预约演示
更新于：2026-10-23
Eniluracil
恩尿嘧啶
更新于：2026-10-23
概要
基本信息
原研机构 |
最高研发阶段临床1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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162
项与 恩尿嘧啶 相关的文献（医药）2026-08-01Journal for ImmunoTherapy of Cancer
Dihydropyrimidine dehydrogenase modulates immune response to checkpoint inhibition in mismatch repair deficient/microsatellite instability-high colorectal cancer
Article
作者: Ashouri, Karam ; Smbatyan, Goar ; Soni, Shivani ; Battaglin, Francesca ; Zhang, Yong ; Lenz, Heinz-Josef ; Soto Trujillo, Steve ; Algaze, Sandra ; Zhang, Lin ; Jayachandran, Priya ; Cerma, Krisida ; Baugh, Aaron G ; Yang, Yan ; Mittal, Pooja ; Ho Lo, Jae ; Kay, Steve A ; Gonzalez, Edgar ; K Singh, Indrakant ; Zhang, Wu ; Castanon, Sofi ; Bergamo, Francesca ; Lonardi, Sara ; Millstein, Joshua ; Yu, Jian ; Torres Gonzalez, Lesly ; T Roussos Torres, Evanthia
Background:
Treatment with immune checkpoint inhibitors (ICIs) has radically improved outcomes for patients with microsatellite instability-high (MSI-H) metastatic colorectal cancer (mCRC). Intrinsic and acquired resistance, however, remains an important concern. Pyrimidine pathway regulates the innate immune response and may offer an opportunity to enhance ICI efficacy via modulation of pyrimidine metabolism. Identification of primary, adaptive and acquired resistance mechanisms and development of actionable strategies to overcome resistance and expand the benefit of ICI is paramount. Our group is the first to show that the dihydropyrimidine dehydrogenase (DPD; gene
DPYD
) metabolic pathway predicts the efficacy of ICI in MSI-H tumors.
Methods:
Retrospective analysis of germline single nucleotide polymorphisms was done in patients with MSI-H CRC cohort (Veneto Institute of Oncology; OIOV-IRCCS, Padua, Italy) treated with immunotherapy.
Dpyd
knockout or overexpressed MC38 MSI-H syngeneic mice models were treated with anti-programmed cell death protein 1 (PD-1) and anti-cytotoxic T-lymphocyte associated protein 4 (CTLA-4) alone or in combination and their effect on tumor growth and its microenvironment was studied.
Results:
In our real-world data analysis, genetic variants in
DPYD
were associated with progression-free survival and tumor response in patients with MSI-H mCRC treated with ICI. In preclinical studies, complete tumor elimination was observed in 100% of mice bearing
Dpyd
knockout tumors treated with a combination of anti-PD-1 and anti-CTLA-4, further validated by pharmacologically inhibiting DPD using eniluracil.
Conclusion:
Our results showed that the pyrimidine pathway has a strong association with immunotherapy treatment response in CRC. These findings may support the development of novel treatment strategies exploiting DPD inhibition in MSI-H tumors and their quick integration into clinic.
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: Yusupbek A. Bauetdinov ; Mikhail M. Maslov ; Konstantin P. Katin ; Elizaveta B. Kalika ; Anastasiya A. Grekova ; Nikolay V. Bondarev ; Alexey I. Kochaev ; Savas Kaya
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
56
项与 恩尿嘧啶 相关的新闻（医药）2026-03-18
·上海起发
CSCO会议诊断试剂临床研究
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
查看全部结果
临床1期 | 18 | 衊選壓糧繭構鹽鹽糧齋(願顧艱蓋鬱憲窪膚製繭) = 36.4% of the patients in the 150 mg BID and 225 mg BID cohorts had grade 3-4 adverse events (AEs) associated with anabolites, similar to the incidence reported for Mono-Cap 蓋夢衊糧鑰顧鑰繭襯鏇 (壓製膚淵鹹淵夢鬱網遞 ) 更多 | 积极 | 2025-05-30 | |||
临床1期 | 12 | 淵顧獵蓋壓築艱鑰夢繭(窪醖夢憲遞選壓艱鑰繭) = 醖淵壓衊襯簾廠積範簾 糧顧鏇餘蓋糧簾餘願襯 (廠廠獵製鏇鏇蓋遞鬱觸 ) 更多 | 积极 | 2024-06-11 | |||
AACR2024 人工标引  | 临床1期 | 18 | NGC-Cap (150 mg bid) | 夢齋選憲願夢淵蓋鑰餘(糧憲窪遞網艱積鑰鹹範) = 艱醖壓選鏇選鹽廠襯餘 鬱窪簾範餘鏇製築廠製 (鹹遞遞鹹獵築衊簾選顧, 23) 更多 | 积极 | 2024-04-05 | |
NGC-Cap (225 mg bid) | 夢齋選憲願夢淵蓋鑰餘(糧憲窪遞網艱積鑰鹹範) = 鹽願鬱衊鏇觸膚鬱簾繭 鬱窪簾範餘鏇製築廠製 (鹹遞遞鹹獵築衊簾選顧, 37) 更多 | ||||||
临床1期 | - | 襯獵繭觸鹽蓋鹹齋鹽簾(鹹選繭願膚範淵觸醖窪) = 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. 簾築餘襯簾艱襯襯餘願 (願築淵膚鬱窪簾淵遞膚 ) | 积极 | 2023-12-19 | |||
临床1期 | - | 5 | 膚積積遞觸顧鬱繭壓膚(艱淵鬱鹽鏇範糧觸膚淵) = 窪蓋鏇餘鹹衊遞獵構廠 蓋糧醖顧蓋夢膚顧夢廠 (鏇鑰壓獵繭鹹製繭鏇窪, 11) | - | 2007-06-20 | ||
临床2期 | 75 | 範襯網觸鏇鏇鬱遞鏇壓(廠壓蓋艱淵築鏇構夢蓋) = 繭築壓鏇繭網鹽廠顧網 遞艱鬱憲壓遞憲構鏇齋 (醖遞齋鏇顧願淵構窪顧 ) | 不佳 | 2002-11-01 |
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