Taguchi T
Osaka University.
Gan To Kagaku Ryoho. 1993 Jan;20(1):10-8.
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.
BOF-A2、Ro09-1390、TT-62和S-1。BOF-A2和S-1都是5-氟尿嘧啶（5-FU）衍生物与5-FU降解抑制剂联合或混合的化合物，目的是延长血液中5-FU水平并增加对肿瘤的选择性毒性。此外，S-1中含有的G1期5-FU磷酸化抑制剂可降低因血液中5-FU水平延长而导致的如腹泻等G1期毒性。Ro09-1390是5'-去氧氟尿苷（5'-DFUR）的改良化合物，旨在减少后者引起的腹泻。TT-62是一种氟尿嘧啶脱氧核苷酸（FdUMP）衍生物，是5-FU的口服活性代谢物，其疗效优于现有的5-FU类抗癌药物，并且对5-FU不表现出交叉耐受性。
