TAS-102: a novel antimetabolite for the 21st century.
TAS-102: a novel antimetabolite for the 21st century.
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TAS-102：21 世纪的新型抗代谢药。
DOI：
10.2217/fon.15.276
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发表时间：
2016
期刊：
影响因子：
3.3
通讯作者：
H. Hochster
中科院分区：
文献类型：
--
作者：
N. Uboha;H. Hochster
TAS-102是一种新型抗代谢联合化疗药物，由重新发现的抗代谢药物三氟胸苷（trifluridine）与胸苷磷酸化酶代谢抑制剂tipiracil以1:0.5的摩尔比组合而成。作用机制研究表明，该药物通过掺入 DNA 发挥作用。临床前和临床研究均表明该药物与 5-氟尿嘧啶无交叉耐药性。 Tipiracil 还可能通过抑制胸苷磷酸化酶而具有抗血管生成作用。最近的随机 II 期和 III 期试验证明了对所有标准药物均无效的转移性结直肠癌的临床活性（改善无进展生存期、体能状态下降时间、延长总体生存期）。 TAS-102 单一疗法现已在日本和美国获得批准用于该适应症。
TAS-102, a novel antimetabolite combination chemotherapy agent, consists of a rediscovered antimetabolite agent, trifluorothymidine (trifluridine) combined with the metabolic inhibitor of thymidine phosphorylase, tipiracil, in a 1:0.5 molar ratio. Mechanism of action studies suggest that this agent works by incorporation into DNA. Both preclinical and clinical studies demonstrate that this agent is noncross-resistant with 5-fluorouracil. Tipiracil may also have antiangiogenic effects through inhibition of thymidine phosphorylase. Recent randomized Phase II and III trials demonstrate clinical activity (improved progression-free survival, time to decrease in performance status, prolonged overall survival) in metastatic colorectal cancer refractory to all standard agents. Monotherapy with TAS-102 has now been approved for this indication in Japan and in the USA.
影响因子：
50.3
作者：
Rahman, L;Voeller, D;Zajac-Kaye, M
通讯作者：
Zajac-Kaye, M
影响因子：
2.9
作者：
ECKSTEIN, JW;FOSTER, PG;SANTI, DV
通讯作者：
SANTI, DV