Lamont E B, Schilsky R L
Department of Medicine, the Robert Wood Johnson Clinical Scholars Program, University of Chicago, Illinois 60637, USA.
Clin Cancer Res. 1999 Sep;5(9):2289-96.
A classic example of a rationally developed class of anticancer drugs, the fluoropyrimidines are now the focus of further rational approaches to cancer chemotherapy as they are transformed into oral formulations. Given alone, oral 5-fluorouracil (5-FU) has erratic absorption and nonlinear pharmacokinetics. However, when oral 5-FU is given as a prodrug and/or paired with a dihydropyrimidine dehydrogenase inhibitor, the resultant 5-FU has linear pharmacokinetics that may approximate the less myelosuppressive continuous i.v. infusion schedule of 5-FU administration without the use of infusion catheters and pumps. We review the preclinical and clinical experience of several of the oral fluoropyrimidines.
氟嘧啶类药物是合理开发的一类抗癌药物的经典例子，随着它们转化为口服制剂，现在已成为癌症化疗进一步合理方法的焦点。单独使用时，口服5-氟尿嘧啶（5-FU）吸收不稳定且药代动力学呈非线性。然而，当口服5-FU作为前药给予和/或与二氢嘧啶脱氢酶抑制剂配对时，所得的5-FU具有线性药代动力学，这可能近似于5-FU给药时骨髓抑制作用较小的持续静脉输注方案，而无需使用输液导管和泵。我们回顾了几种口服氟嘧啶类药物的临床前和临床经验。
