A novel antimetabolite: TAS-102 for metastatic colorectal cancer

被引：8
|
作者：
Miyamoto, Yuji [1 ,2 ]
Lenz, Heinz-Josef [2 ]
Baba, Hideo [1 ]
机构：
[1] Kumamoto Univ, Dept Surg Gastroenterol, Grad Sch Med Sci, 1-1-1 Honjo, Kumamoto 8608556, Japan
[2] Univ So Calif, Kenneth Norris Jr Comprehens Canc Ctr, Div Med Oncol, Los Angeles, CA 90033 USA
来源：
EXPERT REVIEW OF CLINICAL PHARMACOLOGY | 2016年 / 9卷 / 03期
关键词：
refractory; salvage line; metastatic colorectal cancer; TAS-102; phase III; intolerant; chemotherapy; ORAL CHEMOTHERAPEUTIC-AGENT; RANDOMIZED PHASE-III; THYMIDINE KINASE 1; SOLID TUMORS; THYMIDYLATE SYNTHASE; FLUORINATED PYRIMIDINES; 1ST-LINE TREATMENT; ANTITUMOR-ACTIVITY; COMBINATION ANTIMETABOLITE; SYNERGISTIC INTERACTION;
D O I：
10.1586/17512433.2016.1133285
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
TAS-102 is a new oral anti-tumor drug, composed of a thymidine-based nucleoside analog (trifluridine: FTD) and a thymidine phosphorylase inhibitor (tipiracil hydrochloride: TPI). TAS-102 has been shown to significantly improve overall survival and progression-free survival in patients with refractory metastatic colorectal cancer (mCRC) in placebo-controlled randomized phase II and III trials. The current review summarizes mechanisms of action, pharmacokinetics/dynamics and preclinical and clinical data of TAS-102 in colorectal cancer. TAS-102 is a new salvage-line treatment option for patients with mCRC. TAS-102 is well tolerated and has great potential in future clinical drug combination therapies.
引用
收藏
页码：355 / 365
页数：11
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