[Development of fluorinated pyrimidines in Japan].
Four fluorinated pyrimidines that are in the stage of clinical trials at present in Japan were reviewed: BOF-A2, Ro09-1390, TT-62 and S-1. Both BOF-A 2 and S-1 are a compound of 5-FU derivative combined or mixed with an inhibitor of 5-FU degradation in order to prolong the blood 5-FU level as well as increase selective toxicity to tumor. Furthermore, an inhibitor of 5-FU phosphorylation in G1 tract contained in S-1 reduces G1 toxicity such as diarrhea etc due to prolongation of blood 5-FU level. Ro09-1390 is an improved compound of 5'-DFUR, which intends to reduce diarrhea caused by the latter. TT-62 is a FdUMP derivative and an active metabolite of 5-FU for oral formulation, which is superior to available 5-FU type anticancer agents in efficacy, and doesn't show cross tolerance to 5-FU.
Taguchi
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Osaka University.
D000818:Animals; D000970:Antineoplastic Agents / Q000493:pharmacokinetics / Q000627:therapeutic use; D002986:Clinical Trials as Topic; D003841:Deoxycytidine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000493:pharmacokinetics / Q000627:therapeutic use; D004338:Drug Combinations; D005468:Fluorodeoxyuridylate / Q000031:analogs & derivatives* / Q000627:therapeutic use; D005472:Fluorouracil / Q000031:analogs & derivatives* / Q000493:pharmacokinetics / Q000627:therapeutic use; D006801:Humans; D008325:Mammary Neoplasms, Experimental / Q000188:drug therapy; D051379:Mice; D008819:Mice, Nude; D009369:Neoplasms / Q000188:drug therapy / Q000378:metabolism; D009374:Neoplasms, Experimental / Q000188:drug therapy; D010094:Oxonic Acid / Q000493:pharmacokinetics / Q000627:therapeutic use; D011725:Pyridines / Q000493:pharmacokinetics / Q000627:therapeutic use; D051381:Rats; D005641:Tegafur / Q000493:pharmacokinetics / Q000627:therapeutic use
D000970:Antineoplastic Agents; D004338:Drug Combinations; D011725:Pyridines; D003841:Deoxycytidine; C063993:Ro 09-1390; D005468:Fluorodeoxyuridylate; C079198:S 1 (combination); D005641:Tegafur; D010094:Oxonic Acid; C076837:tetradecyl 2'-deoxy-5-fluoro-5'-uridylate; C053194:Emitefur; D005472:Fluorouracil