The oral fluoropyrimidines in cancer chemotherapy.
The oral fluoropyrimidines in cancer chemotherapy.
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发表时间：
1999-09
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通讯作者：
Elizabeth B. Lamont;R. Schilsky
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作者：
Elizabeth B. Lamont;R. Schilsky
作为合理开发的一类抗癌药物的典型例子，氟嘧啶类药物现在已成为进一步合理的癌症化疗方法的焦点，因为它们被转化为口服制剂。单独给药时，口服 5-氟尿嘧啶 (5-FU) 吸收不稳定，药代动力学呈非线性。然而，当口服 5-FU 作为前药和/或与二氢嘧啶脱氢酶抑制剂配对时，所得 5-FU 具有线性药代动力学，可能近似于骨髓抑制程度较低的连续静脉注射。不使用输液导管和泵的 5-FU 输注时间表。我们回顾了几种口服氟嘧啶类药物的临床前和临床经验。
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.