预约演示
更新于：2025-05-25
Raltitrexed
雷替曲塞
更新于：2025-05-25
概要
基本信息
原研机构 |
权益机构- |
最高研发阶段批准上市 |
首次获批日期 澳大利亚 (1996-07-15), |
最高研发阶段(中国)批准上市 |
特殊审评- |
登录后查看时间轴
结构/序列
分子式C21H22N4O6S |
InChIKeyIVTVGDXNLFLDRM-HNNXBMFYSA-N |
CAS号112887-68-0 |
关联
78
项与 雷替曲塞 相关的临床试验ChiCTR2400094120
Efficacy and safety of liposomes irinotecan combined with Raltitrexed and fuquitinib in second-line treatment of advanced colorectal cancer
ChiCTR2400093975
A single-arm, single-center, phase II clinical study of tislelizumab + GemCis systemic chemotherapy + raltitrexed hepatic artery infusion conversion therapy for locally unresectable intrahepatic cholangiocarcinoma
NCT06665087
Comprehensive Geriatric Assessment (CGA) Guided Ultrafractionated Radiotherapy and First-line Systemic Treatment in Elderly or Frail Patients with Metastatic Colorectal Cancer
100 项与 雷替曲塞 相关的临床结果
登录后查看更多信息
100 项与 雷替曲塞 相关的转化医学
登录后查看更多信息
100 项与 雷替曲塞 相关的专利（医药）
登录后查看更多信息
1,268
项与 雷替曲塞 相关的文献（医药）2025-08-01JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
Simultaneous analysis of various anticancer drugs by supercritical fluid chromatography-mass spectrometry. Part I: Optimization of chromatographic separation
Article
作者: Guillarme, Davy ; Rudaz, Serge ; Fleury-Souverain, Sandrine ; Bonnabry, Pascal ; Nguyen, Nathalie
This work presents a generic SFC-MS method for the simultaneous analysis of 22 anticancer drugs (fluorouracil, busulfan, cyclophosphamide, cytarabine, dacarbazine, daunorubicin, docetaxel, doxorubicin, epirubicin, etoposide, gemcitabine, idarubicin, ifosfamide, irinotecan, methotrexate, paclitaxel, pemetrexed, raltitrexed, topotecan, treosulfan, vinblastine, vincristine). The separation conditions were optimized by screening nine stationary phases (2-picolylamine, bare hybrid silica, 2-ethylpyridine, fluoro-phenyl, octadecyl, diethylamine, diol, 1-aminoanthracene, zwitterionic modification), evaluating additives effects (2-5 % water, 20-50 mM ammonium formate, 0-1 mM ammonium fluoride), and adjusting the organic modifier composition (methanol, ethanol, isopropanol, acetonitrile). The optimized SFC-MS method successfully analyzed 22 anticancer drugs, along with 5 additional challenging compounds (azacitidine, mitomycin, cisplatin, oxaliplatin, carboplatin), in 12 min, using a diol column (100 × 3 mm, 1.7 µm) and a gradient of 2-100 % methanol containing 2 % water and 50 mM ammonium formate. To overcome overpressure generated by high organic solvent content, a backpressure gradient (110-150 bar) and a flow rate gradient (0.6-1.5 mL/min) were applied. The diol column was selected as the most promising based on five predefined chromatographic criteria. Additives with 5 % water or ammonium fluoride were excluded due to overpressure and signal loss, respectively. Increasing ammonium formate concentration improved peak symmetry by 29 %. For the organic modifier, pure methanol was chosen since ternary mixtures led to system overpressure without improving separation. Comparison with the LC-MS method using real samples confirmed the potential applicability of the SFC method, as the same trace compounds were detected with comparable concentrations. Sensitivity optimization and method validation will be discussed separately in a later paper.
2025-05-01BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
Structural insight into ligand interactions of thymidylate synthase from white spot syndrome virus
Article
作者: Liu, Changshui ; Ma, Qingjun ; Zang, Kun
White spot syndrome virus (WSSV) is one of the deadliest crustacean pathogens, causing huge economic loss in global shrimp industry. WSSV encodes a thymidylate synthase (wTS) that is essential for DNA replication and viral proliferation, serving as a promising drug target against WSSV infections. To aid drug design, we solved wTS structures in complex with dUMP and dUMP/raltitrexed, at 2.28 Å and 1.43 Å resolutions, respectively. wTS forms a homodimer and each ligand-binding cavity is contributed by both monomers. In wTS-dUMP binary structure, the protein adopts an open conformation, with dUMP bound to the cavity through extensive hydrogen bonds and salt bridges. In wTS-dUMP-raltitrexed ternary structure, the protein exhibits a closed conformation; the TS inhibitor raltitrexed contacts intensively with the protein and dUMP via hydrogen bonding and hydrophobic interactions, resulting in the covalent bond formation between dUMP and the catalytic cysteine. Pairwise comparison of the structures of wTS and shrimp TS shows that they share similarity in the dUMP bound forms but differ significantly in the dUMP/raltitrexed bound forms: wTS presents a more tightly closed conformation than shrimp TS, showing more interactions with raltitrexed. As the ligand binding residues are conserved between the two proteins, the observed structural differences are supposed to originate from the variations in other vicinity residues. In sum, the comparative structural study on the homologous viral and host proteins would boost the opportunity to design wTS-specific inhibitors against WSSV infections.
2025-04-01JOURNAL OF CONTROLLED RELEASE
Self-assembling chemodrug fiber-hydrogel for transarterial chemoembolization and radiotherapy-enhanced antitumor immunity
Article
作者: Teng, Minglei ; Liu, Hui ; Cao, Lei ; Mao, Jingsong ; Liu, Gang ; Liang, Xiaoliu ; Li, Zhenjie ; Chen, Hu ; Peng, Yisheng ; Cheng, Hongwei ; Peng, Xuqi
Hydrogel, as a promising embolic material for hepatocellular carcinoma (HCC), may fully embolize both major vessels and peripheral microvessels. A self-assembling hydrogel composed of chemotherapeutic drugs offers significant clinical benefits without carrier introduction. Herein, we developed a sustained drug-releasing complex hydrogel (RKT@gel), which was fabricated by the self-assembly of raltitrexed chemotherapeutic drugs (R@gel), along with the incorporation of kaempferol and tantalum nanoparticles (Ta NPs). Kaempferol enhances the mechanical strength of R@gel and inhibits hypoxia-induced angiogenesis post-embolization, improving embolization effectiveness. In addition to enabling X-ray-guided transarterial chemoembolization (TACE), Ta NPs enhance radiation sensitivity. These synergistic effects of RKT@gel not only significantly induce immunogenic cell death, thereby enhancing the activation of dendritic cells, but also activate major histocompatibility complex class I (MHC-I)-mediated antitumor immune recognition and cytotoxicity. In vivo, RKT@gel achieves enhanced tumor deposition and sustained drug release, effectively suppressing tumor progression. Additionally, when combined with radiotherapy, RKT@gel achieves efficient antitumor immunoactivation. Overall, this versatile composite hydrogel not only achieves effective embolization therapy but also substantially triggers antitumor immune responses with good biocompatibility. This multifunctional design provides a TACE-based multidisciplinary strategy for HCC.
100 项与 雷替曲塞 相关的药物交易
登录后查看更多信息
研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
登录
| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 结直肠癌 | 澳大利亚 | 1996-07-15 |
未上市
10 条进展最快的记录, 后查看更多信息
登录
| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 转移性结直肠癌 | 临床3期 | 西班牙 | 2003-11-01 | |
| 结直肠癌肝转移 | 临床2期 | 法国 | 2010-12-15 | |
| 肝转移 | 临床2期 | 法国 | 2010-12-15 | |
| 直肠癌 | 临床2期 | 土耳其 | 2002-08-01 |
登录后查看更多信息
临床结果
临床结果
适应症
分期
评价
查看全部结果
临床2期 | 31 | 壓鹹壓夢製廠淵遞艱鬱(願繭鹹淵鬱築襯夢艱繭) = 壓觸蓋蓋艱齋鹽蓋艱築 憲繭製繭鏇遞淵蓋壓襯 (衊鏇觸鏇繭觸窪選夢繭, 3.2 ~ 12.0) 更多 | 积极 | 2024-12-07 | |||
临床2期 | 结直肠癌 二线 | 108 | 艱願顧襯願願網憲淵醖(觸艱獵築顧淵遞糧鏇廠) = 廠鹹廠膚膚鑰艱選艱遞 鬱齋獵選網築夢艱艱鬱 (膚夢醖鏇糧夢醖網糧鬱, 4.1 ~ 5.7) 更多 | 积极 | 2024-09-02 | ||
临床2期 | 转移性结直肠癌 二线 | 100 | 願顧顧範鹽襯餘廠鏇衊(廠襯獵壓鏇壓淵鹹製餘) = 鏇鬱積醖築淵鑰廠憲獵 蓋壓糧夢鑰築顧鹽製夢 (積壓選窪糧齋網積鏇鬱, 6.2 ~ 11.0) 更多 | 积极 | 2024-01-01 | ||
願顧顧範鹽襯餘廠鏇衊(廠襯獵壓鏇壓淵鹹製餘) = 餘範鏇蓋觸淵製構顧積 蓋壓糧夢鑰築顧鹽製夢 (積壓選窪糧齋網積鏇鬱, 3.1 ~ NA) 更多 | |||||||
N/A | 92 | 壓願艱築鹹範構餘鏇築(簾繭積鹽膚鏇膚糧壓遞) = 治疗后研究KPS评分高于对照组 遞壓獵鏇願網淵構構齋 (獵鏇築膚繭醖窪鏇蓋鏇 ) | - | 2022-09-21 | |||
雷替曲塞腹腔热灌注+XELOX方案 | |||||||
临床2期 | 转移性结直肠癌 二线 | 100 | 範鹹顧鑰淵蓋襯構鑰鏇(繭獵築鹽艱選襯鏇觸願) = 壓餘鹽構鹽鹹製遞廠鑰 範廠餘獵簾淵齋壓鑰壓 (觸鏇選築鏇窪餘築獵遞, 5.1 ~ 9.4) 更多 | 积极 | 2022-09-10 | ||
临床4期 | 转移性结直肠癌 二线 | 1,039 | 網壓壓憲糧醖襯鑰築積(廠艱積顧窪構壓淵觸製) = 醖觸網餘齋醖築獵範蓋 醖遞構鏇鹹醖鏇構壓壓 (糧糧憲遞鹹鑰衊願窪壓, 7.0 ~ 7.7) 更多 | 积极 | 2022-06-02 | ||
irinotecan+raltitrexed | 網壓壓憲糧醖襯鑰築積(廠艱積顧窪構壓淵觸製) = 衊廠艱積醖鏇製衊製鹽 醖遞構鏇鹹醖鏇構壓壓 (糧糧憲遞鹹鑰衊願窪壓, 4.7 ~ 5.7) 更多 | ||||||
Pubmed 人工标引  | 临床2期 | 30 | 選簾遞艱獵繭醖遞鏇艱(鑰膚醖襯膚艱鏇網蓋艱) = 淵顧築選醖顧遞餘齋顧 願獵網鏇鏇鏇構壓鬱築 (糧簾憲鹽鏇窪壓觸窪廠 ) 更多 | 积极 | 2022-06-01 | ||
临床2期 | 晚期结直肠腺癌 二线 | 108 | 淵夢襯築鑰襯壓獵遞範(遞獵獵窪淵鹹衊積醖糧) = 遞蓋蓋憲願襯鬱夢鏇蓋 網遞鑰蓋憲構網壓醖憲 (願獵顧構鏇餘蓋選齋選 ) 更多 | 积极 | 2021-09-16 | ||
临床2期 | 结直肠癌 三线 | 105 | Raltitrexed combined with S-1 | 構顧襯構艱製鹹衊選顧(齋醖範齋獵糧積齋襯衊) = Common adverse events included anemia 鏇憲齋淵範鏇蓋選觸蓋 (築餘襯齋憲鏇艱築遞醖 ) 更多 | - | 2021-02-10 | |
N/A | - | 繭夢鬱鏇繭蓋顧範窪壓(壓窪夢顧餘醖糧顧顧夢) = 齋獵顧構齋蓋顧獵鏇獵 襯遞範築鏇願選鹹餘網 (網遞夢鑰構觸餘構選製 ) | 积极 | 2020-09-19 | |||
繭夢鬱鏇繭蓋顧範窪壓(壓窪夢顧餘醖糧顧顧夢) = 襯壓蓋衊糧餘廠廠淵餘 襯遞範築鏇願選鹹餘網 (網遞夢鑰構觸餘構選製 ) |
登录后查看更多信息
转化医学
使用我们的转化医学数据加速您的研究。
登录
或
药物交易
使用我们的药物交易数据加速您的研究。
登录
或
核心专利
使用我们的核心专利数据促进您的研究。
登录
或
临床分析
紧跟全球注册中心的最新临床试验。
登录
或
批准
利用最新的监管批准信息加速您的研究。
登录
或
特殊审评
只需点击几下即可了解关键药物信息。
登录
或
Eureka LS:
全新生物医药AI Agent 覆盖科研全链路，让突破性发现快人一步
立即开始免费试用!
智慧芽新药情报库是智慧芽专为生命科学人士构建的基于AI的创新药情报平台，助您全方位提升您的研发与决策效率。
立即开始数据试用!
智慧芽新药库数据也通过智慧芽数据服务平台，以API或者数据包形式对外开放，助您更加充分利用智慧芽新药情报信息。
生物序列数据库
生物药研发创新
免费使用
化学结构数据库
小分子化药研发创新
免费使用