Pazdur R, Hoff P M, Medgyesy D, Royce M, Brito R
Division of Medicine, University of Texas, M. D. Anderson Cancer Center Houston, USA.
Oncology (Williston Park). 1998 Oct;12(10 Suppl 7):48-51.
Discussed herein are selected oral fluorinated pyrimidines that are converted to 5-fluorouracil (5-FU) in vivo to exert antitumor activity. These agents include capecitabine (Xeloda), tegafur-uracil (UFT) plus leucovorin (Orzel), and S-1 (BMS247616). These agents offer the convenience of an orally administered therapy with potentially fewer toxic effects than conventional bolus regimens of 5-FU plus leucovorin. These oral agents provide prolonged 5-FU exposure at lower peak concentrations than observed with bolus intravenous administration of 5-FU and may confer pharmacoeconomic advantages by reducing administration costs and toxicity-related hospitalizations. These regimens also have the potential for improved therapeutic activity by achieving higher 5-FU concentrations in the tumor or by biochemically modulating 5-FU. Phase III trials in patients with advanced colorectal carcinomas are comparing the antitumor activity of these agents with that of intravenous 5-FU plus leucovorin.
本文讨论了一些选定的口服氟嘧啶，它们在体内转化为5-氟尿嘧啶（5-FU）以发挥抗肿瘤活性。这些药物包括卡培他滨（希罗达）、替加氟-尿嘧啶（优福定）加亚叶酸钙（奥泽尔）和S-1（BMS247616）。这些药物提供了口服治疗的便利性，与传统的5-FU加亚叶酸钙推注方案相比，潜在毒性作用可能更少。这些口服药物在较低的峰值浓度下提供比5-FU静脉推注更长时间的5-FU暴露，并且通过降低给药成本和与毒性相关的住院治疗可能带来药物经济学优势。这些方案还具有通过在肿瘤中达到更高的5-FU浓度或通过生物化学调节5-FU来提高治疗活性的潜力。晚期结直肠癌患者的III期试验正在比较这些药物与静脉注射5-FU加亚叶酸钙的抗肿瘤活性。
