and, when combined with 5-FU, increase 5-FU's bioavailability and cytotoxic effects and decrease its toxicities. Results of Phase I and II studies in patients with a variety of malignancies suggest positive outcomes, including greater efficacy, less drug-related toxicity, lower costs related to drug administration, and greater patientconvenience.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 11/07/20 alle ore 20:45:26