This is an adaptive Phase 2, open-label, randomized, multi-center study evaluating up to 2 regimens of PCS6422 with capecitabine (Cap) vs. standard dose of Cap alone in patients with advanced or metastatic breast cancer. The goal of the study is to assess the efficacy and safety of PCS6422 + Cap as a treatment option for patients with advanced or metastatic breast cancer who are not eligible for anthracycline- or taxane-containing therapies, or other available therapies, including PD-1 or PARP inhibitors.

开始日期2024-10-02

申办/合作机构

Processa Pharmaceuticals, Inc.

NCT04861987

/ Completed临床1期

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

This study is an open label, multicenter study in patients who have advanced, relapsed refractory GI cancer or are not relapsed/refractory but are intolerant to other therapies who, in the judgment of investigators, are candidates for fluoropyrimidine monotherapy.

开始日期2021-06-18

申办/合作机构

Processa Pharmaceuticals, Inc.

NCT01231802

/ Unknown status临床2期

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

The purpose of the study is to determine if eniluracil/5-FU/leucovorin in metastatic breast cancer (MBC) may have efficacy and tolerability advantages over capecitabine monotherapy.

开始日期2011-04-01

申办/合作机构

Fennec Pharmaceuticals, Inc.

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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176

项与恩尿嘧啶相关的文献（医药）

2025-02-01·ESC 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.

2024-12-01·Sustainable 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.

2023-05-01·JOURNAL 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 ; Kalika, Elizaveta B. ; Bauetdinov, Yusupbek A.

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

项与恩尿嘧啶相关的新闻（医药）

2025-07-09

·生物制药小编

没钱实现里程碑，公司选择退货

近日，Processa Pharmaceuticals公司宣布终止了与Opus Genetics的合作协议，将其PCS3117的开发权益退还给Opus。关于终止合作，Processa给出的原因是其认为将PCS3117推进到一个关键里程碑所需的时间和成本太高了。目前，PCS3117已经完成了Ⅱa期临床试验。在2021年6月，双方达成了合作协议，Processa获得了PCS3117中国以外开发和商业化的全球独家权益。PCS3117是Processa开发的一种下一代Gemcitabine（吉西他滨），旨在通过改变吉西他滨或其活性代谢物的代谢、分布或消除方式，同时保持药物杀死癌细胞的机制。就其财务情况看来，Processa选择终止合作算是在情理之中。据公司2025年第一季度财报，截止2025年3月31日，公司的现金及现金等价物仅为289.71万美元。就公司目前的财务状况，难以支持推进PCS3117后续的临床试验，况且，真的达到了，可能也无法支付Opus里程碑款项。今年1月，Processa还通过公开募股筹集了440万美元，当时公司预计可以支持运营到2025年中期。在今年一季度财报告会中，公司尚有PCS6422、PCS499、PCS12852、PCS11T、PCS3117等5条管线相关进展介绍，但是现在公司官网中，研发管线这一栏包括PCS3117在内，只剩三条管线了。PCS499已经应该是已经被放弃了，Processa在一季度财报中曾披露，将专门成立一个子公司来对PCS499进行下一步开发，但是就公司的资金状况看来，这一目标，很难实现。PCS499主要被开发用于治疗脂性渐进性坏死，此前已经完成了Ⅱ期临床试验。PCS12852已经被授权出去了。今年6月，公司就PCS12852与Intact Therapeutics达成合作协议，交易总额为4.55亿美元，包括一笔250万美元的近期付款、2000万美元开发和监管里程碑付款，4.325亿美元商业里程碑付款，以及销售分成。PCS12852为Processa 2020年自Yuhan公司引进而来，是一款高选择性5-HT4受体激动剂，被开发用于治疗胃轻瘫等胃肠道疾病，已完成的Ⅱa期临床试验。此次退货后，只剩下CS6422和PCS11T了。PCS6422是Processa目前最主要的管线，一种口服二氢嘧与啶脱氢酶（DPD）抑制剂，是其2020年从Elion Oncology授权引进而来。目前PCS6422正在转移性乳腺癌Ⅱ期临床试验，与卡培他滨联用，公司预计2025年下半年分享初步数据。PCS11T是一种伊立替康（Irinotecan）前药，也是引进的，2020年6月，Processa自Aposense公司引进，目前尚处于临床前阶段。即便是为了推进这两条管线的后续的开发，仍需公司尽快进行额外融资。参考出处：https://www.globenewswire.com/news-release/2025/07/01/3108392/0/en/Processa-Pharmaceuticals-Provides-Portfolio-and-Business-Update.htmlhttps://www.fiercebiotech.com/biotech/processa-peters-out-hands-licensed-cancer-candidate-back-opus-geneticshttps://www.processapharmaceuticals.com/investors/sec-filings/all-sec-filings/content/0001641172-25-009252/0001641172-25-009252.pdfhttps://www.processapharmaceuticals.com/news-media/press-releases/detail/137/processa-pharmaceuticals-signs-binding-term-sheet-granting

财报引进/卖出临床2期临床1期

2025-07-01

·GlobeNewswire-Health Care

Processa Pharmaceuticals Provides Portfolio and Business Update

Signed binding term sheet granting Intact Therapeutics an exclusive option to license PCS12852Continue enrolling patients in Phase 2 study of PCS6422Strengthened balance sheet with $7M capital infusion VERO BEACH, Fla., July 01, 2025 (GLOBE NEWSWIRE) -- Processa Pharmaceuticals, Inc. (Nasdaq: PCSA), a clinical-stage pharmaceutical company developing next-generation cancer therapies, provides updates on its product pipeline, upcoming milestones and business activities. “We are taking deliberate steps to focus our resources on programs with the highest potential for clinical success and commercial impact,” said Dr. David Young, President Research and Development at Processa. “Our approach continues to center on developing safer, more effective treatments for cancer while creating value through strategic business development and disciplined pipeline management.” “Our NGC-Cap Phase 2 clinical trial in metastatic breast cancer is actively enrolling patients. We continue to anticipate sharing initial data in the second half of 2025,” said George Ng, Chief Executive Officer of Processa Pharmaceuticals. “The streamlining of our development pipeline, signing of strategic partnerships, and optimizing our capital allocation, enable us to make the necessary investments in our science in order to enhance shareholder value.” Key Portfolio Updates: PCS6422 (NGC-Cap): PCS6422, Processa’s lead oncology asset in combination with capecitabine (NGC-Cap), is actively enrolling patients in a Phase 2 study for metastatic breast cancer. The program remains a top priority, with the remaining patients needed for the pre-planned interim analysis expected to be enrolled in the second half of 2025. The trial builds on compelling safety and efficacy signals observed in earlier studies, including improved tolerability and increased exposure to active cancer-killing metabolites.PCS499: Based on preliminary positive results in kidney disease and the FDA allowing surrogate endpoints to now be used in rare kidney diseases, Processa is currently designing a new adaptive pivotal PCS499 Phase III study to discuss with the FDA later this year. In addition, Processa is establishing a dedicated subsidiary to hold PCS499. The move is intended to enhance strategic flexibility in targeting capital raising and potential partnership exploration after meeting with the FDA. PCS12852: As previously announced, Processa has signed a binding term sheet with Intact Therapeutics, Inc. granting an exclusive option to license PCS12852 for gastroparesis and related gastrointestinal motility disorders. Under the terms, Processa is eligible for up to $454 million in milestone payments, a 12% royalty on future sales, and a 3.5% equity stake in Intact. The partnership represents a strategic monetization of non-core assets while maintaining upside potential.PCS11T: PCS11T is Processa’s preclinical oncology asset based on the active metabolite of irinotecan. The company continues to define and explore preclinical and clinical development strategies as well as opportunities to support future development.PCS3117: After determining that the time and cost required to advance PCS3117 to a meaningful milestone would be too high, Processa has terminated the license agreement for PCS3117 and returning the rights to the original licensor. Commitment to Shareholder Value These portfolio changes align with Processa’s strategic intent to focus on oncology assets with strong differentiation, scientific rationale, commercial opportunity and clear regulatory pathways. The company believes this will optimize our human and capital resources, expedite the unlocking of hidden asset value through partnerships, and position the organization to deliver long-term shareholder returns. Investor Webinar Processa CEO George Ng will participate in a live investor webinar on Wednesday, July 9, 2025, at 4:15 p.m. ET to discuss the company’s strategic pipeline realignment and value-creating milestones. To register for the free webinar, please visit: https://www.redchip.com/webinar/PCSA/85765532754 Questions can be pre-submitted to PCSA@redchip.com or online during the live event. About Processa Pharmaceuticals, Inc. Processa is a clinical-stage pharmaceutical company focused on developing the Next Generation Cancer (NGC) drugs with improved safety and efficacy. Processa’s NGC drugs are modifications of existing FDA-approved oncology therapies resulting in an alteration of the metabolism and/or distribution of these drugs while maintaining the existing mechanisms of killing the cancer cells. By combining its novel oncology pipeline with proven cancer-killing active molecules and its Regulatory Science Approach, Processa’s strategy is to develop more effective therapy options with improved tolerability for cancer patients through an efficient regulatory path. In addition to its core oncology programs, Processa is actively pursuing strategic partnerships for non-oncology assets to unlock additional value For more information, visit our website at www.processapharma.com. Forward-Looking Statements This release contains forward-looking statements. The statements in this press release that are not purely historical are forward-looking statements which involve risks and uncertainties. Actual future performance outcomes and results may differ materially from those expressed in forward-looking statements. Please refer to the documents filed by Processa Pharmaceuticals with the SEC, specifically the most recent reports on Forms 10-K and 10-Q, which identify important risk factors which could cause actual results to differ from those contained in the forward-looking statements. Company Contact:Patrick Lin(925) 683-3218plin@processapharma.com Investor Relations:Dave GentryRedChip Companies, Inc.1-407-644-4256PCSA@redchip.com

引进/卖出临床2期临床3期

2025-05-30

·GlobeNewswire-Health Care

Processa Pharmaceuticals Announces Presentation and Publication of Three Abstracts at 2025 ASCO Annual Meeting

HANOVER, Md., May 30, 2025 (GLOBE NEWSWIRE) -- Processa Pharmaceuticals, Inc. (Nasdaq: PCSA), a clinical-stage pharmaceutical company focused on developing the next generation cancer therapies with improved efficacy and safety, today announced the acceptance of three abstracts for the 2025 American Society of Clinical Oncology (ASCO) Annual Meeting, taking place May 30 to June 3, 2025, at McCormick Place in Chicago, Illinois. The abstracts highlight Processa’s pipeline of Next Generation Cancer (NGC) drug candidates, including PCS6422 (NGC-Cap) and PCS11T (NGC-Iri), showcasing both preclinical and clinical advances. Trials in Progress Poster Presentation and Abstract Publication Abstract Title: Adaptive Designed Eniluracil + Capecitabine Phase 2 Trial in Advanced or Metastatic Breast Cancer PatientsAbstract Number: TPS1133 | Poster Board Number: 105bSession Title: Breast Cancer—MetastaticDate & Time: June 2, 2025 | 9:00 AM–12:00 PM CDTDr. David Young, Founder and President of Research & Development at Processa, will be presenting an overview of Processa’s ongoing Phase 2 adaptive design trial evaluating the safety and efficacy of PCS6422 (eniluracil) combined with capecitabine in patients with advanced or metastatic breast cancer. The study explores optimal dosing regimens and a personalized medicine approach to improve outcomes and tolerability. Abstract Publications 1. Abstract Title: Safety and Efficacy of Eniluracil + Capecitabine (6422 + Cap) in Phase 1b Trial Abstract Number: e15152 This online-only abstract provides data from the Phase 1b study that defined the Maximum Tolerated Dose (MTD) and Recommended Phase 2 Dose Range (RP2DR) for NGC-Cap (eniluracil + capecitabine or 6422 + Cap), highlighting its improved safety profile and anti-tumor activity compared to standard capecitabine. 2. Abstract Title: Preclinical Project Optimus Dose Escalation of SN-38 Pro-Drug PCS11T Abstract Number: e15023 This online-only abstract outlines a Project Optimus-aligned approach to define the optimal therapeutic window of PCS11T, a tumor-targeted pro-drug of SN-38. PCS11T is designed to increase drug concentration in tumors while reducing systemic toxicity. “These ASCO presentations and publications reflect the breadth of our oncology pipeline and the progress we’re making across multiple programs,” said Dr. David Young. “From our Phase 2 clinical program in metastatic breast cancer to preclinical innovations with PCS11T, we are leveraging our Regulatory Science Approach and deep oncology expertise to address critical unmet needs.” About Processa Pharmaceuticals, Inc. Processa is a clinical-stage pharmaceutical company focused on developing the Next Generation Cancer (NGC) drugs with improved safety and efficacy. Processa’s NGC drugs are modifications of existing FDA-approved oncology therapies resulting in an alteration of the metabolism and/or distribution of these drugs while maintaining the existing mechanisms of killing the cancer cells. By combining its novel oncology pipeline with proven cancer-killing active molecules and its Regulatory Science Approach, Processa’s strategy is to develop more effective therapy options with improved tolerability for cancer patients through an efficient regulatory path. For more information, visit our website at www.processapharma.com. Forward-Looking Statements This release contains forward-looking statements. The statements in this press release that are not purely historical are forward-looking statements which involve risks and uncertainties. Actual future performance outcomes and results may differ materially from those expressed in forward-looking statements. Please refer to the documents filed by Processa Pharmaceuticals with the SEC, specifically the most recent reports on Forms 10-K and 10-Q, which identify important risk factors which could cause actual results to differ from those contained in the forward-looking statements. Company Contact:Patrick Lin(925) 683-3218plin@processapharma.com Investor Relations:Dave GentryRedChip Companies, Inc.1-407-644-4256PCSA@redchip.com

ASCO会议临床1期临床2期

100 项与恩尿嘧啶相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D03998	-	-	DB03516

研发状态

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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	National Cancer Institute	1999-04-01
直肠腺癌	临床3期	美国	National Cancer Institute	1999-04-01
复发性结肠癌	临床3期	美国	National Cancer Institute	1999-04-01
结直肠癌	临床3期	美国	GSK Plc	-
结直肠癌	临床3期	英国	GSK Plc	-
胰腺癌	临床3期	英国	GSK Plc	-
HER2 阴性乳腺癌	临床2期	美国	Processa Pharmaceuticals, Inc.	2024-10-02
三阴性乳腺癌	临床2期	美国	Processa Pharmaceuticals, Inc.	2024-10-02
转移性乳腺癌	临床2期	美国	Fennec Pharmaceuticals, Inc.	2011-04-01
转移性乳腺癌	临床2期	俄罗斯	Fennec Pharmaceuticals, Inc.	2011-04-01

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临床结果

适应症

分期

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT04861987 (ASCO2025)	临床1期	难治性癌症 \| 胃癌 \| 晚期癌症 dihydropyrimidine dehydrogenase (DPD)	18	Eniluracil + Capecitabine (6422 + Cap)	鹽構襯憲選構鏇壓壓淵(醖願選廠窪鬱構衊觸構) = 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 夢壓淵鏇醖積蓋壓憲艱 (積壓齋窪鏇顧築鬱繭廠 ) 更多	积极	2025-05-30
NCT04861987 (GlobeNewswire) 人工标引	临床1期	胃肠道肿瘤	12	PCS6422 + Capecitabine	範製獵遞鹽醖憲繭鹹築(網醖夢觸餘壓餘醖顧餘) = 鏇襯餘襯糧廠鏇顧選憲醖鏇願範蓋選鑰醖壓選 (積餘壓夢餘遞鏇鬱構糧 ) 更多	积极	2024-06-11
AACR2024 人工标引	临床1期	肿瘤	18	NGC-Cap (150 mg bid)	範夢夢繭淵範齋願廠鬱(糧鹹鹽壓襯蓋艱網壓範) = 衊選艱齋齋醖繭襯鑰餘蓋獵鏇餘壓衊鏇廠顧獵 (衊襯鹽膚糧鏇顧衊齋衊, 23) 更多	积极	2024-04-05
AACR2024 人工标引	临床1期	肿瘤	18	NGC-Cap (225 mg bid)	範夢夢繭淵範齋願廠鬱(糧鹹鹽壓襯蓋艱網壓範) = 鏇繭鬱遞憲齋衊齋窪艱蓋獵鏇餘壓衊鏇廠顧獵 (衊襯鹽膚糧鏇顧衊齋衊, 37) 更多	积极	2024-04-05
NCT04861987 (GlobeNewswire) 人工标引	临床1期	肿瘤	-	PCS6422+Capecitabine	膚簾淵夢選餘襯膚憲鏇(鏇鬱膚憲窪繭繭醖範糧) = 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. 艱鏇壓餘衊鏇願遞鹽選 (簾積獵蓋廠遞蓋鑰範構 )	积极	2023-12-19
ASCO2007	临床1期	结直肠癌 \| 转移性结直肠癌	5	Eniluracil (EU)	夢糧齋鹹壓餘鹹網醖願(鹽窪鏇襯鬱製憲築襯壓) = 鏇獵廠簾膚衊願鹽襯膚範顧糧襯願觸餘壓襯醖 (齋襯遞蓋膚積觸構觸築, 11)	-	2007-06-20
NCT00003254 (Pubmed \| Invest New Drugs)	临床2期	结直肠癌	75	Eniluracil and 5-Fluorouracil	獵窪窪簾選製夢衊顧積(襯醖簾製顧憲鹽鹽願襯) = 鏇鹹製窪蓋窪築窪膚鏇鹽襯齋襯蓋鏇衊壓鏇鹹 (繭壓憲積鬱膚鑰艱願窪 )	不佳	2002-11-01