Schedule dependency of 5-fluorouracil.
5-Fluorouracil (5-FU) is cell-cycle specific for its cytotoxicity and has a pharmacokinetic profile characterized by a short, single-dose half-life of 10 to 20 minutes in plasma. Efforts to maximize its clinical efficacy have been directed at overcoming this short half-life. Strategies have included prolonging intracellular exposure by biochemical modulation or administration by infusional schedules, and more recently by chronic oral dosing. A number of clinical trials comparing routes of administration and biochemical modulation of 5-FU are presented in this article. Issues of dose intensity, differing toxicity profiles, and pharmacoeconomics are reviewed.
Leichman
C G
CG
Roswell Park Cancer Institute, Buffalo, New York, USA.
D000284:Administration, Oral; D000964:Antimetabolites, Antineoplastic / Q000008:administration & dosage* / Q000493:pharmacokinetics; D002453:Cell Cycle / Q000187:drug effects; D002986:Clinical Trials as Topic; D015179:Colorectal Neoplasms / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology; D004334:Drug Administration Schedule; D005472:Fluorouracil / Q000008:administration & dosage* / Q000493:pharmacokinetics; D006801:Humans; D007262:Infusions, Intravenous; D016896:Treatment Outcome
D000964:Antimetabolites, Antineoplastic; D005472:Fluorouracil