5-Fluorouracil: Forty-Plus and Still Ticking. A Review of its Preclinical and Clinical Development

摘要: 5-Fluorouracil (5-FU) and 5-fluoro-2'-deoxyuridine (FdUrd) are pyrimidine analogs that have been part of the therapeutic armamentarium for a variety solid tumors over forty years. 5-FU has customarily required intravenous administration due to poor erratic oral bioavailability, while FdUrd generally employed regional liver or peritoneal cavity. A great deal knowledge gained concerning cellular pharmacology mechanism action since it was first synthesized in late 1950's. more thorough understanding factors influencing metabolic activation its effects generated considerable interest combining with both modulatory agents such as leucovorin methotrexate enhance metabolism cytotoxic effects. In addition, also activity other antineoplastic modalities cisplatin ionizing radiation which can synergize. Appreciation clinical led schedules clinically useful. The preclinical is reviewed provide basis exploring novel approaches permit prodrugs will be described articles this issue.