曲氟尿苷替匹嘧啶在消化道肿瘤中的研究进展

Progress of research on trifluridine-tipiracil usage in gastrointestinal malignancies

曲氟尿苷替匹嘧啶(TAS-102)是一种由曲氟尿苷(FTD)和胸苷磷酸化酶抑制剂(TPI)组成的口服化疗药物。体外和异种移植模型均证实TAS-102对5-氟尿嘧啶耐药的肿瘤具有抗肿瘤活性。基于Ⅲ期临床试验中TAS-102为患者带来生存获益,目前已被批准用于转移性结直肠癌和胃癌患者的三线治疗。近年来,有研究初步表明TAS-102在各种消化道肿瘤中均有一定疗效。本文总结了TAS-102在消化道肿瘤中的临床应用,并对TAS-102联合其他抗肿瘤药物的合理性及临床获益进行综述。

Trifluridine-tipiracil(TAS-102)is an oral chemotherapeutic agent combination comprising a fluoropyrimidine(FTD)and a potent thymidine phosphorylase(TPI)inhibitor.TAS-102 is novel due to its antitumor activity against 5-fluorouracil resistant tumors,demonstrated both by in vitro models and xenografts.TAS-102 is currently approved as a third-line therapeutic strategy for metastatic colorectal and gastric cancer based on phaseⅢrandomized clinical trial data confirming survival benefits with TAS-102.Preliminary data from recent studies suggest a potential expanding role of TAS-102 in various gastrointestinal(GI)cancers.This article summarizes the clinical applications of TAS-102 in the treatment of GI cancers.Additionally,we discuss the rationale and clinical benefits of combining TAS-102 with other anticancer agents in patients with GI cancers.