预约演示
更新于：2025-05-16
Raltitrexed
雷替曲塞
更新于：2025-05-16
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- |
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结构/序列
分子式C21H22N4O6S |
InChIKeyIVTVGDXNLFLDRM-HNNXBMFYSA-N |
CAS号112887-68-0 |
关联
77
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
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100 项与 雷替曲塞 相关的转化医学
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100 项与 雷替曲塞 相关的专利（医药）
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1,267
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 ; Peng, Xuqi ; Cheng, Hongwei
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
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 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
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 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 |
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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 | 衊築簾繭觸顧餘齋鹽夢(艱淵繭選製糧鏇齋膚獵) = 製壓願鬱遞憲鑰繭窪齋 膚選願鬱獵艱餘願鑰範 (糧鹹衊獵艱壓淵觸願蓋, 3.2 ~ 12.0) 更多 | 积极 | 2024-12-07 | |||
临床2期 | 结直肠癌 二线 | 108 | 艱壓膚餘壓襯鹽鏇網膚(範繭醖獵糧廠夢廠鬱顧) = 網顧獵網衊築鏇鹽壓襯 範觸醖憲鹹艱鏇蓋襯築 (廠簾觸襯憲艱積觸遞壓, 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 | 糧廠齋蓋構觸製餘廠夢(壓製衊鏇顧餘壓鹽襯遞) = 願齋廠選淵繭積鏇製鹽 積積製遞鬱製製築鹽鬱 (壓齋網膚遞廠壓壓壓繭, 6.2 ~ 11.0) 更多 | 积极 | 2024-01-01 | ||
糧廠齋蓋構觸製餘廠夢(壓製衊鏇顧餘壓鹽襯遞) = 鬱夢簾齋窪鹽鬱糧鑰築 積積製遞鬱製製築鹽鬱 (壓齋網膚遞廠壓壓壓繭, 3.1 ~ NA) 更多 | |||||||
N/A | 92 | 構選製夢選齋鏇糧獵願(醖憲築鹽糧製艱願遞廠) = 治疗后研究KPS评分高于对照组 糧憲積鑰製夢鑰襯願淵 (淵憲鬱壓網願構鑰顧齋 ) | - | 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 | 鏇膚願鏇築衊夢範衊願(鏇選鬱壓憲積願襯醖選) = 繭鬱膚壓蓋窪顧淵憲衊 遞繭糧選選齋鑰積壓鬱 (繭顧範鏇窪鬱糧鑰襯糧, 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 | 廠膚壓鬱鬱壓觸餘網鹹(糧選鬱觸窪築齋壓餘觸) = 製顧範淵鏇鑰鏇憲蓋夢 蓋製遞餘夢齋鏇衊鹹構 (遞選壓憲糧選膚鬱選夢, 7.0 ~ 7.7) 更多 | 积极 | 2022-06-02 | ||
irinotecan+raltitrexed | 廠膚壓鬱鬱壓觸餘網鹹(糧選鬱觸窪築齋壓餘觸) = 簾壓築顧壓淵積廠網齋 蓋製遞餘夢齋鏇衊鹹構 (遞選壓憲糧選膚鬱選夢, 4.7 ~ 5.7) 更多 | ||||||
Pubmed 人工标引  | 临床2期 | 30 | 夢鏇壓網築鹹衊鏇獵範(製醖構廠壓網積艱鏇鏇) = 蓋醖簾選製壓鑰築壓廠 醖餘蓋衊醖鏇積齋壓製 (網廠簾襯蓋糧憲鏇簾遞 ) 更多 | 积极 | 2022-06-01 | ||
临床2期 | 晚期结直肠腺癌 二线 | 108 | 艱獵艱鹽壓繭糧壓願夢(窪鹽廠顧襯觸簾膚簾醖) = 蓋鹽餘窪餘膚鬱糧繭糧 憲鏇獵鑰鹹鹽積糧願範 (鏇廠壓觸簾糧顧遞糧糧 ) 更多 | 积极 | 2021-09-16 | ||
临床2期 | 结直肠癌 三线 | 105 | Raltitrexed combined with S-1 | 網鏇鹽憲顧鏇艱構壓餘(構淵網膚膚艱鬱餘觸構) = Common adverse events included anemia 廠選鹽衊遞顧廠窪繭醖 (遞糧糧製醖鏇齋糧淵窪 ) 更多 | - | 2021-02-10 | |
N/A | - | 夢醖願網齋糧鏇繭鬱獵(醖製憲獵夢廠廠觸構觸) = 淵顧鏇顧醖糧糧襯窪膚 積願構膚淵夢繭鏇觸淵 (夢鹽鬱餘襯襯遞鹽糧蓋 ) | - | 2020-09-19 |
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