预约演示
更新于：2025-05-23
Eniluracil
恩尿嘧啶
更新于：2025-05-23
概要
基本信息
原研机构 |
最高研发阶段临床2期 |
首次获批日期- |
最高研发阶段(中国)- |
特殊审评孤儿药 (美国) |
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结构/序列
分子式C6H4N2O2 |
InChIKeyJOZGNYDSEBIJDH-UHFFFAOYSA-N |
CAS号59989-18-3 |
关联
13
项与 恩尿嘧啶 相关的临床试验NCT06568692
A Phase 2, Open-Label Study of PCS6422 With Capecitabine in Patients With Advanced or Metastatic Breast Cancer
NCT04861987
A Phase 1b Dose-escalation Study of the Safety and Pharmacokinetics of Fixed-dose PCS6422 with Escalating Doses of Capecitabine Administered Orally to Patients with Advanced, Refractory Gastrointestinal Tract Tumors
NCT01231802
A Comparative, Multicenter, Open-Label, Randomized, Phase 2 Study of the Safety and Antitumor Activity of Oral Eniluracil + 5 Fluorouracil + Leucovorin Versus Capecitabine Monotherapy in Subjects With Metastatic Breast Cancer
100 项与 恩尿嘧啶 相关的临床结果
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100 项与 恩尿嘧啶 相关的转化医学
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100 项与 恩尿嘧啶 相关的专利（医药）
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201
项与 恩尿嘧啶 相关的文献（医药）2025-02-01ESC Heart Failure
Eniluracil blocks AREG signalling‐induced pro‐inflammatory fibroblasts of melanoma in heart failure
Article
作者: Chen, Long ; Ran, Qin
Abstract:
Aims:
Heart failure (HF) is characterized by a heightened risk of melanoma, which often metastasizes to the heart. The overlap pathology between HF and melanoma includes chronic low‐grade inflammation and dysregulation of inflammatory cancer‐associated fibroblasts (iCAFs). The impact of HF on iCAF‐driven tumour inflammation remains obscure.
Methods and Results:
To identify critical genes for HF development, transcriptomic data (GSE57338) containing 313 clinical HF samples [136 healthy controls, 95 ischaemia (ISCH) and 82 dilated cardiomyopathy (DCM)] were analysed to screen differentially expressed genes (DEGs) and perform enrichment analysis. Fifty‐one DEGs in ISCH and 62 DEGs in DCM were identified with log2|fold change (FC)| ≥ 1 and P value ≤0.05. All these genes are involved in extracellular matrix organization, immune/inflammatory responses and Wnt signalling pathways. Then, the overall survival curves and prognostic models of DEGs in melanoma were evaluated. The correlation of gene expression with lymphocyte infiltration levels was assessed. Only aldehyde oxidase 1 (AOX1) and amphiregulin (AREG) maintained the same trend in melanoma as in HF, negatively affecting prognosis by regulating lymphocyte infiltration (log‐rank P value = 0.0017 and 0.0019). The potential drug molecules were screened, and the binding energies were calculated via molecular docking. Eniluracil, a known AOX1 targeting drug, was found to stably bind with AREG (hydrogen bond binding energies: −65.633, −63.592 and −62.813 kcal/mol).
Conclusions:
The increased prevalence of melanoma in HF patients and its propensity for cardiac metastasis may be due to AREG‐mediated systemic low‐grade inflammation. Eniluracil holds promise as a therapeutic agent that may block AREG signalling, inhibiting the activation of iCAF mediated by regulatory T cell (Treg) and neutrophil.
2024-12-01Sustainable Chemistry and Pharmacy
A silica gel-supported schiff base palladium nanocatalyst for sonogashira cross-coupling and synthesis of an anti-cancer chemotherapeutic agent
作者: Sarkar, Shaheen M. ; O'Reilly, Emmet J. ; Khan, Maksudur Rahman Md. ; Hasan, Kamrul ; Rahman, Lutfor Md
This work outlines the synthesis of a low-cost reusable silica gel-supported Schiff-base palladium nanocatalyst and its application in the synthesis of anti-cancer agent Eniuracil via the Sonogashira reaction.Silica gel was functionalized with amino containing silyl followed by the generation of a Schiff base through reaction with 1,10-phenanthroline-2,9-dicarboxaldehyde.Palladium was then coupled in the presence of hydrazine hydrate, resulting in the formation of the silica gel-supported Schiff-base palladium nanocatalys.Successful palladium incorporation was confirmed through Fourier-transform IR spectroscopy (FTIR) and X-ray diffraction (XRD) analyses.Scanning Electron Microscope (SEM) images revealed spherical silica gel particles and Transmission Electron Microscopy (TEM) anal. indicated an average palladium nanoparticle size of 5.92 ± 0.1 nm.The Inductively Coupled Plasma (ICP) and Energy Dispersive X-ray (EDX) data confirmed the anchoring of 0.27 mol% of palladium to the Schiff-base in the catalyst.The industrial efficacy of the catalysts is demonstrated through its application in carbon-to-carbon bond formation between aryl halides and aromatic alkyne via the Sonogashira reaction.Furthermore, the catalyst proved effective in the synthesis of the anti-cancer agent Eniuracil, a vital component in fluoropyrimidine-based chemotherapy.The catalyst exhibited reusability without significant loss of productivity.
2023-05-01JOURNAL OF MOLECULAR LIQUIDS
Adsorption of 40 low molecular weight drugs on pristine and fluorinated C60 fullerenes: Ab initio, statistical and neural networks analysis
作者: Kochaev, Alexey I. ; Maslov, Mikhail M. ; Grekova, Anastasiya A. ; Katin, Konstantin P. ; Bondarev, Nikolay V. ; Kaya, Savas ; Bauetdinov, Yusupbek A. ; Kalika, Elizaveta B.
Loading of 40 small drugs mols. with mol. weights in 47-210 g/mol range consisted of H, C, N, O, F, S elements on C60, C60F2 and C60F48 fullerenes are studied with the d. functional theory.Adsorption energies as well as deformation energies of fullerenes and drugs are calculatedThe C60F2 is recognized as the most active drugs adsorbent.Mean adsorption energies averaged over all considered drugs are 0.41, 0.59 and 0.54 eV with standard deviations of 0.10, 0.09 and 0.14 eV for C60, C60F2 and C60F48 fullerenes, resp.Mean energies of drug-induced deformations of C60, C60F2 and C60F48 are 8.6, 12.0 and 16.6 meV, resp.Multilinear regressions and neural networks were proposed for prediction of adsorption energies based on dipole moments and frontier MOs of the drugs.Achievable accuracy of such predictions is about 0.1 eV.Altretamine antibiotic is recognized as the notable drug possessing extremely high binding energies about 1 eV with fullerenes.IR spectral shifts due to its loading on fullerene carriers are calculated
45
项与 恩尿嘧啶 相关的新闻（医药）2024-10-14
临床结果上市批准临床2期抗体药物偶联物
100 项与 恩尿嘧啶 相关的药物交易
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研发状态
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 |
|---|---|---|---|---|
| 晚期结直肠腺癌 | 临床3期 | 美国 | 1999-04-01 | |
| 直肠腺癌 | 临床3期 | 美国 | 1999-04-01 | |
| 复发性结肠癌 | 临床3期 | 美国 | 1999-04-01 | |
| 结直肠癌 | 临床3期 | 美国 | - | |
| 结直肠癌 | 临床3期 | 英国 | - | |
| 胰腺癌 | 临床3期 | 英国 | - | |
| HER2 阴性乳腺癌 | 临床2期 | 美国 | 2024-10-02 | |
| 三阴性乳腺癌 | 临床2期 | 美国 | 2024-10-02 | |
| 转移性乳腺癌 | 临床2期 | 美国 | 2011-04-01 | |
| 转移性乳腺癌 | 临床2期 | 俄罗斯 | 2011-04-01 |
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临床结果
临床结果
适应症
分期
评价
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临床1期 | 12 | 齋艱選膚遞鏇廠襯顧齋(鏇選構夢顧積壓獵襯夢) = 艱觸衊窪築齋淵窪餘鹹 廠鏇醖襯遞衊築鬱夢膚 (構淵築壓廠願鏇選積襯 ) 更多 | 积极 | 2024-06-11 | |||
AACR2024 人工标引  | 临床1期 | 18 | NGC-Cap (150 mg bid) | 膚鬱齋積遞願選鬱齋繭(願網壓淵壓襯構襯夢鹹) = 糧窪遞夢範獵淵製鏇鑰 網餘構醖淵餘夢淵選鹹 (餘淵觸網鬱鹹範醖夢獵, 23) 更多 | 积极 | 2024-04-05 | |
NGC-Cap (225 mg bid) | 膚鬱齋積遞願選鬱齋繭(願網壓淵壓襯構襯夢鹹) = 鏇獵範襯壓壓夢觸憲鹹 網餘構醖淵餘夢淵選鹹 (餘淵觸網鬱鹹範醖夢獵, 37) 更多 | ||||||
临床1期 | - | 窪艱鹹憲獵獵鬱鬱積壓(網憲築鏇鹹簾網鏇蓋膚) = the side effect profile for 5-FU exposures from NGC-Cap had a similar anabolite side effect profile to FDA-approved capecitabine.
In addition, the side effects associated with FBAL (fluoro-beta-alanine, the primary catabolite formed from the metabolism of 5-FU), such as hand-foot syndrome, that can lead to capecitabine intolerance, were almost non-existent, likely because FBAL exposure was approximately 1% of the exposure seen after FDA-approved capecitabine administration. 鏇觸壓鏇鏇蓋觸蓋衊憲 (艱淵膚製廠積獵淵壓選 ) | 积极 | 2023-12-19 | |||
临床1期 | 5 | 餘鏇築餘範願遞繭夢醖(鹹製範選繭艱願壓壓築) = 齋壓艱簾遞餘鹹醖壓鹽 製膚蓋範糧膚餘壓網廠 (夢獵鏇醖築選蓋顧糧鹽, 11) | - | 2007-06-20 | |||
临床2期 | 75 | 夢製製製鹽網夢襯製廠(築糧觸憲衊醖鑰鹹鹽夢) = 齋鹹醖夢夢窪鏇齋膚膚 鏇糧艱獵願鹽窪衊艱齋 (選鏇鬱醖餘網鏇選廠鹹 ) | 不佳 | 2002-11-01 |
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