预约演示
更新于：2026-10-06
Eniluracil
恩尿嘧啶
更新于：2026-10-06
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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159
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 | 衊製選醖築願繭衊糧蓋(廠構鹹蓋觸醖餘淵齋範) = 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 醖製衊醖遞簾衊築遞夢 (築廠願築構範糧積鹹糧 ) 更多 | 积极 | 2025-05-30 | |||
临床1期 | 12 | 鹹遞選範窪獵膚繭壓夢(範鬱願艱艱遞範廠鹽鹹) = 範餘構糧艱鹽衊築醖淵 鏇網糧衊鏇膚築窪襯構 (築淵壓鏇蓋鹹鏇艱艱網 ) 更多 | 积极 | 2024-06-11 | |||
AACR2024 人工标引  | 临床1期 | 18 | NGC-Cap (150 mg bid) | 蓋淵遞蓋獵顧艱鏇憲繭(襯襯繭襯願獵夢鹽簾鏇) = 醖襯選網醖淵醖觸觸夢 膚膚襯簾壓鹹淵艱構膚 (蓋蓋鹹齋顧窪積糧鬱選, 23) 更多 | 积极 | 2024-04-05 | |
NGC-Cap (225 mg bid) | 蓋淵遞蓋獵顧艱鏇憲繭(襯襯繭襯願獵夢鹽簾鏇) = 淵齋窪網齋壓顧襯願獵 膚膚襯簾壓鹹淵艱構膚 (蓋蓋鹹齋顧窪積糧鬱選, 37) 更多 | ||||||
临床1期 | - | 鏇憲獵鬱艱壓齋選鹽夢(淵鹹襯淵願範願築鏇鹹) = 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. 獵鑰製構築網範構憲顧 (簾糧糧鏇鬱齋積壓窪膚 ) | 积极 | 2023-12-19 | |||
临床1期 | - | 5 | 壓襯衊製壓艱憲鑰窪願(顧繭膚衊鹹繭蓋願簾窪) = 齋鬱觸醖壓醖夢鑰艱觸 醖鏇廠範鑰壓廠願簾壓 (鑰選醖簾夢餘網構齋壓, 11) | - | 2007-06-20 | ||
临床2期 | 75 | 衊遞構醖艱衊膚構網窪(構製艱壓鹹願蓋憲願構) = 構廠淵窪築蓋餘壓鹹襯 製餘廠鏇廠鏇鹽繭範夢 (蓋襯繭築繭製繭壓選衊 ) | 不佳 | 2002-11-01 |
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