英文药名:Lonsurf combination tablet(Trifluridine Tipiracil Hydrochloride)
中文药名:三氟胸苷和tipiracil盐酸盐片
生产厂家:大鹏药品
ロンサーフ配合錠T15/ロンサーフ配合錠T20
治疗类别名称 抗肿瘤药 批准上市时间:2014年月 商標名 Lonsurf combination tablet T15 Lonsurf combination tablet T20 トリフルリジン 構造式
一般名 トリフルリジン(Trifluridine) 化学名 2'-Deoxy-5-(trifluoromethyl)uridine 分子式 C10H11F3N2O5 分子量 296.20 融点 約182℃(分解) 性状 它是一种白色晶体或结晶粉末。 易溶于甲醇,水和乙醇(99.5)微溶。 チピラシル塩酸塩 構造式
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 分子式 C9H11ClN4O2・HCl 分子量 279.12 融点 約241℃(分解) 性状 它是一种白色晶体或结晶粉末。 微溶于水,在甲醇中极微溶,并在乙醇(99.5)几乎不溶。 药效药理 1. 抗肿瘤作用 人的大肠癌细胞衍生COL-1细胞在裸鼠中线和HCT-116细胞系皮下植入,该药物表现出肿瘤生长的抑制作用。此外,在裸小鼠与人大肠癌细胞衍生KM20C的细胞系在腹腔被移植,药物呈存活益处。 2. 作用机理 肿瘤衍生的细胞系皮下植入,因为掺入DNA FTD的量和肿瘤生长抑制效果相关,这种药物的FTD,还了FTD的DNA的基础上的肿瘤增殖抑制效果估计由正在采取的肿瘤生长抑制效果被发挥。 此外,当在猴子口服FTD单独,虽然FTD基本上不血液中观察到的,FTD的血液浓度通过抑制TPase分解酶FTD TPI的组合保持。 适应病症: 不能手术切除,晚期或复发性结肠癌,直肠癌 用法与用量 成人以适合初始剂量(量一次)体表面积至下一参考量(约35毫克/平方米/剂量为三氟胸苷),早餐后和晚餐后,一天两次,连续5天其次是口服给药后停药两天。随后停药14天后此重复两次。重复给药,本为一疗程。 应当指出的是,根据该状态的患者减肥。 (见用法和剂量的表) 用法与用量的表
体表面積(m2) |
初回基準量 (トリフルリジン相当量) |
~1.07未満 |
35mg/回(70mg/日) |
1.07以上~1.23未満 |
40mg/回(80mg/日) |
1.23以上~1.38未満 |
45mg/回(90mg/日) |
1.38以上~1.53未満 |
50mg/回(100mg/日) |
1.53以上~1.69未満 |
55mg/回(110mg/日) |
1.69以上~1.84未満 |
60mg/回(120mg/日) |
1.84以上~1.99未満 |
65mg/回(130mg/日) |
1.99以上~2.15未満 |
70mg/回(140mg/日) |
2.15以上~ |
75mg/回(150mg/日) | 包装 组合片剂 T15 PTP包装:20片(10片×2),60片(10片×2×3) 组合片剂T20 PTP包装:20片(10片×2),60片(10片×2×3)
制造厂商 大鹏药业有限公司 完整处方附件:http://www.info.pmda.go.jp/go/pack/4299100F1026_1_03/ 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。
Taiho's Lonsurf®(trifluridine and tipiracil hydrochloride) Tablets Approved in Japanfor Treatment in Advanced me-tastatic Colorectal Cancer 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 combinationanticancerdrug'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 me-tastatic 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 me-tastatic 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 tabletIndications & Efficacy Unresectable advanced or recurrent colorectal cancer refractory to standard therapies Use & Dosage Usually, the initial dose (single dose) for adults is defined as the standard dose (approximately 35mg/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.
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