摘要
5-氟尿嘧啶(5-FU)作为一种细胞周期特异性抗代谢药物,因其抗瘤谱广,有效率高,被广泛应用于各类实体瘤的治疗。随着现代肿瘤学的不断发展,替加氟、卡莫氟、尿嘧啶替加氟(UFT)、卡培他滨、替吉奥、TAS-102等一系列新型5-FU衍生物被逐渐研发出来,并继续在消化系统肿瘤、肺癌、乳腺癌等多种肿瘤治疗中发挥重要的抗肿瘤作用。目前关于5-FU及其衍生物抗肿瘤作用的研究进展尚无全面、详尽的总结,本文对此进行概括与综述,以提高临床肿瘤科医师对经典抗代谢类肿瘤药物的认识。
引文
[1] Heidelberger C, Chaudhuri NK, Danneberg P, et al. Fluorinated pyrimidines, a new class of tumour-inhibitory compounds[J]. Nature, 1957, 179(4561):663-666.
[2] Baba H, Teramoto K, Kawamura T, et al. Dihydropyrimidine dehydrogenase and thymidylate synthase activities in hepatocellular carcinomas and in diseased livers[J]. Cancer Chemother Pharmacol, 2003, 52(6):469-476.
[3]韩晓燕,卫洪波,连建学,等. 5-氟尿嘧啶不同给药途径的药代动力学研究和临床应用[J].中国新药杂志, 1999, 8(1):20-23.
[4]时静,陈海生,段存贤,等. 5-氟尿嘧啶治疗药物监测的研究现状[J].中国临床药学, 2016, 32(11):1053-1056.
[5] Kaldate RR, Haregewoin A, Grier CE, et al. Modeling the 5-fluorouracil area under the curve versus dose relationship to develop a pharmacokinetic dosing algorithm for colorectal cancer patients receiving FOLFOX6[J]. Oncologist, 2012,17(3):296-302.
[6] Meta-analysis Group In Cancer, Piedbois P, Rougier P, et al.Efficacy of intravenous continuous infusion of fluorouracil compared with bolus administration in advanced colorectal cancer[J]. J Clin Oncol, 1998, 16(1):301-308.
[7]陈昕,梁超,雷开键,等.时辰化疗作用机制的生物学研究进展[J].现代预防医学, 2008, 35(2):201-207.
[8]刘德传,刘庆春,钟志凯,等.时辰化疗临床研究综述[J].中国临医药指南, 2010, 8(17):61-62.
[9]张力,林忠,夏忠军,等.大剂量醛氢叶酸+5FU持续滴注48小时(双周疗法)治疗晚期大肠癌的临床研究[J].癌症,2000, 19(4):296-299.
[10]黄敏.氟尿嘧啶类抗癌药耐药机理及化疗增敏剂的研究进展[J].国外医学(肿瘤学分册), 1998, 25(2):94-97.
[11]徐旭,徐寰骞,黄新恩.紫杉醇脂质体或紫杉醇联合替加氟和奥沙利铂治疗晚期胃癌的比较[J].中国新药与临床杂志, 2011, 30(6):467-470.
[12]李永亮,刑珊珊,罗以,等.替加氟或氟尿嘧啶联合奥沙利铂对结直肠癌术后辅助化疗的疗效比较[J].世界华人消化杂志, 2013, 21(31):3460-3463.
[13]罗兴喜,陈涛.氟尿嘧啶类抗癌药物新发展[J].岭南现代临床外科, 2004, 4(4):299-300.
[14] Maehara Y, Anai H, Kusumoto H, et al. Colorectal carcinoma in vitro is more sensitive to 1-hexylcarbamoyl-5-fluorouracil compared with six other antitumor drugs:carboquone, adriamycin, mitomycin C, aclacinomycin A, cisplatin, 5-fluorouracil[J]. Dis Colon Rectum, 1988, 31(1):62-67.
[15] Koyama Y. 1-Hexylcarbamoyl-5-fluorouracil(HCFU)—a masked 5-fluorinated pyrimidine[J]. Cancer Treat Rev,1981, 8(2):147-156.
[16]史冬梅.卡莫氟为主联合化疗治疗晚期消化道肿瘤的临床研究[J].中国医药指南, 2014, 12(2):98-100.
[17]周际昌.抗癌药物的临床应用[M].北京:化学工业出版社, 2001:64-66.
[18] Nio Y, Iguchi C, Yamasawa K. Oral UFT(uracil plus futrafu)for neoadjuvant chemotherapy of gastric cancer[J].Gastric Cancer, 1999, 2(1):64-73.
[19] Ho DH, Pazdur R, Covington W, et al. Comparison of 5-fluorouracil pharmacokinetics in patients receiving continuous 5-fluorouracil infusion and oral uracil plus N1-(2’-tetrahydrofuryl)-5-fluorouracil[J]. Clin Cancer Res, 1998,4(9):2085-2088.
[20]贺文茜,张宁,孙京栋. UFTP方案治疗晚期胃癌近期疗效观察[J].临床肿瘤学杂志, 2011, 6(2):146-148.
[21] Douillard JY, Hoff PM, Skillings JR, et al. Multicenter phase study of uracil/tegafur and oral leucovorin versus fluorouracil and leucovorin in patients with previously untreated metastatic colorectal cancer[J]. J Clin Oncol, 2002,20(17):3605-3616.
[22] Carmichael J, Popiela T, Radstone D, et al. Randomized comparative study of tegafur/uracil and oral leucovorin versus parenteral fluorouracil and leucovorin in patients with previously untreated metastatic colorectal cancer[J].J Clin Oncol, 2002, 20(17):3617-3627.
[23]吴剑.替吉奥胶囊治疗晚期胃癌的近期疗效[J].北方药学, 2016, 13(10):39.
[24]米希茂,张素娟.替吉奥单药治疗老年进展期胃癌的临床研究[J].中国药物与临床, 2016, 16(10):1479-1481.
[25] Koizumi W, Kurihara M, Nakano S, et al. Phase II study of S-1, a novel oral derivative of 5-fluorouracil, in advanced gastric cancer. For the S-1 Cooperative Gastric Cancer Study Group[J]. Oncology, 2000, 58(3):191-197.
[26] Takahashi I, Kakeji Y, Emi Y, et al. S-1 in the treatment of advanced and recurrent gastric cancer:current state and future prospects[J]. Gastric Cancer, 2003, 6(1):28-33.
[27] Boku N, Gastrointestinal Oncology Study Group of Japan Clinical Oncology Group. Chemotherapy for metastatic disease:review from JCOG trials[J]. Int J Clin Oncol,2008, 13(3):196-200.
[28] Sasako M, Sakuramoto S, Katai H, et al. Five-year outcomes of a randomized phase III trial comparing adjuvant chemotherapy with S-1 versus surgery alone in stage II or III gastric cancer[J]. J Clin Oncol, 2011, 29(33):4387-4393.
[29] Twelves C, Glynne-Jones R, Cassidy J, et al. Effect of hepatic dysfunction due to liver metastases on the pharmacokinetics of capecitabine and its metabolites[J]. Clin Cancer Res, 1999, 696(5):1696-1702.
[30]晋国权,李淼.Ⅱ、Ⅲ期结肠癌患者TS、TP和DPD表达水平与5-Fu为基础的化疗疗效及预后的关系研究[J].河北医药, 2017, 39(6):805-809.
[31] Cassidy J, Clarke S, Díaz-Rubio E, et al. XELOX vs FOLFOX-4 as first-line therapy for metastatic colorectal cancer:NO16966 updated results[J]. Br J Cancer, 2011,105(1):58-64.
[32] Burki TK. TAS-102 in metastatic colorectal cancer[J]. Lancet Oncol, 2018, 19(1):e18.
[33] Yasue F, Kimura M, Usami E, et al. Risk factors contributing to the development of neutropenia in patients receiving oral trifluridine-tipiracil(TAS-102)chemotherapy for advanced/recurrent colorectal cancer[J]. Pharmazie, 2018,73(3):178-181.