塞来昔布(Celecoxib) - 药物靶点：COX-2_在研适应症：偏头痛，疼痛，牙痛_专利_临床

概要

基本信息

简介CELEBREX是一种非甾体抗炎药。Celecoxib具有镇痛，抗炎和退热作用。CELEBREX的作用机制被认为是通过抑制前列腺素合成，主要通过抑制COX-2而实现的。Celecoxib是体外前列腺素合成的强效抑制剂。治疗期间达到的Celecoxib浓度已经产生了体内效果。前列腺素使传入神经末梢变得敏感，并增强了缓激肽诱导动物模型疼痛的作用。前列腺素是炎症介质。由于Celecoxib是前列腺素合成的抑制剂，因此其作用机制可能是通过减少外周组织中的前列腺素而实现的。CELEBREX适用于骨关节炎（OA），类风湿性关节炎（RA），少年类风湿性关节炎（JRA），强直性脊柱炎（AS），急性疼痛，原发性痛经。它最初由辉瑞公司在1998年在美国上市，用于治疗关节炎。

药物类型

小分子化药

别名

Celecoxib (JAN/USP/INN)、p-(5-p-Tolyl-3-(trifluoromethyl)pyrazol-1-yl)benzenesulfonamide、AD-2111

+ [23]

靶点

COX-2

作用方式

抑制剂

作用机制

COX-2抑制剂(环氧化酶-2抑制剂)

治疗领域

肿瘤免疫系统疾病感染+ [7]

在研适应症

偏头痛疼痛牙痛+ [18]

非在研适应症

光化性角化病食管腺癌前列腺腺癌+ [49]

原研机构

Pfizer Inc.

在研机构

Scilex Pharmaceuticals, Inc.

Carwin Pharmaceutical Associates LLCUpjohn EESV

+ [8]

非在研机构

Pfizer Inc.

Viatris, Inc.

Pharmacia Corp.

+ [12]

权益机构

Ethypharm SAS

Dr. Reddy's Laboratories Ltd.

Scilex Pharmaceuticals, Inc.

+ [6]

最高研发阶段批准上市

首次获批日期

美国 (1998-12-31),

骨关节炎类风湿关节炎

最高研发阶段(中国)批准上市

特殊审评加速批准 (美国)、孤儿药 (美国)、优先审评 (中国)

登录后查看时间轴

结构/序列

分子式C17H14F3N3O2S

InChIKeyRZEKVGVHFLEQIL-UHFFFAOYSA-N

CAS号169590-42-5

关联

791

项与塞来昔布相关的临床试验

IRCT20200306046708N1

/ Suspended临床2/3期IIT

Celecoxib added to mood stabilizer for treating acute mania: A randomized, double-blind, placebo-controlled trial

开始日期2633-12-15

申办/合作机构

Mashhad University of Medical Sciences

NCT03590821

/ Not yet recruiting早期临床1期IIT

Modulating Celecoxib Induced Blood Pressure Changes by Timed Administration of Aspirin and the Human Chronobiome

To determine whether timed administration of aspirin ameliorates the effects of celecoxib on blood pressure.

开始日期2026-12-01

申办/合作机构

University of Pennsylvania

NCT07139405

/ Not yet recruiting临床2期

A DOUBLE-BLIND, RANDOMIZED, ACTIVE-CONTROLLED, PARALLEL-GROUP, PHASE II TRIAL TO EVALUATE THE SAFETY, TOLERABILITY, AND SUPERIORITY OF TRIGLYTZA® OVER METFORMIN IN PATIENTS WITH INADEQUATE GLYCEMIC CONTROL OVER 24 WEEKS OF TREATMENT

Type 2 diabetes (T2DM) is still very difficult to treat because current medicines mostly help with symptoms but don't stop the damage happening inside the pancreas. Many people who start on common treatments like Metformin, and even newer drugs like Ozempic, eventually stop responding to them. This is because these drugs don't address the real problem: the gradual loss of the pancreas' ability to make insulin and the body's increasing resistance to it.
Myopharm is developing a new treatment called TriGlytza®, which combines existing medicines (Celecoxib and Valsartan) with Metformin. This new approach is designed to target the inflammation and biological pathways that cause ongoing damage in Type 2 diabetes, aiming to protect the pancreas and reduce insulin resistance. Early animal studies and past clinical trials with the individual drugs show promising results.
The number of people with Type 2 diabetes is expected to double by 2045, and the disease brings huge health and financial costs. It also raises the risk of heart disease, stroke, kidney damage, nerve problems, vision loss, certain cancers, and even conditions like Alzheimer's. Because of this, a treatment that addresses the root causes rather than just symptoms could make a major difference.
TriGlytza® aims to provide a safe, affordable, and more effective long-term treatment than current options, helping people manage their diabetes better and avoid related health problems.

开始日期2026-02-01

申办/合作机构

Myopharm Ltd.

100 项与塞来昔布相关的临床结果

登录后查看更多信息

100 项与塞来昔布相关的转化医学

登录后查看更多信息

100 项与塞来昔布相关的专利（医药）

登录后查看更多信息

10,003

项与塞来昔布相关的文献（医药）

2026-01-01·SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY

A near-infrared AIE probe targeting COX-2 for imaging of Cancer cells

Article

作者: Liu, Jianxi ; Xue, Ying ; Liu, Wanhui ; Shen, Li ; Zhang, Yonglin ; Zhu, Yanping ; Chen, Shulin ; Wang, Aiping ; Xu, Lixiao ; Hu, Jiale

High expression of cyclooxygenase-2 (COX-2) in the inflammatory tumor microenvironment is a critical target for early cancer diagnosis. We designed and synthesized a series of near-infrared (NIR) fluorescent probes based on the aggregation-induced emission (AIE) mechanism for targeted COX-2 imaging. Leveraging a D-π-A quinoline-malononitrile core, we developed probes YL-180 (non-targeted control), YL-181 (celecoxib conjugate), and YL-186 (indomethacin conjugate). Notably, this work represents the first report combining this specific AIE core with established COX-2 targeting ligands, celecoxib and indomethacin, for this application. These probes exhibit characteristic AIE properties, with YL-181 showing fluorescence enhancement up to approximately 9.7-fold from pure THF in aggregated state, effectively overcoming the aggregation-caused quenching (ACQ) issue. They also possess favorable optical features including NIR emission (>650 nm) and large Stokes shifts (>200 nm). Their aggregation behavior and nanoparticle formation were characterized by DLS and TEM. In vitro cellular imaging revealed that YL-181 achieved superior tumor cell selectivity, demonstrating approximately 22-fold higher fluorescence intensity in MCF-7 cancer cells over normal HUVEC cells (around 4-fold for YL-186 over normal HUVEC cells). A competitive assay confirmed YL-181's specific COX-2 binding. Furthermore, YL-181 sensitively reflected intracellular COX-2 levels, with fluorescence decreasing by approximately 97 % from untreated upon COX-2 inhibition and increasing by around 135 % from untreated upon induction. Molecular docking and dynamics simulations provided insights into the specific binding mode and dynamic stability of YL-181 with COX-2 from an atomic perspective. In vivo imaging validated YL-181's excellent tumor targeting ability and high contrast performance in mouse models, showing a tumor-to-background ratio (TBR) of around 1.83 from normal tissue background, consistent with ex vivo organ analysis. Our highly sensitive and selective COX-2 targeted AIE probe, YL-181, holds significant potential for precise early tumor imaging.

2025-12-01·CANCER CHEMOTHERAPY AND PHARMACOLOGY

Protective effect of celecoxib against capecitabine induced hand and foot syndrome in patients with colorectal Cancer

Article

作者: Kettana, Ahmed M ; Mostafa, Tarek M ; Ghannam, Amr A ; El-Afify, Dalia R

BACKGROUND:

Hand-foot syndrome (HFS) is the most common adverse effect of capecitabine.

OBJECTIVE:

We aimed at evaluating the protective effect of celecoxib against capecitabine induced hand and foot syndrome in patients with colorectal cancer (CRC).

METHODS:

In this randomized controlled parallel study, 44 newly diagnosed patients with stage II CRC were randomly allocated into two groups; Group 1(control group; n = 22) which received 6 cycles of capecitabine-based chemotherapy (cycle is every 3 weeks) and group 2 (celecoxib group; n = 22) which received 6 cycles of capecitabine-based chemotherapy (cycle is every 3 weeks) in addition to 200 mg of oral celecoxib twice daily for 14 days of the 3-week cycle. At baseline and after the 6th chemotherapy cycle the patients' quality of life (QOL) was assessed using hand and foot syndrome (HFS) specific QOL questionnaire (HFS-14). Moreover, blood samples were collected in order to evaluate the serum levels of cyclooxygenase-2 (COX-2), tumour necrosis factor-alpha (TNF-α) and malondialdehyde (MDA). Data was analysed using paired and un-paired t-tests.

RESULTS:

At the end of the study and as compared to control group, celecoxib treated group showed significantly lower incidence of HFS (P = 0.015). Additionally, celecoxib treated group showed significant decline in the serum levels of TNF-α (P = 0.016) and MDA (P = 0.014) which was associated with non-significant difference in the serum level of COX-2 between the two groups (P = 0.476). Celecoxib was safe and well-tolerated throughout the study period.

CONCLUSION:

Celecoxib may represent a potential protective agent against capecitabine induced hand and foot syndrome in patients with colorectal cancer.

2025-12-01·BIOORGANIC & MEDICINAL CHEMISTRY

Virtual screening, synthesis, optimization and anti-inflammatory activity of novel chromones as specific COX-2 inhibitors

Article

作者: Yu, Shuyan ; Zhang, Mengdi ; Wang, Min ; Chen, Jianping ; Wang, Laibing ; Guo, Huiqing ; Ma, Yuheng ; Qin, Meng

In this study, we pioneered the use of SMARTS screening to construct a chromone database, and the Discovery Studio was used to achieve precise molecular docking of COX-2 through LibDock and CDOCKER, and successfully locked 7 hit compounds from the massive chromone library. In cell experiments, Q7 had a significant inhibitory effect on LPS-induced PGE₂ (IC₅₀ = 68.23 ± 8.94 μM) and NO (IC₅₀ = 44.83 ± 2.01 μM) in RAW264.7 cells, and its anti-inflammatory activity was superior to that of the traditional anti-inflammatory agents ibuprofen [IC₅₀(PGE₂) = 246.5 ± 3.8 μM] and L-canavanine [IC₅₀(NO) = 440.0 ± 7.9 μM]. Still, the activity was not as good as that of celecoxib [IC₅₀ (PGE₂) = 0.882 ± 0.021 μM], and the western blot of Q7 further confirmed its targeted inhibition of COX-2. On this basis, the structure of Q7 was optimized by flexible docking design, and 30 Q7 derivatives were synthesized one by one, all of which showed certain anti-inflammatory activities, among which Q7-9 [IC₅₀(PGE₂) = 0.209 ± 0.022 μM, IC₅₀(COX-2) = 0.121 ± 0.010 μM], Q7-25 [IC₅₀(PGE₂) = 0.267 ± 0.017 μM, IC₅₀(COX-2) = 0.228 ± 0.021 μM] and Q7-26 [IC₅₀(PGE₂) = 0.161 ± 0.018 μM, IC₅₀(COX-2) = 0.137 ± 0.004 μM] exhibited anti-inflammatory activity better than celecoxib and had a moderate selectivity index (SI_Q7_-₉ > 826). Q7-28 (IC₅₀ = 0.014 ± 0.001 μM) and Q7-29 (IC₅₀ < 0.0128 μM) had significant inhibitory effects on NO. In addition, by constructing a 3D-QSAR model, the anti-inflammatory structures of chromone and isoflavone molecules for COX-2 and iNOS targets were systematically revealed. This study provided an important reference and basis for the research and development of new chromone non-steroidal anti-inflammatory drugs, and Q7-9 was expected to be a candidate drug with high safety and specific COX-2 inhibitors.

520

项与塞来昔布相关的新闻（医药）

2025-09-13

·肿瘤界

BMJ发表逸仙团队预防卡培他滨所致严重手足综合征新策略

点击蓝字关注我们卡培他滨是临床上广泛使用的口服化疗药物，适用于多种实体瘤的治疗，手足综合征（HFS）是其最常见的不良反应之一，发生率介于29%至73%之间。尽管HFS不会危及生命，但是2/3级HFS会严重影响患者的生活质量，导致患者无法耐受，由于无显著有效且安全的预防方案，临床上“被迫”通过卡培他滨的减量或停药来缓解HFS，影响治疗疗效和患者生存预后。因此，探索安全有效的预防卡培他滨所致的2/3级HFS的策略成为临床亟待解决的难题。严重手足综合征（HFS）例图 2025年9月11日，中山大学孙逸仙纪念医院乳腺肿瘤中心龚畅教授团队联合全国共7家单位，在国际顶尖医学期刊《英国医学杂志》(BMJ)上发表了一项题为“Effect of methylcobalamin on capecitabine induced hand-foot syndrome in patients with HER2 negative early breast cancer: multicentre, double blind, randomised, placebo controlled, phase 3 trial”的重要临床研究成果。该项多中心、随机、双盲、安慰剂对照的III期临床研究证实，口服甲钴胺可显著降低HER2阴性早期乳腺癌患者在卡培他滨辅助强化治疗中2/3级手足综合征的发生率，且未观察到特殊不良反应，为该类患者提供了一种有效且安全的HFS预防新方案。目前，临床上有以使用塞来昔布、外用扶他林软膏和尿素乳膏等预防卡培他滨相关HFS的方法。然而存在一定的局限：长期使用塞来昔布可能增加心血管事件风险；有关扶他林软膏的临床研究对HFS评估不够全面（仅评估手部）；尿素乳膏可减少1级HFS发生，但对2/3级HFS的预防效果尚不明确。以上局限性导致这些药物在卡培他滨所致HFS的预防指南中证据等级和推荐强度均相对有限（最高仅为IIB级）。因此，临床仍需更安全、高效的预防手段。甲钴胺作为维生素B12的一种衍生物，可通过增强细胞外调节蛋白激酶（ERK1/2）和蛋白激酶B（AKT）活性促进神经修复与再生，缓解神经病理性疼痛和感觉异常，改善小纤维神经病变。因此，甲钴胺具备预防卡培他滨所致HFS的潜在可能性。基于这一背景，研究团队牵头开展了临床研究，共纳入234例接受卡培他滨辅助治疗的HER2阴性早期乳腺癌患者，随机分为甲钴胺组（117例）和安慰剂组（117例）。结果显示，甲钴胺组2/3级HFS发生率为14.5%（17例），安慰剂组为29.1%（34例），率差为−14.5%（95%置信区间：−24.9%至−4.1%）。两组其他治疗相关不良事件发生率相近，甲钴胺组为75.2%（88/117），安慰剂组为81.2%（95/117）。未报告甲钴胺特有的不良反应。此外，甲钴胺组因HFS导致卡培他滨减量或停药的比例低于安慰剂组（7.7% vs.13.7%）。在临床实践中，卡培他滨不仅用于HER2阴性早期乳腺癌的辅助强化治疗，还广泛应用在晚期乳腺癌以及其他实体瘤领域（如胃癌、食管癌、结直肠癌等）。本研究为接受卡培他滨抗肿瘤治疗患者的HFS管理提供了新证据，可保障卡培他滨足量足疗程治疗，从而提升治疗效果，保障患者获益，并有望为相关预防指南的更新补充高级别临床依据。研究摘要图通讯作者简介龚畅教授中山大学孙逸仙纪念医院乳腺外科教授/主任医师、外科学博士、博士生导师、乳腺诊断专科主任；任中国抗癌协会乳腺癌整合防筛专委会常委、中国抗癌协会乳腺癌专委会委员、中国女医师协会乳腺专委会常委、中国女医师协会临床肿瘤专委会委员、中国医师协会医学遗传医师分会肿瘤医学学组组员。主持科技部国家重点研发计划（课题组长）1项、科技部重大专项（课题组长）1项、国家自然科学基金7项，省部级基金7项。CSCO基金2项。入选科技部、教育部、广东省杰青等人才项目5项。主编人卫出版社专著《组织标记在乳腺疾病精准诊疗中的应用》。研究成果获广东省科技进步二等奖（第一完成人），并被中国年轻乳腺癌诊疗专家共识以及包括研究生教材《疾病学基础》《肿瘤学》在内的17本参与编写的专著引用。获专利12项, 开发软件2项。以通讯作者（含共同）在BMJ，Molecular Cancer，Advanced Science，Cell Reports Medicine，Med，Oncologist等杂志发表论文35篇，总引用近3000次，高被引论文4篇。声明：本文由“肿瘤界”整理与汇编，欢迎分享转载，如需使用本文内容，请务必注明出处。来源：中山大学孙逸仙纪念医院原标题：《BMJ》发表逸仙团队预防卡培他滨所致严重手足综合征新策略编辑：lagertha 审核：南星

临床结果临床3期

2025-09-12

·ioncology

英国医学杂志叒发中国乳腺癌研究

点击蓝字，关注我们 HER2阴性早期乳腺癌大约占全部乳腺癌的80%至85%，化疗后卡培他滨辅助治疗可显著改善此类患者生存结局。不过，手足综合征是限制卡培他滨剂量的常见不良反应，分为1至3级，发生于29%至73%的患者，特征为手掌和足底出现红斑、神经疼痛、水肿和感觉异常，逐渐发展为脱屑、糜烂、溃疡和水疱。虽然不超过3级的手足综合征并不致命，但是严重影响生活质量，并且通常需要减少或停止卡培他滨治疗，这将影响剂量强度和整体治疗效果。虽然维生素B6、塞来昔布、尿素乳膏已被研究用于预防卡培他滨相关手足综合征，但是维生素B6并未显著降低手足综合征风险，尿素乳膏预防2级或3级手足综合征的作用仍不确定，塞来昔布由于心血管安全问题而长期用药受限导致指南推荐级别相对较低。因此，迫切需要更有效、更安全的治疗方案预防HER2阴性早期乳腺癌患者卡培他滨辅助治疗发生2级或3级手足综合征。既往研究表明，小纤维神经病变可能是卡培他滨诱发手足综合征手掌足底神经疼痛和感觉异常的潜在病因。钴胺素（维生素B12）活性形式之一甲钴胺问世于1963年，通过甲基化循环促进神经突生长和神经元存活可缓解神经疼痛和感觉异常，临床常用于治疗维生素B12缺乏所致巨幼红细胞贫血、糖尿病周围神经病变和化疗所致神经毒性反应，已于2018年进入《国家基本药物目录》，目前京东、美团、饿了么的零售价格每盒（0.5毫克×20片）仅几元至几十元。2013年12月至2015年2月，山东大学附属山东省立医院对80例胃癌、结直肠癌或乳腺癌患者大剂量维生素B6±甲钴胺防治卡培他滨所致手足综合征进行随机比较，结果发现可减少发生率、延长发生时间。2017年8月至2018年10月，南方医科大学南方医院51例晚期乳腺癌患者回顾分析表明，甲钴胺对卡培他滨所致手足综合征有防治作用。2018年1月至2020年1月，厦门大学附属妇女儿童医院对176例卡培他滨化疗女性乳腺癌患者维生素B6±甲钴胺防治卡培他滨所致手足综合征进行随机比较，结果发现能够有效降低发生率，提高生活能力及生活质量。那么，甲钴胺能否降低HER2阴性早期乳腺癌卡培他滨辅助治疗患者手足综合征风险？ 2025年9月11日，国际四大医学期刊之一、英国医学会官方期刊《英国医学杂志》在线发表中山大学孙逸仙纪念医院、中山大学公共卫生学院、中山大学肿瘤防治中心、肇庆市第一人民医院、广州医科大学第一附属医院、北京大学深圳医院、深圳市前海蛇口自贸区医院、东莞市人民医院、广州医科大学第二附属医院的2020-KY-007研究报告，首次对甲钴胺预防HER2阴性早期乳腺癌卡培他滨辅助治疗患者手足综合征的有效性和安全性进行多中心安慰剂双盲随机对照。这是继北京PHILA研究、上海BCTOP-T-A01研究之后，《英国医学杂志》创刊185年以来第三次发表中国乳腺癌随机对照临床研究，也是第一次发表中国乳腺癌药物不良反应干预研究。 2020-KY-007 (NCT05165069): The Efficacy and Safety of Mecobalamin in the Prevention of Capecitabine Induced Hand Foot Syndrome Official Title: The Efficacy and Safety of Mecobalamin in the Prevention of Capecitabine Induced Hand Foot Syndrome in Breast Cancer Patients: a Multicenter, Phase III, Randomized, Double-blind, Controlled Trial 该研究于2022年1月至2024年2月在中国七家医院入组年龄18～75岁经病理证实为HER2阴性早期乳腺癌计划术后卡培他滨辅助治疗女性234例，按1比1随机分为两组，每天三次口服甲钴胺0.5毫克或安慰剂，疗程最长24周。主要终点为全部患者卡培他滨治疗期间首次≥2级手足综合征发生率。结果，甲钴胺组（117例）与安慰剂组（117例）相比： ≥2级手足综合征发生率：14.5%比29.1%（风险差：-14.5%，95%置信区间：-24.9%至-4.1%；单侧P=0.003）手足综合征所致卡培他滨减量或停药比例：7.7%比13.7%（风险差：-6.0%，95%置信区间：-13.9%至1.9%）其他不良事件发生率：75.2%比81.2% 未见甲钴胺相关不良事件根据亚组分析，无论患者年龄、绝经状态、乳腺癌分期、激素受体、既往化疗方案、卡培他滨起始剂量如何，结果都有利于甲钴胺。因此，该研究结果表明，HER2阴性早期乳腺癌术后卡培他滨辅助治疗女性，口服甲钴胺与安慰剂相比，≥2级手足综合征发生率显著降低14.5%，手足综合征所致卡培他滨减量或停药比例降低6%，其他不良事件发生率相似，而且未见意外安全问题，支持对此类患者用甲钴胺预防卡培他滨相关严重手足综合征。该研究还表明，中国乳腺癌高水平研究已经从生存数量拓展至生存质量。 BMJ. 2025 Sep 11;390:e084290. IF: 42.7 Effect of methylcobalamin on capecitabine induced hand-foot syndrome in patients with HER2 negative early breast cancer: multicentre, double blind, randomised, placebo controlled, phase 3 trial. Xia Y, Zhu Y, Ling L, Xu F, Yang Y, Ye J, Tan W, Chen Z, Liu Q, Wei W, Zhang J, Zhang A, Zhang L, Song E, Gong C. Sun Yat-sen Memorial Hospital, Sun Yat-sen University, Guangzhou, China; School of Public Health, Sun Yat-sen University, Guangzhou, China; Sun Yat-sen University Cancer Centre, Guangzhou, China; The First People's Hospital of Zhaoqing, Zhaoqing, China; The First Affiliated Hospital of Guangzhou Medical University, Guangzhou, China; Peking University Shenzhen Hospital, Shenzhen, China; Shenzhen Qianhai Shekou Free Trade Zone Hospital, Shenzhen, China; Dongguan People's Hospital, Dongguan, China; The Second Affiliated Hospital of Guangzhou Medical University, Guangzhou, China. OBJECTIVE: To evaluate whether methylcobalamin could effectively and safely prevent hand-foot syndrome in patients with human epidermal growth factor receptor 2 (HER2) negative early breast cancer receiving adjuvant capecitabine treatment. DESIGN: Multicentre, double blind, randomised, placebo controlled, phase 3 trial. SETTING: Seven hospitals in China between January 2022 and February 2024. PARTICIPANTS: Women aged 18-75 years with pathologically confirmed HER2 negative early breast cancer who were scheduled to receive adjuvant capecitabine treatment. INTERVENTIONS: Eligible patients were randomly assigned in a 1:1 ratio to receive methylcobalamin at a dose of 0.5 mg orally, three times daily, or a placebo for a maximum of 24 weeks. MAIN OUTCOME MEASURES: The primary endpoint was the incidence of grade ≥2 hand-foot syndrome occurring for the first time during capecitabine treatment in the intention-to-treat analysis. RESULTS: 234 patients were randomly assigned to receive methylcobalamin (n=117) or placebo (n=117) and were included in the intention-to-treat and safety analysis. Grade ≥2 hand-foot syndrome occurred in 17 (14.5%) of 117 patients in the methylcobalamin group and 34 (29.1%) of 117 patients in the placebo group (risk difference -14.5%, 95% confidence interval -24.9% to -4.1%; one sided P value=0.003). The rate of reduction or discontinuation of capecitabine treatment because of hand-foot syndrome was 7.7% (9 of 117) in the methylcobalamin group and 13.7% (16 of 117) in the placebo group (risk difference -6.0%, 95% confidence interval -13.9% to 1.9%). The two groups showed similar incidence of any other adverse events (88 (75.2%) in the methylcobalamin group and 95 (81.2%) in the placebo group). No methylcobalamin specific adverse events were observed. CONCLUSIONS: Oral methylcobalamin significantly lowered the severity of hand-foot syndrome by reducing the incidence of grade ≥2 symptoms without unexpected safety concerns in women with HER2 negative early breast cancer who were receiving adjuvant capecitabine treatment. The findings support the use of methylcobalamin to prevent capecitabine associated severe hand-foot syndrome in this patient population. TRIAL REGISTRATION: ClinicalTrials.gov NCT05165069 PMID: 40935571 DOI: 10.1136/bmj-2025-084290 （来源：SIBCS）声明凡署名原创的文章版权属《肿瘤瞭望》所有，欢迎分享、转载。本文仅供医疗卫生专业人士了解最新医药资讯参考使用，不代表本平台观点。该等信息不能以任何方式取代专业的医疗指导，也不应被视为诊疗建议，如果该信息被用于资讯以外的目的，本站及作者不承担相关责任。

临床结果临床研究诊断试剂

2025-09-10

·PRNewswire

NeuroSense's Drug Candidate Shows Early Signals of Benefit in Alzheimer's Patient-Derived Neurons

Initial Phase 2 RoAD trial results demonstrate improvements in brain-cell connectivity and health, with a favorable safety profile CAMBRIDGE, Mass., Sept. 10, 2025 /PRNewswire/ -- NeuroSense Therapeutics Ltd. (Nasdaq: NRSN) ("NeuroSense"), a late-clinical stage biotechnology company developing novel treatments for severe neurodegenerative diseases, today announced positive initial results from its collaboration with NeuroKaire in the ongoing RoAD Phase 2 clinical trial evaluating PrimeC for Alzheimer's disease (AD). Using NeuroKaire's proprietary technology to generate brain cells from each patient's blood, analysis of samples from clinically characterized AD patients demonstrated that: PrimeC treatment enhanced neuroplasticity, a key feature in supporting brain health and function and underlying memory formation and retention. No treatment-related toxicity was observed, demonstrating the safety of PrimeC combination. NeuroSense's RoAD study is a randomized, double-blind, placebo-controlled Phase 2 trial enrolling mild-to-moderate AD patients, designed to evaluate safety, efficacy, and biological activity of PrimeC over 12 months. These results provide an early, patient-specific view of how PrimeC may affect disease-relevant human neurons, reinforcing the program's mechanistic rationale and guiding precision development in AD. NeuroKaire's proprietary technology reprograms blood sample cells into induced pluripotent stem cells (iPSCs) and differentiates them into mature human cortical neurons. After validation, neurons are exposed to PrimeC, and advanced high-content imaging using AI-driven analytics quantifies key features of neuronal structure. This generates composite response profiles tied to neuroplasticity, connectivity, and cell health. Alon Ben-Noon, CEO of NeuroSense, stated: "This is exactly the kind of early, decision-enabling signal RoAD was designed to uncover. By integrating NeuroKaire's patient-derived neuron platform with our clinical program, we observed measurable gains in brain-cell connectivity and a favorable safety profile. These findings strengthen PrimeC's mechanistic rationale in Alzheimer's and enable us to focus development with greater precision." Dr. Daphna Laifenfeld, CSO of NeuroKaire, commented: "Our platform is designed to detect subtle, disease-relevant changes in human neurons with the sensitivity modern drug development requires. This collaboration demonstrates how a bench-to-clinic 360° workflow can transform a simple blood draw into actionable, patient-specific insights, accelerating innovation for people living with AD." These results will be presented at the CNS Summit 2025 in Boston, November 2nd – 5th by David Pattison, VP Business Development at NeuroKaire. NeuroSense and NeuroKaire will continue evaluating PrimeC's cellular effects in parallel with clinical outcomes from the RoAD trial, with top-line data expected following study completion. About Alzheimer's Disease Alzheimer's disease (AD) is a progressive neurodegenerative disorder and the leading cause of dementia worldwide, affecting more than 30 million people globally. AD is characterized by memory loss, cognitive decline, and behavioral changes, and currently has no cure. Existing therapies provide only limited symptomatic relief, leaving a significant unmet need for disease-modifying treatments that can slow or halt progression. Given the complexity of AD, approaches that target multiple disease mechanisms simultaneously, such as PrimeC, hold potential to deliver meaningful therapeutic advances for patients and their families. About PrimeC PrimeC, NeuroSense's lead drug candidate, is a novel extended-release oral formulation composed of a unique fixed-dose combination of two FDA-approved drugs: ciprofloxacin and celecoxib. PrimeC is designed to synergistically target several key mechanisms of ALS and AD, that contribute to neuron degeneration, inflammation, iron accumulation and impaired ribonucleic acid ("RNA") regulation to potentially inhibit the progression of ALS and AD. About NeuroKaire NeuroKaire, founded in 2018 by Talia Cohen-Solal, Ph.D., and Daphna Laifenfeld, Ph.D., is developing personalized medicine solutions to optimize treatment for psychiatric and neurological diseases. The company's proprietary AI-powered platform, Stemifai, leverages stem cell differentiation and machine learning to inform and advance CNS drug development processes. To learn more, follow us on LinkedIn or on Twitter @Genetikaplus. About NeuroSense NeuroSense Therapeutics, Ltd. is a clinical-stage biotechnology company focused on discovering and developing treatments for patients suffering from debilitating neurodegenerative diseases. NeuroSense believes that these diseases, which include amyotrophic lateral sclerosis (ALS), Alzheimer's disease and Parkinson's disease, among others, represent one of the most significant unmet medical needs of our time, with limited effective therapeutic options available for patients to date. Due to the complexity of neurodegenerative diseases and based on strong scientific research on a large panel of related biomarkers, NeuroSense's strategy is to develop combined therapies targeting multiple pathways associated with these diseases. For additional information, we invite you to visit our website and follow us on LinkedIn, YouTube and X. Information that may be important to investors may be routinely posted on our website and these social media channels. Forward-Looking Statements This press release contains "forward-looking statements" that are subject to substantial risks and uncertainties. All statements, other than statements of historical fact, contained in this press release are forward-looking statements. Forward-looking statements contained in this press release may be identified by the use of words such as "anticipate," "believe," "contemplate," "could," "estimate," "expect," "intend," "seek," "may," "might," "plan," "potential," "predict," "project," "target," "aim," "should," "will" "would," or the negative of these words or other similar expressions, although not all forward-looking statements contain these words. Forward-looking statements are based on NeuroSense Therapeutics' current expectations and are subject to inherent uncertainties, risks and assumptions that are difficult to predict and include statements regarding the results of the ongoing RoAD Phase 2 clinical trial evaluating PrimeC for Alzheimer's disease (AD). Further, certain forward-looking statements are based on assumptions as to future events that may not prove to be accurate. The future events and trends may not occur and actual results could differ materially and adversely from those anticipated or implied in the forward looking statements. These risks include the risk that final results of the ongoing RoAD Phase 2 clinical trial evaluating PrimeC for Alzheimer's disease (AD) will not be consistent with its positive initial results, the risk of a delay in submission by the Company of its regulatory dossier, that regulatory approvals for PrimeC will be delayed or not obtained in Canada or elsewhere; unexpected R&D costs or operating expenses, insufficient capital to complete development of PrimeC, a delay in the reporting of additional results from PARADIGM clinical trial, the timing of expected regulatory and business milestones, risks associated with meeting with the FDA and Health Canada to determine the best path forward following the results from PARADIGM clinical trial, including a delay in any such meeting; the potential for PrimeC to safely and effectively target ALS; preclinical and clinical data for PrimeC; the uncertainty regarding outcomes and the timing of current and future clinical trials; timing for reporting data; the development and commercial potential of any product candidates of Neurosense; the ability of NeuroSense to remain listed on Nasdaq; and other risks and uncertainties set forth in NeuroSense's filings with the Securities and Exchange Commission (SEC). You should not rely on these statements as representing our views in the future. More information about the risks and uncertainties affecting NeuroSense is contained under the heading "Risk Factors" in the Annual Report on Form 20-F filed with the Securities and Exchange Commission on April 4, 2024 and NeuroSense's subsequent filings with the SEC. Forward-looking statements contained in this announcement are made as of this date, and NeuroSense undertakes no duty to update such information except as required under applicable law. Logo: SOURCE NeuroSense WANT YOUR COMPANY'S NEWS FEATURED ON PRNEWSWIRE.COM? 440k+ Newsrooms & Influencers 9k+ Digital Media Outlets 270k+ Journalists Opted In GET STARTED

临床2期临床结果

100 项与塞来昔布相关的药物交易

登录后查看更多信息

外链

KEGG	Wiki	ATC	Drug Bank
D00567	塞来昔布	L01XX33 M01AH01	DB00482

研发状态

批准上市

10 条最早获批的记录,

登录

后查看更多信息

适应症	国家/地区	公司	日期
偏头痛	美国	Scilex Pharmaceuticals, Inc.	2020-05-05
疼痛	日本	Astellas Pharma, Inc.	2011-12-22
牙痛	日本	Viatris Pharmaceutical GK	2011-12-22
滑囊炎	日本	Viatris Pharmaceutical GK	2009-06-17
颈臂综合征	日本	Astellas Pharma, Inc.	2009-06-17
颈臂综合征	日本	Viatris Pharmaceutical GK	2009-06-17
腰痛	日本	Viatris Pharmaceutical GK	2009-06-17
腰痛	日本	Astellas Pharma, Inc.	2009-06-17
肩周炎	日本	Astellas Pharma, Inc.	2009-06-17
肌腱病	日本	Viatris Pharmaceutical GK	2009-06-17
肌腱病	日本	Astellas Pharma, Inc.	2009-06-17
腱鞘炎	日本	Viatris Pharmaceutical GK	2009-06-17
镇痛	日本	Viatris Pharmaceutical GK	2007-01-26
炎症	日本	Viatris Pharmaceutical GK	2007-01-26
幼年特发性关节炎	美国	Upjohn US 2 LLC	2006-12-15
原发性痛经	美国	Upjohn US 2 LLC	2001-10-18
急性疼痛	中国	Viatris Pharmaceuticals LLC	2000-08-01
强直性脊柱炎	奥地利	Upjohn EESV	2000-03-29
强直性脊柱炎	比利时	Upjohn EESV	2000-03-29
强直性脊柱炎	塞浦路斯	Upjohn EESV	2000-03-29

未上市

10 条进展最快的记录,

登录

后查看更多信息

适应症	最高研发状态	国家/地区	公司	日期
先兆偏头痛	申请上市	加拿大	Scilex Holding Co.	2023-12-26
无先兆偏头痛	申请上市	加拿大	Scilex Holding Co.	2023-12-26
光化性角化病	临床3期	美国	Dr. Reddy's Laboratories Ltd. (Russia)	2017-02-14
痛风性关节炎	临床3期	美国	Viatris, Inc.	2008-02-01
痛风性关节炎	临床3期	加拿大	Viatris, Inc.	2008-02-01
痛风性关节炎	临床3期	哥伦比亚	Viatris, Inc.	2008-02-01
痛风性关节炎	临床3期	哥斯达黎加	Viatris, Inc.	2008-02-01
痛风性关节炎	临床3期	墨西哥	Viatris, Inc.	2008-02-01
痛风性关节炎	临床3期	秘鲁	Viatris, Inc.	2008-02-01
痛风性关节炎	临床3期	菲律宾	Viatris, Inc.	2008-02-01

登录后查看更多信息

临床结果

适应症

分期

评价

查看全部结果

研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT00652925 (FDA_CDER) 人工标引	临床3期	幼年特发性关节炎	-	CELECOXIB 3 mg/kg	鹽構獵憲構廠繭餘選艱(築觸願壓鬱艱網選範廠) = 餘範齋獵糧顧艱鏇選觸簾糧簾窪鏇觸憲選顧製 (淵繭遞齋選糧蓋餘壓餘 )	积极	2025-07-29
				CELECOXIB 6 mg/kg	鹽構獵憲構廠繭餘選艱(築觸願壓鬱艱網選範廠) = 構醖積蓋鑰鑰餘衊遞醖簾糧簾窪鏇觸憲選顧製 (淵繭遞齋選糧蓋餘壓餘 )
ASCO2025	N/A	晚期头颈部鳞状细胞癌	97	Dual Oral Metronomic Therapy (OMT)	憲積襯壓顧壓鬱繭獵鏇(廠願壓鬱膚繭憲構顧膚) = 獵顧廠選淵顧獵窪淵壓網簾製鬱糧鹹繭蓋壓獵 (選遞鬱壓廠壓齋鹽餘網 ) 更多	积极	2025-05-30
				Triple Oral Metronomic Therapy (OMT)	憲積襯壓顧壓鬱繭獵鏇(廠願壓鬱膚繭憲構顧膚) = 糧衊網糧襯遞觸憲窪蓋網簾製鬱糧鹹繭蓋壓獵 (選遞鬱壓廠壓齋鹽餘網 ) 更多
NCT04162873 (CTgov)	临床2期	下咽癌 \| 口腔鳞状细胞癌复发 \| 鼻窦癌 ... 更多	13	Quality-of-Life Assessment+celecoxib (Celecoxib Arm)	壓壓憲積齋範願鏇憲構(築齋鏇鹽鏇簾鑰壓窪簾) = 襯窪鏇醖醖選夢蓋窪鏇願構廠廠窪餘衊選憲觸 (範製簾獵壓範製襯糧製, 9.19) 更多	-	2025-02-12
				Placebo (Placebo Arm)	壓壓憲積齋範願鏇憲構(築齋鏇鹽鏇簾鑰壓窪簾) = 鏇鬱鬱衊衊窪鹽範範淵願構廠廠窪餘衊選憲觸 (範製簾獵壓範製襯糧製, 20.04) 更多
NCT05974501 (CTgov)	临床4期	关节置换术并发症 \| 膝关节炎 \| 术后疼痛	84	Lyrica+Ropivacaine+Acetaminophen+Oxycodone+Dexamethasone+Celebrex+Meloxicam (Preoperative Adductor Canal Block Group)	糧壓窪夢選憲製鑰衊範(願鹹繭衊醖範願顧鏇壓) = 製醖鏇遞構簾鏇餘願鑰蓋繭蓋製壓憲範鏇艱簾 (憲窪壓夢積鏇築衊遞積, 膚積憲醖廠築繭遞鏇糧 ~ 製淵廠顧簾艱壓壓簾壓) 更多	-	2025-02-12
				Lyrica+Ropivacaine+Acetaminophen+Oxycodone+Dexamethasone+Celebrex+Meloxicam (Postoperative Adductor Canal Block Group)	糧壓窪夢選憲製鑰衊範(願鹹繭衊醖範願顧鏇壓) = 壓衊壓醖醖選鬱觸網簾蓋繭蓋製壓憲範鏇艱簾 (憲窪壓夢積鏇築衊遞積, 淵築構築齋餘觸鹽範糧 ~ 醖憲築艱淵鹽壓夢顧築) 更多
NCT01150045 (CALGB/SWOG 80702, ASCO_GI2025)	临床3期	III期结肠癌辅助 ctDNA positive	-	Celecoxib + FOLFOX	憲網遞夢襯醖鏇醖築夢(衊繭憲艱觸膚鹹願願憲) = 鏇齋廠餘鏇衊衊糧淵構鏇窪簾遞遞膚選積壓遞 (衊繭窪願觸糧廠觸襯夢 )	积极	2025-01-23
				Placebo + FOLFOX	憲網遞夢襯醖鏇醖築夢(衊繭憲艱觸膚鹹願願憲) = 膚艱獵願築獵襯願顧衊鏇窪簾遞遞膚選積壓遞 (衊繭窪願觸糧廠觸襯夢 )
NCT03643744 (CTgov)	临床1期	光化性角化病	12	Celecoxib 200mg (PDT + Celecoxib)	襯膚觸衊糧鏇壓淵窪壓(鑰糧繭願鏇窪襯鬱衊遞) = 觸蓋繭夢鬱醖鑰醖醖簾積壓廠齋鏇築艱憲鑰簾 (齋糧鬱壓選觸積繭構壓, 107) 更多	-	2024-12-19
				Placebo (PDT + Placebo)	襯膚觸衊糧鏇壓淵窪壓(鑰糧繭願鏇窪襯鬱衊遞) = 醖淵餘壓願鹹範壓齋積積壓廠齋鏇築艱憲鑰簾 (齋糧鬱壓選觸積繭構壓, 19) 更多
NCT04765644 (ASCENT, CTgov)	临床4期	-	44	celecoxib+L-arginine (Celecoxib)	範鑰網窪窪膚積積蓋鏇(憲壓簾膚蓋齋鏇窪醖糧) = 築餘範膚築遞窪觸繭製糧顧蓋獵醖願窪壓獵憲 (糧艱構繭窪鏇艱鏇蓋願, 0.35) 更多	-	2024-10-28
				Placebo+L-arginine + placebo (Placebo)	範鑰網窪窪膚積積蓋鏇(憲壓簾膚蓋齋鏇窪醖糧) = 選窪鬱衊蓋餘獵觸衊顧糧顧蓋獵醖願窪壓獵憲 (糧艱構繭窪鏇艱鏇蓋願, 0.33) 更多
NCT03859024 (CTgov)	临床4期	尿道狭窄 \| 术后疼痛	48	Acetaminophen+Oxycodone+Ibuprofen 800 mg (Standard Protocol)	觸遞網網觸憲鬱鑰壓窪(壓觸鏇獵淵鹽願壓鬱鏇) = 鏇簾顧膚製衊繭壓艱醖膚夢蓋淵蓋構鬱遞顧積 (構衊繭構夢範繭蓋蓋顧, 艱顧醖選蓋鏇糧淵齋蓋 ~ 獵鏇壓夢遞繭艱襯衊鏇) 更多	-	2024-09-19
				Acetaminophen+Oxycodone+Dexamethasone+Ibuprofen 800 mg+Bupivacaine+celebrex+Gabapentin (Enhanced Recovery Protocol)	觸遞網網觸憲鬱鑰壓窪(壓觸鏇獵淵鹽願壓鬱鏇) = 網鬱衊窪遞製襯糧鑰壓膚夢蓋淵蓋構鬱遞顧積 (構衊繭構夢範繭蓋蓋顧, 積積夢繭膚築膚膚範壓 ~ 淵鹹選蓋製築膚醖願醖) 更多
NCT05077969 (CTgov)	临床2期	SARS-CoV-2 急性呼吸道疾病	4	Famotidine+celecoxib (Group 1 (Study Product))	獵鬱積糧夢簾壓鹽鑰窪 = 願構觸顧齋壓築選繭糧餘積衊廠顧鹽壓醖鏇鹽 (糧積簾觸蓋鹹積憲鏇窪, 膚顧壓鑰網廠糧憲積鑰 ~ 鏇製觸蓋鑰艱蓋憲鏇構) 更多	-	2024-07-09
				Placebo (Group 2 (Reference Therapy))	獵鬱積糧夢簾壓鹽鑰窪 = 簾範範獵艱鹽鹽醖鏇遞餘積衊廠顧鹽壓醖鏇鹽 (糧積簾觸蓋鹹積憲鏇窪, 齋鬱網選鹹構獵憲繭醖 ~ 蓋獵築製鏇鹽蓋簾積夢) 更多
NCT04015908 (CTgov)	临床4期	-	100	Pregabalin+Acetaminophen+Oxycodone+celecoxib (Multi-modal)	範淵衊蓋憲糧醖廠廠鹽(膚蓋醖糧襯鑰艱鏇廠憲) = 憲襯艱繭襯網夢顧衊窪範範齋顧繭觸壓蓋製鏇 (窪鏇獵憲願遞壓憲鏇鬱, 淵糧襯範衊構觸範膚遞 ~ 醖糧膚醖餘遞壓製鬱廠) 更多	-	2024-07-08
				Percocet (Control)	範淵衊蓋憲糧醖廠廠鹽(膚蓋醖糧襯鑰艱鏇廠憲) = 鏇糧觸襯鹽鹹製遞蓋淵範範齋顧繭觸壓蓋製鏇 (窪鏇獵憲願遞壓憲鏇鬱, 糧製夢顧築蓋觸繭淵觸 ~ 齋築夢艱構觸構醖網衊) 更多