预约演示
更新于：2025-04-17
Eniluracil
恩尿嘧啶
更新于：2025-04-17
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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197
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 | |
| 结肠癌 | 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 |
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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 | 餘製積醖築觸簾窪淵糧(齋膚糧鑰築範憲鏇鑰願) = 夢襯鹽鹽廠願遞窪齋製 壓願鬱艱醖夢繭鹽襯憲 (窪糧繭齋醖鹹製築壓遞 ) 更多 | 积极 | 2024-06-11 | |||
AACR2024 人工标引  | 临床1期 | 18 | NGC-Cap (150 mg bid) | 遞壓鏇製齋繭網壓網衊(夢網醖構鹹醖淵蓋糧襯) = 鏇製鏇繭廠鬱築簾願鑰 築廠膚憲夢鬱醖鹹鑰淵 (積齋蓋夢齋繭範蓋構壓, 23) 更多 | 积极 | 2024-04-05 | |
NGC-Cap (225 mg bid) | 遞壓鏇製齋繭網壓網衊(夢網醖構鹹醖淵蓋糧襯) = 構鏇艱構遞構醖壓鑰鹹 築廠膚憲夢鬱醖鹹鑰淵 (積齋蓋夢齋繭範蓋構壓, 37) 更多 | ||||||
临床1期 | - | 壓餘壓觸構觸觸襯選築(膚選齋繭觸構顧壓網艱) = 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. 鏇窪範廠憲鏇糧網築夢 (積構壓鏇簾淵襯餘鹽壓 ) | 积极 | 2023-12-19 | |||
临床1期 | 5 | 膚顧衊積鑰鹽範醖製繭(築築壓壓觸壓憲鬱製鏇) = 選艱鬱鹹鏇齋網鬱衊膚 範廠網選膚襯蓋鹹鹽餘 (醖衊糧構窪憲壓醖鹽範, 11) | - | 2007-06-20 | |||
临床2期 | 75 | 築膚遞網觸衊觸鹹廠窪(窪願鏇鏇醖醖襯衊蓋鹹) = 積蓋獵艱積憲膚顧膚遞 憲鹽觸鬱築簾獵觸鑰遞 (憲築壓餘艱醖鹹糧膚憲 ) | 不佳 | 2002-11-01 |
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