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.

NCT00827580 / Terminated临床1期IIT

A Pilot Study of Eniluracil Containing Ointment for Prevention of Hand Foot Syndrome (HRS) Following Capecitabine (Xeloda)

A pilot study of eniluracil containing ointment for prevention of hand foot syndrome (HRS) following capecitabine (Xeloda).

开始日期2009-01-01

申办/合作机构

West Virginia University

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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151

项与恩尿嘧啶相关的文献（医药）

2021-01-01·Therapeutic advances in medical oncology2区 · 医学

Oral drugs in the treatment of metastatic colorectal cancer

2区 · 医学

ReviewOA

作者: Ortega Morán, Laura ; García-Alfonso, Pilar ; Grasso Cicala, Silvina ; Soto Alsar, Javier ; Calvo Ferrandiz, Pilar Aitana ; Blanco Codesido, Montserrat ; Muñoz Martín, Andrés Jesús ; Torres Pérez-Solero, Gabriela

Colorectal cancer (CRC) is one of the most common forms of cancer, with an estimated 1.36 million new cases and almost 700,000 deaths annually. Approximately 21% of patients with CRC have metastatic disease at diagnosis. The objective of this article is to review the literature on the efficacy and safety of oral drugs available for the treatment of metastatic colorectal cancer (mCRC). Several such drugs have been developed, and fluoropyrimidines are the backbone of chemotherapy in this indication. They exert their antitumour activity by disrupting the synthesis and function of DNA and RNA. Oral fluoropyrimidines include prodrugs capecitabine, tegafur, eniluracil/5-fluorouracil, tegafur/uracil, tegafur/gimeracil/oteracil and trifluridine/tipiracil (FTD/TPI). Oral drugs offer several advantages over injectable formulations, including convenience, flexibility, avoidance of injection-related adverse events (AEs) and, in some circumstances, lower costs. However, oral drugs may not be suitable for patients with gastrointestinal obstruction or malabsorption, they may result in reduced treatment adherence and should not be co-administered with drugs that interfere with absorption or hepatic metabolism. Oral fluoropyrimidines such as capecitabine, as monotherapy or in combination with oxaliplatin, irinotecan or bevacizumab, are as effective as intravenous 5-fluorouracil (5-FU) in first-line treatment of mCRC. Other oral fluoropyrimidines, such as FTD/TPI, are effective in patients with mCRC who are refractory, intolerant or ineligible for 5-FU. In addition, oral fluoropyrimidines are used in adjuvant treatment of mCRC. Regorafenib is an oral multikinase inhibitor used in patients in whom several previous lines of therapy have failed. Frequent AEs associated with oral drugs used in the treatment of CRC include hand-foot syndrome and gastrointestinal and haematological toxicities.

2014-02-01·Clinical breast cancer3区 · 医学

Eniluracil Plus 5-Fluorouracil and Leucovorin: Treatment for Metastatic Breast Cancer Patients in Whom Capecitabine Treatment Rapidly Failed

3区 · 医学

Article

作者: Rivera, Edgardo ; Chang, Jenny C ; Semiglazov, Vladimir ; Burdaeva, Olga ; Kirby, M Gray ; Spector, Thomas

BACKGROUND:

As part of a comparative phase II study of eniluracil/5-FU/Lv vs. capecitabine (Xeloda), an oral 5-FU prodrug for MBC, patients with rapid PD during capecitabine therapy crossed over to take eniluracil/5-FU/Lv.

PATIENTS AND METHODS:

Ten evaluable patients with radiologically documented PD within 70 days of capecitabine treatment were treated with a modified oral weekly eniluracil/5-FU/Lv regimen.

RESULTS:

After switching to eniluracil/5-FU/Lv, 3 (30%) patients had PR. Six (60%) had SD, producing a total of 90% with PR or SD. The median PFS was 140 days (vs. 42.5 days for capecitabine). Four (40%) patients had > 7 months PFS. Eniluracil/5-FU/Lv was well tolerated with mild to moderate diarrhea and nausea as the most common side effects.

CONCLUSION:

These positive efficacy and safety results encourage a larger study in patients with rapid PD during capecitabine treatment. Eniluracil/5-FU/Lv might enable these patients to continue with oral 5-FU rather than switching to the generally less well tolerated intravenous microtubule-interfering agents. In addition, the eniluracil/5-FU/Lv regimen might also provide any overall survival contribution of 5-FU that, for pharmacokinetic reasons, was not provided by capecitabine and would not be provided if these patients progressed directly to the other approved treatments.

2011-10-01·Cancer chemotherapy and pharmacology4区 · 医学

Final results of a prematurely discontinued Phase 1/2 study of eniluracil with escalating doses of 5-fluorouracil administered orally in patients with advanced hepatocellular carcinoma

4区 · 医学

Article

作者: Gilberto de Lima Lopes ; William P. Peters ; Alex Y. Chang ; Jennifer S. Dicksey ; Melvin Palalay

PURPOSE:

Eniluracil (EU) is a potent dihydropyrimidine (DPD) inhibitor, which improves the oral bio-availability of 5-fluorouracil (5-FU) and may overcome fluoropyrimidine (FP) resistance in hepatocellular carcinoma (HCC). Based on preclinical evidence, we aimed at studying a new dosing schedule for the combination with sequential administration, a lower dose of EU and higher doses of 5-FU than previously investigated.

METHODS:

Patients with a diagnosis of hepatocellular carcinoma were eligible for this Phase 1/2 study. The primary endpoint for the Phase 1 was the determination of dose-limiting toxicity (DLT) and the maximum tolerated dose (MTD) of oral 5-FU when given 14 h after oral EU 5 mg, weekly for 3 out of 4 weeks. The starting dose of 5-FU was 20 mg, followed by 30 mg and 80 mg. Secondary endpoints were anti-tumor activity, pharmacokinetics, and DPD activity in peripheral blood mononuclear cells. RECIST was used for assessment of efficacy and NCI CTC-AE version 3.0 for describing toxicity.

RESULTS:

Nine patients enrolled in the trial. Median age was 53 years. All patients were Asian (one from Hawaii, 8 from Singapore). Prior treatment was as follows: liver surgery, 2 patients; chemo-embolization, 2 patients; thalidomide, 3 patients; adriamycin, 3 patients. Patients received a median of 2 cycles (range, 1-14) of therapy. No DLTs were seen up to the 80-mg 5-FU cohort. Out of 3 patients in the 80-mg cohort, one had pancytopenia. One patient at the 20-mg cohort had stable disease that lasted for 14 months.

CONCLUSION:

EU, at a 5.0-mg weekly dose, was well tolerated. There was no evidence of dose-related safety effects. This trial did not define the MTD for oral 5-FU. No objective responses by RECIST were noted but one patient had stable disease and a decrease of 28% in the sum of the largest diameters of her target lesions. The study was terminated early because of CNS-related toxicities noted in the single higher dose levels in a companion study, AHX-03-104.

项与恩尿嘧啶相关的新闻（医药）

2024-06-16

·药明康德

显著延长肝癌患者生存期的细胞疗法；可同时减重并降低心血管风险的小分子疗法…… | 一周盘点

▎药明康德内容团队编辑本期看点 1. 既能减重又能降低心血管风险的小分子疗法NT-0796在早期临床试验中表现积极。 2. T细胞受体（TCR）T细胞疗法SCG101在晚期乙型肝炎病毒（HBV）相关肝细胞癌（HCC）患者中展现出抗病毒和抗肿瘤双重活性，显著延长患者的生存期。 3. 白血病患者在接受造血干细胞移植后接受一剂INB-100治疗，100%可评估的患者于今年5月31日时仍然存活，并且维持完全缓解（CR）达到1年。药明康德内容团队整理 NT-0796：公布1b/2a期临床试验数据 NodThera宣布其在炎症性肥胖受试者中进行的临床1b/2a期心血管风险研究取得了积极数据，该研究旨在评估其在研口服、可穿透血脑屏障的NLRP3炎性小体抑制剂NT-0796，对患者的炎症、心血管和代谢风险参数的影响。NLRP3炎症小体是一种经过高度验证的抗炎药物靶点。分析显示，NT-0796可有效减少患者体内C反应蛋白（CRP）水平，并使患者的体重显著减少。此外，接受NT-0796治疗患者的其他促炎和心脏代谢生物标志物也有所减少，这是该研究的次要终点。与以往的试验一致，NT-0796总体上安全且耐受性良好，不良事件主要是轻度和短暂的，未观察到严重不良事件。NodThera目前正在为针对肥胖症，以及包括其他心脏代谢疾病和帕金森病在内的临床2期研究做准备。 SCG101：公布首次人体临床试验结果星汉德生物（SCG Cell Therapy）宣布，其自主研发的HBV特异性TCR-T细胞疗法SCG101入选了2024年度欧洲肝脏研究协会年会（EASL Congress 2024）的焦点精选报告。SCG101是一种针对乙型肝炎病毒表面抗原（HBsAg）的特异性自体TCR-T细胞疗法。星汉德生物依托自主研发的独有GianT技术平台，筛选高亲力且高活性的天然TCR，可以有效靶向实体肿瘤中通过主要组织相容性复合体（MHC）表达的细胞内抗原。临床前和临床研究数据显示，SCG101具有肿瘤抑制和HBV cccDNA根除作用，可实现抗肿瘤和抗病毒功能。此次公布的研究结果显示，SCG101在晚期HBV相关HCC患者中展现出抗病毒和抗肿瘤双重活性，显著延长了患者的生存期。至稿件截止日，客观缓解率（ORR）为33%，获得部分缓解（PR）的患者均维持缓解超过6个月，其中1例实现了靶病灶完全缓解（pCR），且持续缓解超过27个月。此外，患者的肿瘤应答与SCG101的抗病毒活性高度相关。4例血清HBsAg显著下降并维持在低水平的患者的肿瘤缩小，且无进展生存期和总生存期显著延长至5.9个月和19.0个月。 INB-100 IN8bio：公布1期临床试验的新数据 IN8bio公司公布了其在研现货型γδ T细胞疗法INB-100的最新1期临床试验结果。INB-100是一款来自健康供体的同种异体γδ T细胞，在体外经过扩增和激活后，被输注到白血病患者体内。在这项研究者发起的1期临床试验中，白血病患者在接受造血干细胞移植后，接受一剂INB-100的治疗。这些患者包括高风险和复发急性髓系白血病（AML）患者，他们此前已接受过多种疗法治疗，包括嵌合抗原受体（CAR）T细胞疗法。截至2024年5月31日的数据，100%可评估的白血病患者仍然存活并且维持CR达到1年。此前发表的历史数据显示，高达50%的血液癌症患者在接受造血干细胞移植和减轻强度预处理（reduced intensity conditioning）的情况下会出现复发，并且在复发后不久去世。在这10名患者中，两名接受INB-100治疗的患者已经无癌三年半，另一名患者接近3年无癌。数据同时显示，接受单次治疗后的365天里，同种异体γδ T细胞能够长期持久地在体内扩增。新闻稿指出，这是首次同种异体细胞疗法表现出持续的扩增和持久性。安全性方面，INB-100没有出现剂量限制性毒性，未发现细胞因子释放综合征（CRS），神经毒性或免疫效应细胞相关神经毒性综合征（ICANS），未发现严重感染。 Delpacibart braxlosiran （AOC 1020）：公布1/2期临床试验的初步数据 Avidity Biosciences宣布其用于治疗面肩肱型肌营养不良症（FSHD）的在研抗体寡核苷酸偶联物（AOC）delpacibart braxlosiran（del-brax，AOC 1020）在临床1/2期试验FORTITUDE中的初步积极数据。FSHD是由于DUX4基因异常表达所引起。DUX4蛋白的异常表达导致肌肉细胞基因表达的变化，造成FSHD患者肌肉功能的终身、渐进性丧失。根据新闻稿，del-brax是首个旨在治疗FSHD根本原因的在研AOC疗法，由一种专有的转铁蛋白受体1（TfR1）靶向单克隆抗体，与靶向DUX4 mRNA的siRNA偶联所组成。 ▲Del-brax下调患者受DUX4调控的基因表达（图片来源：参考资料[2]）此次公布的结果显示，FSHD患者接受该疗法后，其受DUX4调控的基因一致性地下调超过50%，并且患者的肌肉功能有改善的趋势。根据此积极结果，Avidity计划加速FORTITUDE研究中注册队列的启动。 Bexicaserin（LP352）：公布1b/2a期临床试验的新数据 Longboard Pharmaceuticals公司公布了PACIFIC研究的开放标签扩展（OLE）研究的积极数据。PACIFIC研究旨在评估其在研疗法bexicaserin（LP352）用于治疗与广泛发育性和癫痫性脑病相关癫痫发作的疗效与安全性。Bexicaserin是一款高选择性、口服、新型5-HT2C受体超激动剂，为潜在的“best-in-class”疗法。所有41例完成PACIFIC研究的患者均选择参加OLE研究。结果显示，在OLE研究中接受bexicaserin治疗约6个月的可评估受试者（n=40）的中位可数运动性癫痫发作频率较进入PACIFIC研究时的基线水平降低56.1%。其中，在PACIFIC研究中被随机分配到接受bexicaserin治疗组的受试者（n=31）减少了54.9%，在PACIFIC研究中被随机分配到安慰剂组的受试者在OLE研究中过渡到bexicaserin治疗，这类患者（n=9）减少了57.3%。安全性方面，观察到的最常见的治疗伴发不良事件为上呼吸道感染、COVID-19、肺炎、鼻窦炎、癫痫发作和食欲下降。一名受试者因嗜睡而停药，一名受试者因撤回同意而停药。 JIN-A02：公布1/2期临床试验的新数据 J INTS BIO公司公布了其进行中的用于治疗非小细胞肺癌（NSCLC）的新型第4代口服EGFR酪氨酸激酶抑制剂（TKI）JIN-A02的1期临床研究的最新情况。JIN-A02具有高度的选择性，可有效对抗携带EGFR C797S双突变或三突变的NSCLC，并具有高脑渗透率和体内疗效。截至目前，已有两名患者达到了确认的PR，还有3名患者达到了疾病稳定（SD）。此外，研究人员还在1例达到SD的患者中观察到脑转移灶缩小28.6%。安全性方面，未报告剂量限制性毒性，也没有发现皮疹、腹泻或心脏毒性这类通常与EGFR TKI的使用相关的副作用。 PCS6422：公布1b期临床试验的初步数据 Processa Pharmaceuticals公司公布了其下一代卡培他滨组合疗法（NGC-Cap）治疗III/IV期胃肠道癌症患者的1b期临床试验的初步结果。口服卡培他滨在体内代谢后会变成5-氟尿嘧啶（5-FU），进而代谢成两种分子，一种能主动杀死癌细胞，一种只会产生副作用。二氢嘧啶脱氢酶（DPD）在5-FU转化为引起副作用的分子方面起着重要作用。PCS6422能够不可逆地抑制DPD。在相当剂量水平下，PCS6422单药在动物中既没有毒性也不具有活性。而当与卡培他滨或5-FU联合给药时，PCS6422降低了5-FU向仅引起副作用的分子的代谢，从而使更多的5-FU到达癌细胞。Processa Pharmaceuticals公司将PCS6422与低剂量的卡培他滨结合使用，组成了NGC-Cap。此次公布的结果显示，在所有接受一剂PCS6422后再接受7天卡培他滨治疗的可评估患者中，12例可评估患者的疾病控制率为66.7%（8/12），包括2例PR和6例SD。这些患者的无进展生存期约为5-11个月。相比之下，在卡培他滨产品说明书中，301例接受卡培他滨单药治疗的转移性结直肠癌患者的总缓解率约为21%，患者发生进展的时间约为4.5个月。安全性方面，与卡培他滨单药治疗相比，在所有NGC-Cap剂量组中，5-FU的暴露量更高，副作用的发生情况相似或更少。 ▲欲了解更多前沿技术在生物医药产业中的应用，请长按扫描上方二维码，即可访问“药明直播间”，观看相关话题的直播讨论与精彩回放参考资料（可上下滑动查看） [1] NodThera’s NLRP3 Inhibitor NT-0796 Meets Primary Endpoint of Inflammation Reversal in Phase Ib/IIa Trial in Obese Subjects with Cardiovascular Risk. Retrieved June 14, 2024 from https://www.nodthera.com/news/nodtheras-nlrp3-inhibitor-nt-0796-meets-primary-endpoint-of-inflammation-reversal-in-phase-ib-iia-trial-in-obese-subjects-with-cardiovascular-risk/ [2] 重磅｜EASL 最新突破性数据：星汉德生物TCR-T细胞治疗晚期肝癌患者总生存期显著延长并伴随乙肝表面抗原清除，获选最佳精选报告. Retrieved June 14, 2024 from https://www.prnasia.com/story/450060-1.shtml [3] Avidity Announces Unprecedented AOC 1020 Data from Phase 1/2 FORTITUDE™ Trial Demonstrating Greater Than 50 Percent Reduction in DUX4 Regulated Genes and Trends of Functional Improvement in People Living with Facioscapulohumeral Muscular Dystrophy. Retrieved June 14, 2024 from https://www.prnewswire.com/news-releases/avidity-announces-unprecedented-aoc-1020-data-from-phase-12-fortitude-trial-demonstrating-greater-than-50-percent-reduction-in-dux4-regulated-genes-and-trends-of-functional-improvement-in-people-living-with-facioscapulohumeral-m-302170099.html [4] Avidity Biosciences Investor & Analyst Event Series – Vol. 9: Preliminary Data from Phase 1/2 FORTITUDE™ trial of AOC 1020 in people living with FSHD. Retrieved June 14, 2024 from https://aviditybiosciences.investorroom.com/events-and-presentations#:~:text=Avidity%20Biosciences%20Investor%20%26%20Analyst%20Event%20Series%20%E2%80%93%20Vol.%209%3A%20Preliminary%20Data%20from%20Phase%201/2%20FORTITUDE%E2%84%A2%20trial%20of%20AOC%201020%20in%20people%20living%20with%20FSHD [5] IN8bio Presents Positive Data Demonstrating Durable 1-year Complete Remission in 100% of Evaluable Patients in Phase 1 Trial of INB-100. Retrieved June 14, 2024, from https://www.globenewswire.com/news-release/2024/06/13/2898625/0/en/IN8bio-Presents-Positive-Data-Demonstrating-Durable-1-year-Complete-Remission-in-100-of-Evaluable-Patients-in-Phase-1-Trial-of-INB-100.html [6] Longboard Pharmaceuticals Announces Positive Interim Results from the Open-Label Extension (OLE) of the Phase 1b/2a PACIFIC Study Evaluating Bexicaserin in Participants with Developmental and Epileptic Encephalopathies (DEEs). Retrieved June 14, 2024, from [7] Processa Pharmaceuticals Announces Positive Efficacy Results from Preliminary Evaluation of Phase 1b Dose-escalating Trial with NGC-Cap in Gastrointestinal Cancer. Retrieved June 14, 2024, from https://www.globenewswire.com/news-release/2024/06/11/2896777/0/en/Processa-Pharmaceuticals-Announces-Positive-Efficacy-Results-from-Preliminary-Evaluation-of-Phase-1b-Dose-escalating-Trial-with-NGC-Cap-in-Gastrointestinal-Cancer.html [8] J INTS BIO, ASCO 2024 - JIN-A02 showed tumor reductions including brain metastasis in the ongoing first-in-human, dose-finding Phase 1 clinical study. Retrieved June 14, 2024, from https://www.prnewswire.com/news-releases/j-ints-bio-asco-2024--jin-a02-showed-tumor-reductions-including-brain-metastasis-in-the-ongoing-first-in-human-dose-finding-phase-1-clinical-study-302168022.html [9] Surrozen Presents Preliminary Results from Phase 1a Study of SZN-043 in Healthy Volunteers and Patients with a History of Liver Cirrhosis at the 2024 European Association for the Study of the Liver (EASL) in Milan. Retrieved June 14, 2024, from https://www.globenewswire.com/news-release/2024/06/10/2896001/0/en/Surrozen-Presents-Preliminary-Results-from-Phase-1a-Study-of-SZN-043-in-Healthy-Volunteers-and-Patients-with-a-History-of-Liver-Cirrhosis-at-the-2024-European-Association-for-the-S.html [10] Eilean Therapeutics Announces FDA Clearance of Investigational New Drug (IND) Application for Lomonitinib for the Treatment of Acute Myeloid Leukemia (AML). Retrieved June 14, 2024, from https://www.prnewswire.com/news-releases/eilean-therapeutics-announces-fda-clearance-of-investigational-new-drug-ind-application-for-lomonitinib-for-the-treatment-of-acute-myeloid-leukemia-aml-302167897.html [11] Ensem Therapeutics Announces Achievement of Milestone Following Entry of Small Molecule CDK2 Inhibitor into Clinical Trials for Solid Tumors. Retrieved June 14, 2024, from https://www.businesswire.com/news/home/20240612661711/en/ [12] Zumutor Biologics Announces Dosing of First Patient with ZM008, a First-in-Class Anti LLT1 Antibody. Retrieved June 14, 2024, from https://www.prnewswire.com/news-releases/zumutor-biologics-announces-dosing-of-first-patient-with-zm008-a-first-in-class-anti-llt1-antibody-302170537.html [13] KSQ Therapeutics Announces First Patient Dosed in Clinical Development Program for KSQ-001EX, a CRISPR/Cas9 Engineered Tumor Infiltrating Lymphocyte (eTIL®) Therapy. Retrieved June 14, 2024, from https://ksqtx.com/news-events/ksq-therapeutics-announces-first-patient-dosed-in-clinical-development-program-for-ksq-001ex-a-crispr-cas9-engineered-tumor-infiltrating-lymphocyte-etil-therapy/ [14] City of Hope CAR T Cell Therapy for Advanced Prostate Cancer Demonstrates Positive Results in Phase 1 Clinical Trial. Retrieved June 14, 2024, from https://www.businesswire.com/news/home/20240612751963/en [15] Assembly Biosciences Doses First Participant in Phase 1a/b Clinical Trial of Herpes Simplex Virus Helicase-Primase Inhibitor Candidate ABI-5366. Retrieved June 14, 2024, from https://investor.assemblybio.com/news-releases/news-release-details/assembly-biosciences-doses-first-participant-phase-1ab-clinical [16] VYNE Therapeutics Announces Dosing of First Participants in Phase 1a Trial of Novel BD2-Selective BET Inhibitor VYN202. Retrieved June 14, 2024, from https://vynetherapeutics.com/press-releases/vyne-therapeutics-announces-dosing-of-first-participants-in-phase-1a-trial-of-novel-bd2-selective-bet-inhibitor-vyn202/ 免责声明：药明康德内容团队专注介绍全球生物医药健康研究进展。本文仅作信息交流之目的，文中观点不代表药明康德立场，亦不代表药明康德支持或反对文中观点。本文也不是治疗方案推荐。如需获得治疗方案指导，请前往正规医院就诊。版权说明：本文来自药明康德内容团队，欢迎个人转发至朋友圈，谢绝媒体或机构未经授权以任何形式转载至其他平台。转载授权请在「药明康德」微信公众号回复“转载”，获取转载须知。分享，点赞，在看，聚焦全球生物医药健康创新

细胞疗法临床结果临床1期

2024-06-11

·GlobeNewswire-Health Care

Processa Pharmaceuticals Announces Positive Efficacy Results from Preliminary Evaluation of Phase 1b Dose-escalating Trial with NGC-Cap in Gastrointestinal Cancer

Eight of 12 evaluable patients (66.7%) had progression-free survival (PFS) ranging from 5 to 11 months At the highest NGC-Cap dose, all three evaluable patients had PFS with two partial responses (PR) and one stable disease (SD) For all NGC-Cap doses, 5-Fluorouracil (5-FU) exposure was greater and fluoro-beta-alanine (FBAL) exposure was lower with a better or similar side-effect profile than monotherapy capecitabine HANOVER, MD., June 11, 2024 (GLOBE NEWSWIRE) -- Processa Pharmaceuticals, Inc. (Nasdaq: PCSA) (Processa or the Company), a clinical-stage pharmaceutical company focused on developing the next generation of chemotherapeutic drugs with improved efficacy and safety, today announced positive efficacy results from the preliminary evaluation of its recently completed Phase 1b clinical trial which defined the Maximum Tolerated Dose (MTD) and Recommended Phase 2 Dose Range (RP2DR) for Next Generation Capecitabine (NGC-Cap) administered to patients with Stage III or IV gastrointestinal tract (GI) cancer. “We are encouraged by the preliminary efficacy analysis from our NGC-Cap Phase 1b dose-escalating safety/tolerability trial demonstrating some anti-tumor activity in patients with advanced GI cancer who have progressive cancer after relapsing or not responding to prior therapy. The favorable response is likely due to NGC-Cap’s ability to distribute more 5-FU to cancer cells than monotherapy capecitabine. The promising Phase 1b safety and tolerability profile plus these early efficacy signals provide validation for further development of NGC-Cap,” stated David Young, PharmD, Ph.D., President of Research and Development at Processa. “From this Phase 1b trial, we have been able to define the MTD and the RP2DR to use in our Phase 2 Optimal Dosage Regimen trial in breast cancer in the third quarter of 2024.” Dr. Young added, “Given the need for more effective chemotherapy treatment with improved tolerability across multiple types of cancer, we believe that NGC-Cap has the potential to provide a safer, more efficacious option to treat the different cancers for which capecitabine and 5-FU are presently used.” The NGC-Cap Phase 1b trial is evaluating ascending doses of capecitabine when administered after a single dose of PCS6422 in Stage III or IV patients with advanced, relapsed or refractory progressive GI cancer. All patients relapsed from or failed all other treatments, including prior treatment with capecitabine or 5-FU. For all doses of capecitabine in the Phase 1b NGC-Cap trial, exposure to 5-FU was greater and exposure to FBAL was lower with a better or similar side effect profile compared with monotherapy capecitabine. In addition, preliminary analysis of the efficacy data demonstrated early evidence of anti-tumor activity of capecitabine combined with PCS6422, which was assessed using RECIST 1.1 evaluations (Response Evaluation Criteria in Solid Tumors) by scans every eight weeks. Key Efficacy Findings from Preliminary Analysis of NGC-Cap Phase 1b Clinical Trial (NCT04861987) In all evaluable patients receiving one dose of PCS6422 and seven days of capecitabine, PR or SD was observed in 66.7% (8 out of 12) of evaluable patients, including two with PR and six with SD. The length of PFS was approximately 5 to 11 months across these patients.At the MTD of 225 mg of capecitabine dosed twice daily after a single dose of PCS6422, all three evaluable patients (100%) had PFS with the time to progression being approximately 5 to 7 months.At the second highest dose of 150 mg capecitabine dosed twice daily after a single dose of PCS6422, 66.7% (2 out of 3) of evaluable patients had SD with the time to progression of approximately 3 to 7 months.These two dosage regimens will be further evaluated in the Phase 2 trial in breast cancer patients to determine the optimal dosage regimen for the pivotal trial.By comparison, in the capecitabine product label, 301 metastatic colorectal cancer patients treated with monotherapy capecitabine had an overall response rate of approximately 21% and the time to progression of approximately 4.5 months. About Capecitabine Administered with PCS6422 (NGC-Cap) NGC-Cap combines the administration of PCS6422, the Company’s irreversible dihydropyrimidine dehydrogenase (DPD) enzyme inhibitor, with low doses of capecitabine. Capecitabine is the oral form of 5-FU, and along with 5-FU is among the most widely used chemotherapy drugs, particularly for the treatment of solid tumors. When metabolized (after oral ingestion) it becomes 5-FU in the body, which, in turn, metabolizes to molecules called anabolites that actively kill duplicating cells, such as cancer cells, and to molecules called catabolites that only cause side effects. The presence of the DPD enzyme plays an integral role in the undesirable conversion of 5-FU to catabolites. PCS6422 irreversibly inhibits DPD. PCS6422 is neither toxic nor active as a single agent in animals at comparable dose levels. However, when administered in combination with capecitabine or 5-FU, PCS6422 decreases the metabolism of 5-FU to the catabolites that only cause side effects, allowing more of the 5-FU to reach the cancer cells. About Processa Pharmaceuticals, Inc. Processa is a clinical-stage pharmaceutical company focused on developing the Next Generation Chemotherapy (NGC) drugs to improve the safety and efficacy of cancer treatment. By combining its novel oncology pipeline with proven cancer-killing active molecules and the Processa Regulatory Science Approach, as well as experience in defining Optimal Dosage Regimens for FDA approvals, Processa not only will provide better therapy options to cancer patients but will also increase the probability of FDA approval for its NGC drugs following an efficient path to approval. Processa’s NGC drugs are modifications of existing FDA-approved oncology drugs resulting in an alteration of the metabolism and/or distribution of these drugs while maintaining the existing mechanisms of killing the cancer cells. The Company’s approach to drug development is based on more than 30 years of expertise to efficiently design and conduct clinical trials that demonstrate a positive benefit/risk relationship. The Processa team has a track record of obtaining over 30 indication approvals across almost every division of the FDA. Using its proven Regulatory Science Approach, the Processa Team has experience defining the Optimal Dosage Regimen using the principles of the FDA’s Project Optimus Oncology initiative. The advantages of Processa’s NGCs are expected to include fewer patients experiencing side effects that lead to dose discontinuation, more significant cancer response and a greater number of patients – in excess of 200,000 for each NGC drug – who will benefit from each NGC drug. Processa is currently 1) starting to initiate sites for the Phase 2 study that will identify the optimal dosage regimen for Next Generation Capecitabine (PCS6422 and capecitabine to treat breast, metastatic colorectal, gastrointestinal, pancreatic and other cancers), 2) defining the design of the Next Generation Gemcitabine (PCS3117 to treat pancreatic, biliary, lung, ovarian, breast and other cancers) Phase 2 optimal dosage regimen study to discuss with FDA, and 3) defining the formulation and toxicology program for Next Generation Irinotecan (PCS11T to treat lung, colorectal, gastrointestinal, pancreatic and other cancers). 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 Contact:Yvonne BriggsLHA Investor Relations(310) 691-7100ybriggs@lhai.com # # #

临床1期临床结果临床2期

2024-05-06

·GlobeNewswire-Health Care

Processa Pharmaceuticals to Participate in the EF Hutton Annual Global Conference

HANOVER, Md., May 06, 2024 (GLOBE NEWSWIRE) -- Processa Pharmaceuticals, Inc. (Nasdaq: PCSA) (“Processa” or the “Company”), a clinical-stage pharmaceutical company focused on developing the next generation of chemotherapeutic drugs with improved efficacy and safety, today announced that management will be participating in the EF Hutton Annual Global Conference being held May 15, 2024 at The Plaza Hotel in New York City. Management will be holding one-on-one meetings with investors. About Processa Pharmaceuticals, Inc. Processa is a clinical-stage pharmaceutical company focused on developing the Next Generation Chemotherapy (NGC) drugs to improve the safety and efficacy of cancer treatment. By combining its novel oncology pipeline with proven cancer-killing active molecules and the Processa Regulatory Science Approach, as well as experience in defining Optimal Dosage Regimens for FDA approvals, Processa not only will provide better therapy options to cancer patients, but will also increase the probability of FDA approval for its NGC drugs following an efficient path to approval. Processa’s NGC drugs are modifications of existing FDA-approved oncology drugs resulting in an alteration of the metabolism and/or distribution of these drugs while maintaining the existing mechanisms of killing the cancer cells. The Company’s approach to drug development is based on more than 30 years of expertise to efficiently design and conduct clinical trials that demonstrate a positive benefit/risk relationship. The Processa team has a track record of obtaining over 30 approvals for indications across almost every division of the FDA. Using its proven Regulatory Science Approach, the Processa Team has experience defining the Optimal Dosage Regimen using the principles of the FDA’s Project Optimus Oncology initiative. The advantages of Processa’s NGCs are expected to include fewer patients experiencing side effects that lead to dose discontinuation, more significant cancer response and a greater number of patients – in excess of 200,000 for each NGC drug – who will benefit from each NGC drug. Currently under development are three NGC treatments: Next Generation Capecitabine (PCS6422 and capecitabine to treat breast, metastatic colorectal, gastrointestinal, pancreatic and other cancers), Next Generation Gemcitabine (PCS3117 to treat pancreatic, biliary, lung, ovarian, breast and other cancers) and Next Generation Irinotecan (PCS11T to treat lung, colorectal, gastrointestinal, pancreatic and other cancers). For more information, visit our website at www.processapharma.com. Company Contact:Patrick Lin(925) 683-3218plin@processapharma.com Investor Relations Contact:Yvonne BriggsLHA Investor Relations(310) 691-7100ybriggs@lhai.com # # #

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

10 条进展最快的记录,

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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	-
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
肝细胞癌	临床2期	中国	Fennec Pharmaceuticals, Inc.	2006-04-27
局部晚期肝细胞癌	临床2期	美国	Fennec Pharmaceuticals, Inc.	2006-04-27

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临床结果

适应症

分期

评价

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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 (GlobeNewswire) 人工标引	临床1期	胃肠道肿瘤	12	PCS6422 + Capecitabine	積蓋鑰襯憲夢鑰餘獵願(憲艱襯鹹夢製艱構選醖) = 襯觸鹽廠膚蓋遞鑰鏇艱衊艱鏇鑰蓋膚選顧鑰網 (艱簾積積壓簾構鏇蓋鑰 ) 更多	积极	2024-06-11
GlobeNewswire 人工标引	临床1期	肿瘤	-	PCS6422+Capecitabine	範範築壓繭願遞窪醖齋(壓網鬱壓選淵膚積網齋) = 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. 構鹽鬱醖壓醖簾壓壓壓 (構糧齋選願餘製鏇積醖 )	积极	2023-12-19
ASCO2007	临床1期	结直肠癌 \| 转移性结直肠癌	5	Eniluracil (EU)	蓋積鬱窪鑰築繭構遞鬱(簾築鹽窪簾簾夢顧憲夢) = 衊糧鏇鹹積積獵艱鹹觸範夢簾鹹齋簾簾夢窪蓋 (糧觸憲壓觸衊夢簾廠膚, 11)	-	2007-06-20
NCT00003254 (Pubmed \| Invest New Drugs)	临床2期	结直肠癌	75	Eniluracil and 5-Fluorouracil	簾齋憲衊憲顧襯顧鏇衊(願襯選顧衊築淵鏇憲觸) = 網網淵淵築醖願艱憲夢獵鏇餘窪鑰顧壓顧鏇窪 (鑰繭觸構襯夢築範淵廠 )	不佳	2002-11-01