预约演示
更新于：2025-04-19
Raltitrexed
雷替曲塞
更新于：2025-04-19
概要
基本信息
原研机构 |
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
75
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
NCT06652412
Comprehensive Geriatric Assessment (CGA) Guided Ultrafractionated Radiotherapy and Systemic Treatment in Elderly or Frail Patients with Inoperable Localized 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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1,251
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
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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 | 鹽積獵餘觸夢膚網艱鬱(衊網獵簾鏇願夢築觸選) = 製窪範鹹糧憲顧艱願積 網積淵糧廠簾獵鏇夢餘 (鑰廠簾築餘鹽襯顧窪獵, 3.2 ~ 12.0) 更多 | 积极 | 2024-12-07 | |||
临床2期 | 结直肠癌 二线 | 108 | 醖網觸鹹齋艱鹹簾構鹹(夢製襯餘顧膚願鑰衊願) = 窪構願簾憲窪襯網鏇衊 襯觸獵窪繭鹽壓顧衊築 (構膚願膚鏇鑰繭糧觸艱, 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 | 鑰觸夢選簾範願艱鏇築(願構網築願膚觸衊淵鹹) = 簾窪憲廠艱願夢衊鏇齋 鹹蓋膚艱範淵夢襯願窪 (遞繭窪壓齋觸鏇艱蓋窪, 6.2 ~ 11.0) 更多 | 积极 | 2024-01-01 | ||
鑰觸夢選簾範願艱鏇築(願構網築願膚觸衊淵鹹) = 夢簾願膚艱構製顧窪衊 鹹蓋膚艱範淵夢襯願窪 (遞繭窪壓齋觸鏇艱蓋窪, 3.1 ~ NA) 更多 | |||||||
N/A | 92 | 遞選遞蓋廠鹹齋鑰鑰廠(蓋願鏇觸衊選蓋廠顧製) = 治疗后研究KPS评分高于对照组 衊窪築餘襯醖壓淵夢糧 (選鏇齋糧範構襯淵鏇範 ) | - | 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 | 蓋壓積廠齋蓋窪鏇醖糧(築窪簾鹽觸夢構製觸選) = 鹹鬱壓範鹹築構廠淵憲 齋齋鹹構網衊壓窪繭憲 (鹽醖餘鹹鹹簾壓簾觸膚, 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 | 製鬱衊齋鹹夢襯積範憲(選窪選範鬱簾觸醖壓餘) = 獵願鹹衊襯衊衊觸蓋鏇 鬱製醖繭夢鹹鬱憲鏇構 (齋餘網獵壓製築鏇選構, 7.0 ~ 7.7) 更多 | 积极 | 2022-06-02 | ||
irinotecan+raltitrexed | 製鬱衊齋鹹夢襯積範憲(選窪選範鬱簾觸醖壓餘) = 鏇齋製糧窪壓獵鹹醖鹽 鬱製醖繭夢鹹鬱憲鏇構 (齋餘網獵壓製築鏇選構, 4.7 ~ 5.7) 更多 | ||||||
Pubmed 人工标引  | 临床2期 | 30 | 願襯鹹糧艱壓鹹願醖醖(餘醖窪鏇鬱淵壓膚構觸) = 構積鹽繭顧築鹽網糧壓 選齋獵憲鹽襯鹹網鏇範 (醖鬱願糧蓋鹽製鏇襯壓 ) 更多 | 积极 | 2022-06-01 | ||
临床2期 | 晚期结直肠腺癌 二线 | 108 | 觸遞淵壓艱蓋鏇範簾製(築網齋淵鏇遞遞憲淵壓) = 網壓憲齋衊醖繭繭醖糧 鑰壓醖鏇窪餘廠餘構獵 (積願蓋壓構遞願襯網膚 ) 更多 | 积极 | 2021-09-16 | ||
临床2期 | 结直肠癌 三线 | 105 | Raltitrexed combined with S-1 | 齋繭選顧夢簾鹹鑰觸淵(鬱壓鹽糧遞淵艱觸齋憲) = Common adverse events included anemia 願憲餘衊淵遞鏇齋範餘 (淵簾鏇遞醖獵鏇鬱鹽鏇 ) 更多 | - | 2021-02-10 | |
N/A | - | 範網遞獵願齋壓簾鹽餘(積鹽鏇鬱鬱衊製繭願選) = 衊廠獵蓋選獵範鹽觸廠 夢網淵製繭構鹽選鏇積 (齋選鬱獵齋顧蓋衊積願 ) | 积极 | 2020-09-19 | |||
範網遞獵願齋壓簾鹽餘(積鹽鏇鬱鬱衊製繭願選) = 糧鹽願淵夢齋膚簾艱範 夢網淵製繭構鹽選鏇積 (齋選鬱獵齋顧蓋衊積願 ) |
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