英文药名：Lonsurf combination tablet T15/T20（Trifluridine/Tipiracil Hydrochloride） 中文药名：氟尿苷/Tipiracil盐酸盐配合锭 生产厂家：大鹏药业 ロンサーフ配合錠T15／ロンサーフ配合錠T20 药品类别：抗恶性肿瘤剤 上市批准日期：2014年5月 商標名 Lonsurf combination tablet T15 Lonsurf combination tablet T20 トリフルリジン 一般名 トリフルリジン（Trifluridine） 化学名 2'-Deoxy-5-(trifluoromethyl)uridine 構造式 分子式 C10H11F3N2O5 分子量 296.20 融点 約182℃（分解） 性状 它是一种结晶性粉末或白色结晶。 它是易溶于甲醇，微溶于乙醇（99.5）和水。 チピラシル塩酸塩 一般名 チピラシル塩酸塩（Tipiracil Hydrochloride） 化学名 5-Chloro-6-[(2-iminopyrrolidin-1-yl)methyl]pyrimidine-2,4 (1H,3H)-dione monohydrochloride 構造式 分子式 C9H11ClN4O2・HCl 分子量 279.12 融点 約241℃（分解） 性状 它是一种结晶性粉末或白色结晶。 它易溶于水，微，极微溶于甲醇，和乙醇（99.5）几乎不溶。 审批条件 为了验证这种药物的疗效和安全性的宗旨，为治疗不能手术切除的晚期或复发，大肠癌第三期临床试验正在进行立即结果的测试后，才能进行评价提交。 适应病症 大肠癌的治疗不能手术切除的晚期或复发。 剂量与用法 每日两次后晚餐和早餐后，连续5天，如下的参考量，按体表面积的起始剂量（1剂量）成人2天的休息口服剂量后。从用药停药14天就重复两次后。此外，根据患者的病情减轻。 （见表剂量和用法） 药效药理 1. 抗肿瘤效果 在裸鼠皮下植入HCT-116细胞系和人结肠癌衍生COL-1细胞系，这种药物表现出肿瘤生长的抑制作用。此外，在裸小鼠腹膜内移植了人大肠癌细胞来源的细胞系KM20C，这种药物显示出生存益处。 2. 作用机序 在裸鼠皮下植入人肿瘤衍生的细胞系，FTD的掺入DNA的量的肿瘤生长抑制效果密切相关，这种药物的肿瘤生长抑制效果也基于该FTD时，FTD的DNA据估计肿瘤生长抑制效应是由掺入作用。 另外，当口服单独给予FTD猴子，FTD难以在血液中观察到的，FTD的血液浓度是通过使用能抑制ATP酶活分解酶FTD TPI的组合保持。 包装规格： 组合片T15 PTP包装：20錠（10錠×2）、60錠（10錠×2×3） 组合片：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/ 治疗晚期结直肠癌药物TAS-102获日本MHLW批准 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。 Anticancer Drug Lonsurf® Combination Tablet Receives NHI Reimbursement Price Listing and is Scheduled for Launch Taiho Pharmaceutical Co., Ltd. (HQ: Tokyo, President and Representative Director: Masayuki Kobayashi) announced today that the oral anticancer drug "Lonsurf® combination tablet T15, T20" (nonproprietary names: trifluridine and tipiracil hydrochloride; development code: TAS-102) had received a National Health Insurance (NHI) reimbursement price listing. Lonsurf is scheduled for launch in Japan on May 26. Lonsurf is an oral nucleoside antitumor agent developed by Taiho. Based on the results of Phase II clinical trial conducted in Japan, Taiho received approval on March 24, 2014 for the manufacture and marketing, initially in Japan, for the indications of "unresectable advanced or recurrent colorectal cancer (only if refractory to standard therapies)." A global Phase III clinical trial (RECOURSE) in patients with refractory metastatic colorectal cancer (mCRC) demonstrated a significant improvement in overall survival (OS), the trial's primary endpoint, in the TAS-102 arm compared to the placebo arm. Based on these results, the company plans to pursue regulatory submissions in the United States and Europe. Taiho is proud to make Lonsurf available to physicians in Japan as a new treatment option for patients with unresectable advanced or recurrent colorectal cancer refractory to standard therapies. About Lonsurf Lonsurf is an oral 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. About RECOURSE The RECOURSE trial is a global, randomized, double-blind, placebo-controlled Phase III comparison trial evaluating the efficacy and safety of orally administered TAS-102 in patients with refractory mCRC. The trial enrolled 800 patients who received at least two prior regimens of standard chemotherapies for mCRC and were refractory to, or failed, those chemotherapies. The trial was conducted in Japan, North America, Europe and Australia. Patients were randomly assigned to receive either TAS-102 or placebo in order to investigate the efficacy of TAS-102. The primary objective of the RECOURSE trial was improvement in overall survival (OS) versus placebo. Product Summary (for the Japanese market) Brand name Lonsurf® combination tablet T15, T20 Nonproprietary name Trifluridine and tipiracil hydrochloride 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 regimen twice, a 14-day rest follows, completing one course, which is then repeated. The dose can be decreased according to the patient's condition. Date of manufacturing and marketing approval March 24, 2014 Date listed in NHI reimbursement price listing May 23, 2014 Date of initial marketing in Japan May 26, 2014 Packaging Lonsurf combination tablet T15 PTP Packaging: 20 tablets (10 tablets x 2 sheets); 60 tablets (10 tablets x 2 x 3 sheets) Lonsurf combination tablet T20 PTP Packaging: 20 tablets (10 tablets x 2 sheets); 60 tablets (10 tablets x 2 x 3 sheets) NHI reimbursement price Manufacturing Distributor Taiho Pharmaceutical Co., Ltd.