更新于：2024-06-19
Tipiracil Hydrochloride
盐酸替匹嘧啶
更新于：2024-06-19
概要
基本信息
非在研机构- |
最高研发阶段临床1期 |
首次获批日期- |
最高研发阶段(中国)- |
特殊审评- |
结构
分子式C9H12Cl2N4O2 |
InChIKeyKGHYQYACJRXCAT-UHFFFAOYSA-N |
CAS号183204-72-0 |
关联
14
项与 盐酸替匹嘧啶 相关的临床试验3T: A Phase II Single Arm Open Label Study of Tucatinib Combined With Trastuzumab and TAS-102 in Molecularly Selected Patients With HER2+ Metastatic Colorectal Cancer
Phase Ib Open-Label Study to Evaluate Safety, Tolerability, Immunogenicity and Efficacy of Multiple Subcutaneous Injections of PolyPEPI1018 Vaccine as an Add-on Immunotherapy to TAS-102 in Late-Stage Metastatic Colorectal Cancer Subjects
Ramucirumab Plus Trifluridine/Tipiracil (TAS-102) for Patients With Previously Treated Advanced Gastric or Gastroesophageal Junction Adenocarcinoma: An Investigator-Initiated, Randomized Non-Inferiority Phase 2 Study
100 项与 盐酸替匹嘧啶 相关的临床结果
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100 项与 盐酸替匹嘧啶 相关的转化医学
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100 项与 盐酸替匹嘧啶 相关的专利（医药）
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386
项与 盐酸替匹嘧啶 相关的文献（医药）2024-03-04The oncologist
Trifluridine/Tipiracil Plus Bevacizumab for Vulnerable Patients With Pretreated Metastatic Colorectal Cancer: A Retrospective Study (WJOG14520G)
Article
作者: Shimokawa, Hozumi ; Nishina, Shinichi ; Tsuzuki, Takao ; Matsumoto, Toshihiko ; Kawakami, Takeshi ; Shinohara, Yudai ; Hasegawa, Hiroko ; Muro, Kei ; Yamazaki, Kentaro ; Ohta, Takashi ; Kito, Yosuke ; Nishina, Tomohiro ; Akiyoshi, Kohei ; Mitani, Seiichiro ; Chiba, Yasutaka ; Kumanishi, Ryosuke ; Katsuya, Hiroo ; Hironaka, Shuichi ; Kawakami, Hisato
Abstract:
Background:
Trifluridine/tipiracil (FTD/TPI) plus bevacizumab has shown clinical benefit for metastatic colorectal cancer (mCRC) refractory to standard therapy. However, few data have been available for patients with pretreated mCRC who are intolerant of intensive therapy (vulnerable).
Methods:
We performed a multicenter retrospective study (WJOG14520G; TWILIGHT) of FTD/TPI plus bevacizumab for vulnerable patients with pretreated mCRC. Eligibility criteria included previous chemotherapy (although patients treated with all key cytotoxic agents, a fluoropyrimidine, oxaliplatin, and irinotecan, were excluded) and intolerance of full-dose combination therapy with oxaliplatin or irinotecan at the start of FTD/TPI plus bevacizumab.
Results:
The median age of 93 evaluable patients was 79 years (range, 21-90). Intolerance of intensive therapy was attributable to an older age in 60 (65%) patients, serious concomitant disease in 24 (26%) patients, and a poor performance status in 19 (20%) patients. FTD/TPI plus bevacizumab was administered as second-line treatment in 74 (80%) patients and as third- or fourth-line treatment in 19 (20%) patients. The objective response rate was 4.9% (95% confidence interval [CI], 1.4%-12.2%), and the disease control rate was 67.9% (95% CI, 56.6%-77.8%). With a median follow-up time of 21.6 months, median overall survival and progression-free survival were 18.6 months (95% CI, 12.1-23.2) and 6.3 months (95% CI, 5.0-8.3), respectively. Neutropenia of grade ≥3 developed in 50 (54%) patients, whereas 2 (2%) patients experienced febrile neutropenia, and no treatment-related death was observed.
Conclusion:
Our data show the potential efficacy and acceptable safety profile of FTD/TPI plus bevacizumab for vulnerable patients with pretreated mCRC.
2024-03-01Clinical colorectal cancer
Cost-Effectiveness of the New Combination Trifluridine/Tipiracil Plus Bevacizumab for the Third-Line Treatment for Metastatic Colorectal Cancer in Italy
Article
作者: Giuliani, Jacopo ; Tommasi, Marina ; Napoli, Giuseppe ; Mandarà, Marta ; Mantoan, Beatrice ; Mangiola, Daniela ; Fiorica, Francesco ; Muraro, Marco
2024-02-01Journal of pharmaceutical and biomedical analysis
Simultaneous determination of tipiracil, trifluridine and its metabolite 5-trifluoromethyluracil in human plasma using segmented polarity LC-MS/MS: A fully validated assay with clinical application
Article
作者: Ding, Li ; Li, Xianjing ; Zhang, Xinrui ; Zhou, Qiaoyun ; Shu, Chang ; Zhang, Rong
Trifluridine (FTD) and tipiracil (TPI) hydrochloride tablets (TAS-102) were used for the treatment of patients with metastatic rectal cancer that was resistant to conventional chemotherapy drugs. In this study, a rapid and sensitive liquid chromatography-tandem mass spectrometry method was developed and fully validated for the simultaneous determination of TPI, FTD, and the metabolite 5-trifluoromethyluracil (FTY) of FTD in human plasma. The plasma samples were prepared by protein precipitation. The chromatography separation was performed using ACE Excel 3 AQ (100 × 2.1 mm i.d., 1.7 µm, ACE, England) column protected by a security guard cartridge (4.0 × 2.0 mm i.d., 5 µm, Phenomenex, USA) with a gradient elution of 0.05% acetic acid in water and methanol at a flow rate of 0.35 mL/min. The MS/MS analysis was performed by using multiple reaction monitoring with the segmented polarity (positive for TPI: m/z 243.1→183.0, and negative for FTD: m/z 295.1→252.0 and FTY: m/z 178.9→158.9) electrospray ionization mode. The segmented polarity mode was designed to achieve two advantages: better sensitivity and simultaneous determination of the analytes with different ion polarities. The calibration ranges were as follows: 1.00-250 ng/ for TPI, 8.00-8000 ng/mL for FTD and 5.00-1250 ng/mL for FTY. The selectivity, accuracy, precision, matrix effect, recovery, carryover, dilution integrity and stability test results meet ICH acceptance criteria. The method was evaluated using the RGB model and successfully applied to a clinical study in patients with solid tumors. For TPI, FTD and FTY, the maximum plasma concentration was 137-147 ng/mL, 6160-6240 ng/mL and 724-725 ng/mL, respectively; the plasma elimination half-life was 1.69-1.78 h, 1.70 h, and 3.09-3.14 h, respectively, after an oral administration of 60 mg TAS-102.
100 项与 盐酸替匹嘧啶 相关的药物交易
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研发状态
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 肿瘤 | 临床1期 | - | - |
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临床结果
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适应症
分期
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临床2期 | 转移性微卫星稳定结直肠癌 Microsatellite Stable | 18 | nivolumab+trifluridine+tipiracil | 窪鬱築醖鏇衊鏇鏇蓋構(蓋鏇壓鏇製觸觸願網餘) = 構範鹽艱鹹夢網鬱憲壓 壓廠願窪遞襯廠鹹餘願 (齋簾餘蓋糧蓋衊夢構艱, 1.8 ~ 5.1) 更多 | 不佳 | 2021-02-01 | |
临床1期 | 24 | 選淵襯夢襯餘壓窪築網(鹹餘膚繭廠築獵鹹範窪) = 35mg/㎡ [grade 3 febrile neutropenia] 繭蓋夢糧範齋積淵衊餘 (鹹壓餘壓簾壓範廠夢憲 ) | 积极 | 2019-05-01 | |||
临床3期 | 112 | 廠顧鹹壓築壓艱鑰選艱(鏇齋齋製繭夢蓋鑰顧壓) = 鑰蓋獵醖願窪襯鹹襯遞 餘醖襯鹽醖範襯膚構夢 (窪選積淵壓廠餘選廠選 ) 更多 | 积极 | 2017-02-01 | |||
Placebo | 廠顧鹹壓築壓艱鑰選艱(鏇齋齋製繭夢蓋鑰顧壓) = 遞淵餘繭製網繭醖鹹廠 餘醖襯鹽醖範襯膚構夢 (窪選積淵壓廠餘選廠選 ) 更多 | ||||||
临床3期 | 412 | (≥65 y) | 夢夢構構鬱遞築範選範(積獵鏇鬱願網製蓋鏇憲) = 鬱淵簾鹽膚齋廠糧襯繭 膚獵簾夢夢製糧襯廠壓 (範願齋繭鏇淵鏇餘遞簾 ) 更多 | 积极 | 2016-02-01 | ||
placebo (≥65 y) | 夢夢構構鬱遞築範選範(積獵鏇鬱願網製蓋鏇憲) = 築遞獵鬱鏇壓膚膚廠願 膚獵簾夢夢製糧襯廠壓 (範願齋繭鏇淵鏇餘遞簾 ) 更多 | ||||||
临床3期 | 800 | (Updated Analysis) | 醖願繭繭醖鬱窪艱網窪(夢夢膚壓夢鏇餘網製膚) = 夢顧鹽構鹽窪襯選築獵 築壓窪鹹糧夢範觸衊構 (膚鹽願網觸襯築鏇廠淵, 6.6 ~ 7.8) 更多 | 积极 | 2016-02-01 | ||
placebo (Updated Analysis) | 醖願繭繭醖鬱窪艱網窪(夢夢膚壓夢鏇餘網製膚) = 網獵餘遞鬱壓積範衊製 築壓窪鹹糧夢範觸衊構 (膚鹽願網觸襯築鏇廠淵, 4.6 ~ 5.9) 更多 |
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