2014年3月24日，日本MHLW批准大鹏药业Taiho Pharma的TAS-102（曲氟胸苷+tipiracil），用于治疗不可切除型或复发型晚期结直肠癌。曲氟胸苷是一种核苷类抗癌药，干扰癌细胞DNA的合成，tipiracil是胸苷磷酸化酶抑制剂，减少曲氟胸苷的降解。
英文药名：Trifluridine/Tipiracil Hydrochloride
中文药名：三氟尿苷/Tipiracil盐酸盐片
商品名：
Lonsurf combination tablet T15
Lonsurf combination tablet T20
缩写名：TAS-102
原研和生产厂商：日本大鹏药业(TaihoPharma)
上市国家：日本
上市日期：2014年3月24日
适应症：
不可切除的晚期或复发型结直肠癌
作用机制：
TAS-102是新型组合抗代谢药物，由核苷类似物FTD(三氟胸苷，Trifluridine)与TPI(Tipiracil)组成。FTD在DNA的复制时代替胸腺嘧啶直接溶入DNA链，引起DNA的功能障碍，干扰癌细胞DNA的合成；TPI可以抑制和FTD分解相关的胸腺嘧啶磷酸化酶，从而维持FTD的血液浓度，减少FTD的降解。
剂量与用法：
每次约35mg/m2(以FTD计)，每日两次，早晚餐后，连续5天，
作用机理
在裸鼠皮下植入人肿瘤衍生的细胞系，肿瘤抑制效果与FTD掺入DNA的量密切相关。另外，当单独给予猴子FTD口服时，在血液中几乎监测不到FTD，而TPI的应用能使FTD保持有效的血药浓度。
主要不良反应：
TAS-102的主要不良反应是血液毒性（贫血，中性粒细胞减少，白细胞减少）和消化系统（腹泻，恶心，呕吐）。3级以上的不良反应发现率，TAS-102给药组和安慰剂组各为：中性粒细胞减少37.9％、0％，贫血18.2％，3.0％，血小板减少5.1％，0.4％，发热性中性粒细胞减少症3.8％、0％，腹泻3.0％，0.4％，呕吐2.1％，0.4％，恶心1.9％，1.1％，倦怠感3.9％，5.7％，口腔炎0.4％、0%。
包装规格：
组合片剂 T15
PTP包装：20錠（10錠×2）、60錠（10錠×2×3）

组合片剂 T20
PTP包装：20錠（10錠×2）、60錠（10錠×2×3）

制造厂商
大鹏药业有限公司
注：使用以原处方为准：http://www.info.pmda.go.jp/go/pack/4299100F1026_1_03/

ロンサーフ配合錠T15／ロンサーフ配合錠T20

Taiho Pharmaceutical Co., Ltd. (HQ: Tokyo, President: Masayuki Kobayashi) announced today that it has obtained approval in Japan from the Ministry of Health, Labour and Welfare to manufacture and market the oral combination anticancer drug ''Lonsurf? combination tablet T15, T20'' (nonproprietary names: trifluridine and tipiracil hydrochloride; development code: TAS-102), for the treatment of patients with unresectable advanced or recurrent colorectal cancer (only if refractory to standard therapies).
Japan is the first country in the world to grant marketing authorization for Lonsurf. The approval is based primarily on the results of a randomized, double blind placebo controlled Phase II clinical trial conducted in Japan (J003-10040030). Taiho is conducting a global Phase III clinical trial (RECOURSE) on patients with metastatic colorectal cancer refractory to standard chemotherapies.
Lonsurf is a combination drug of trifluridine (FTD) and tipiracil hydrochloride (TPI). FTD is an antineoplastic nucleoside analog, which is incorporated directly into DNA, thereby interfering with the function of DNA. The blood concentration of FTD is maintained via TPI, which is an inhibitor of the FTD-degrading enzyme thymidine phosphorylase.
Taiho Pharmaceutical is proud to make Lonsurf available to physicians in Japan as a new treatment option for patients with metastatic colorectal cancer refractory to standard therapies.
Product Summary (for the Japanese market)
Brand name
Lonsurf combination tablet T15, T20
Nonproprietary name
Trifluridine and tipiracil hydrochloride combination tablet
Indications & Efficacy
Unresectable advanced or recurrent colorectal cancer (only if refractory to standard therapies)
Use & Dosage
Usually, the initial dose (single dose) for adults is defined as the standard dose (approximately 35 mg/m2/dose of FTD) according to body surface area. Lonsurf is administered twice daily, after breakfast and after the evening meal, for five consecutive days, followed by a two-day rest. After repeating the above twice, a 14-day rest follows, completing one course, which is then repeated.The dose can be decreased or increased according to the patient's condition.