title: The oral fluorouracil prodrugs.
abstract: Discussed herein are selected oral fluorinated pyrimidines that are converted to 5-fluorouracil (5-FU) in vivo to exert antitumor activity. These agents include capecitabine (Xeloda), tegafur-uracil (UFT) plus leucovorin (Orzel), and S-1 (BMS247616). These agents offer the convenience of an orally administered therapy with potentially fewer toxic effects than conventional bolus regimens of 5-FU plus leucovorin. These oral agents provide prolonged 5-FU exposure at lower peak concentrations than observed with bolus intravenous administration of 5-FU and may confer pharmacoeconomic advantages by reducing administration costs and toxicity-related hospitalizations. These regimens also have the potential for improved therapeutic activity by achieving higher 5-FU concentrations in the tumor or by biochemically modulating 5-FU. Phase III trials in patients with advanced colorectal carcinomas are comparing the antitumor activity of these agents with that of intravenous 5-FU plus leucovorin.
authors.affiliation: Division of Medicine, University of Texas, M. D. Anderson Cancer Center Houston, USA.
authors.forename: R
authors.initials: R
authors.lastname: Pazdur
authors.forename: P M
authors.initials: PM
authors.lastname: Hoff
authors.forename: D
authors.initials: D
authors.lastname: Medgyesy
authors.forename: M
authors.initials: M
authors.lastname: Royce
authors.forename: R
authors.initials: R
authors.lastname: Brito
mesh_terms: D000284:Administration, Oral; D000964:Antimetabolites, Antineoplastic / Q000008:administration & dosage*; D000069287:Capecitabine; D003841:Deoxycytidine / Q000008:administration & dosage / Q000031:analogs & derivatives / Q000737:chemistry; D005472:Fluorouracil / Q000008:administration & dosage*; D006801:Humans; D002955:Leucovorin / Q000008:administration & dosage; D010094:Oxonic Acid / Q000008:administration & dosage / Q000737:chemistry; D011355:Prodrugs; D011725:Pyridines / Q000008:administration & dosage / Q000737:chemistry; D005641:Tegafur / Q000008:administration & dosage / Q000737:chemistry; D014498:Uracil / Q000008:administration & dosage / Q000737:chemistry
chemical_list: D000964:Antimetabolites, Antineoplastic; D011355:Prodrugs; D011725:Pyridines; D003841:Deoxycytidine; D005641:Tegafur; D014498:Uracil; D010094:Oxonic Acid; D000069287:Capecitabine; D002955:Leucovorin; D005472:Fluorouracil