[5'-DFUR (doxifluridine)].
5'-DFUR is converted to 5-FU by pyrimidine nucleoside phosphorylase. The activity of this enzyme is higher in tissue tissue than in most normal tissues, leading to a significantly higher conversion to 5-FU and 5-FU concentration in the tumor tissue than in normal tissue and serum. This activation mechanism provides this compound with high tumor selective toxicity. Based on these characteristics, 5'-DFUR has shown significant antitumor activity with less toxicity and immunosuppressive activity in experimental models. In the clinical study, 5'-DFUR has shown antitumor activity in gastric, colo-rectum and breast cancer. Especially in breast cancer, high response was observed including CR cases and also suggested a fast onset of action and long duration of efficacy. In the safety, major adverse reaction was diarrhea but it was controllable. Bone marrow suppression and CNS toxicity were very mild. 5'-DFUR can be a good candidate for the combination regimen and surgical adjuvant chemotherapy.
D000818:Animals; D000970:Antineoplastic Agents / Q000378:metabolism / Q000627:therapeutic use*; D002286:Carcinoma, Ehrlich Tumor / Q000378:metabolism; D004341:Drug Evaluation; D005467:Floxuridine / Q000378:metabolism / Q000627:therapeutic use*; D005472:Fluorouracil / Q000378:metabolism; D005770:Gastrointestinal Neoplasms / Q000188:drug therapy* / Q000378:metabolism; D006801:Humans; D008114:Liver Neoplasms, Experimental / Q000378:metabolism; D051379:Mice; D012513:Sarcoma, Experimental / Q000378:metabolism
D000970:Antineoplastic Agents; D005467:Floxuridine; D005472:Fluorouracil; C025034:doxifluridine