氟嘧啶类药物在胃肠道肿瘤中的作用：从实验室到临床
The Role of Fluoropirimidines in Gastrointestinal Tumours: from the Bench to the Bed.
作者信息
Hernando-Cubero Jorge, Matos-García Ignacio, Alonso-Orduña Vicente, Capdevila Jaume
机构信息
Medical Oncology Department, Miguel Servet University Hospital, Paseo Isabel la Católica 1-3, 5009, Zaragoza, Spain.
Medical Oncology Department, Vall d´Hebron University Hospital, Vall d´Hebron Institute of Oncology (VHIO), Pg Vall d´Hebron 119-129, 08035, Barcelona, Spain.
出版信息
J Gastrointest Cancer. 2017 Jun;48(2):135-147. doi: 10.1007/s12029-017-9946-5.
PURPOSE
Gastrointestinal tumours are one of the most common types of cancer. Therapeutic options include surgery, radiotherapy, local ablation techniques, targeted agents, and chemotherapy. Fluoroprimidines are one of the most active drug families in digestive tumours and remains the cornerstone of the most commonly used chemotherapy schemes.
METHODS
We review the molecular basis of thymidylate synthase inhibition and the mechanisms of action of 5-fluorouracil, next generation oral fluoropyrimidines (capecitabine, tegafur and the latest S-1 and TAS-102) and antifolates.
RESULTS
In addition, mechanisms and biomarkers of resistance and toxicity are explored. Finally, new fluoropyrimidines development and clinical trials ongoing in digestive tumours are reviewed.
CONCLUSIONS
Further research is necessary to avoid resistance mechanisms, improve clinical outcomes and continue reducing toxicities. Until new drugs become available, the optimization of current therapies should be a priority.
目的
胃肠道肿瘤是最常见的癌症类型之一。治疗选择包括手术、放疗、局部消融技术、靶向药物和化疗。氟嘧啶是消化系统肿瘤中活性最高的药物家族之一，仍然是最常用化疗方案的基石。
方法
我们回顾了胸苷酸合成酶抑制的分子基础以及5-氟尿嘧啶、新一代口服氟嘧啶（卡培他滨、替加氟以及最新的S-1和TAS-102）和抗叶酸药物的作用机制。
结果
此外，还探讨了耐药性和毒性的机制及生物标志物。最后，对正在进行的消化系统肿瘤新型氟嘧啶研发和临床试验进行了综述。
结论
有必要进行进一步研究以避免耐药机制、改善临床结果并持续降低毒性。在有新药可用之前，优化当前治疗应是首要任务。
Zotero 插件