Milano G, Ferrero J-M, François E
Oncopharmocology Unit, Centre Antoine-Lacassagne, 33 Avenue de Valombrose, 06189 Nice Cedex 2, France.
Br J Cancer. 2004 Aug 16;91(4):613-7. doi: 10.1038/sj.bjc.6601973.
The main purpose of the present review article was to shed light on the different 5-fluorouracil (5-FU) prodrugs by underlining their respective pharmacological features in terms of metabolic activation, dihydropyrimidine dehydrogenase inhibition, pharmacokinetic profile and biomodulation ability. Oral fluoropyrimidines differ particularly as concerns their pharmacokinetic profile and especially in the delivery of circulating 5-FU. More clinical studies need to be performed incorporating tumour predictive markers during oral fluoropyrimidine-based treatment. The new possibilities are to achieve pharmacomodulation of oral fluoropyrimidines, notably for UFT and capecitabine, that open up the prospect of establishing significant novel treatment protocols based on drug combinations.
本综述文章的主要目的是通过强调不同的5-氟尿嘧啶（5-FU）前药在代谢活化、二氢嘧啶脱氢酶抑制、药代动力学特征和生物调节能力方面各自的药理学特性，来阐明这些前药。口服氟嘧啶在药代动力学特征方面存在差异，尤其是在循环5-FU的递送方面。在基于口服氟嘧啶的治疗过程中，需要进行更多纳入肿瘤预测标志物的临床研究。新的可能性在于实现口服氟嘧啶的药物调节，特别是对于优福定（UFT）和卡培他滨，这为基于药物组合建立重要的新型治疗方案开辟了前景。
