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更新于：2026-09-02

Fluorouracil

氟尿嘧啶

更新于：2026-09-02

概要

基本信息

药物类型

小分子化药

别名

5-fluoro-1H-pyrimidine-2,4-dione、5-Fluoropyrimidine-2,4-dione、5-Fluorouracil

+ [38]

靶点

TYMS

作用方式

抑制剂

作用机制

TYMS抑制剂(胸苷酸合成酶抑制剂)

治疗领域

肿瘤消化系统疾病内分泌与代谢疾病+ [10]

在研适应症

胰腺腺癌胃腺癌食管癌+ [93]

非在研适应症

腺泡细胞癌胆道腺癌转移性腺癌+ [120]

原研机构

Spectrum Pharmaceuticals, Inc.

在研机构

Lineberger Comprehensive Cancer Center

Kyowa Kirin Co., Ltd.

National Cancer Institute

+ [24]

非在研机构

Wake Forest School of Medicine

The Cleveland Clinic Foundation

Mayo Clinic

+ [49]

权益机构

Dr. Reddy's Laboratories Ltd.

Hill Dermaceuticals, Inc.

Extrovis AG

+ [1]

最高研发阶段批准上市

首次获批日期

美国 (1962-04-25),

乳腺癌结直肠癌胰腺癌+ [1]

最高研发阶段(中国)批准上市

特殊审评孤儿药 (美国)

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结构/序列

分子式C4H3FN2O2

InChIKeyGHASVSINZRGABV-UHFFFAOYSA-N

CAS号51-21-8

关联

3,015

项与氟尿嘧啶相关的临床试验

NCT07748611

/ Not yet recruiting临床2期IIT

SMART-PANC: SMAD4 Tailored Neoadjuvant Therapy for Pancreatic Cancer, A Phase ll Non-Randomized, Single Center Pilot Study

This phase II trial tests the impact of using SMAD4-mutant status to personalize chemotherapy in treating patients with pancreatic ductal adenocarcinoma (PDAC) that can be removed by surgery (resectable) or that may be between resectable and unresectable (borderline resectable) before undergoing surgery (neoadjuvant). PDAC is one of the most aggressive and fastest growing tumors. SMAD4, a tumor suppressor gene, acts like a brake on cell growth and helps to prevent tumor cells from growing. However, losing it makes the tumor more aggressive and often resistant to standard of care (SOC) treatments regimens, such as gemcitabine with nab-paclitaxel and fluorouracil, leucovorin, irinotecan, and oxaliplatin (FOLFIRINOX). Gemcitabine is a chemotherapy drug that blocks the cells from making deoxyribonucleic (DNA) and may kill tumor cells. Paclitaxel is in a class of medications called antimicrotubule agents. It stops tumor cells from growing and dividing and may kill them. Nab-paclitaxel is an albumin-stabilized nanoparticle formulation of paclitaxel which may have fewer side effects and work better than other forms of paclitaxel. Fluorouracil, a type of antimetabolite, stops cells from making DNA and it may kill tumor cells. Leucovorin is a form of folic acid. It is a type of chemoprotective agent and a type of chemosensitizing agent. Irinotecan is in a class of antineoplastic medications called topoisomerase I inhibitors. It blocks a certain enzyme needed for cell division and DNA repair and may kill tumor cells. Oxaliplatin is in a class of medications called platinum-containing antineoplastic agents. It damages the cell's DNA and may kill tumor cells. Instead of a one-sized fits all treatment approach with SOC therapies, matching therapy based on SMAD4 mutation status may use this specific genetic weakness against the tumor. This approach to neoadjuvant therapy may dramatically alter the path of treatment and improve outcomes, including complete resection rates, in patients with resectable or borderline resectable PDAC.

开始日期2027-02-03

申办/合作机构

Northwestern University

[+1]

NCT07271355

/ Not yet recruiting临床3期IIT

Investigation of Mitomycin C PIPAC - FOLFIRI Combination for Unresectable Appendiceal or Colorectal Peritoneal Metastases Treatment (IMPACT): A Multicenter, Randomized, Open-Label, Phase 3 Trial

This phase III trial studies how well pressurized intraperitoneal aerosolized chemotherapy (PIPAC) with mitomycin works versus (vs) standard chemotherapy (leucovorin calcium, fluorouracil, and irinotecan hydrochloride [FOLFIRI regimen] plus bevacizumab) in treating patients with appendix or colorectal cancer that cannot be removed by surgery (unresectable) and has spread from where it first started (primary site) to the abdominal cavity (peritoneal metastases). PIPAC is a new therapeutic approach that is minimally invasive, does not require surgery (laparotomy), and can be frequently repeated. Chemotherapy is delivered as a pressurized mist directly inside the abdominal cavity (peritoneum) during a minimally invasive surgery called a laparoscopy. The pressure helps the chemotherapy absorb into the cancer tissue and spread more evenly. Mitomycin is an antibiotic used as a chemotherapy drug. It stops or slows the growth of cancer cells and other rapidly growing cells by damaging their deoxyribonucleic acid (DNA). Standard chemotherapy drugs, such as those in the FOLFIRI regimen, are given via infusion into a vein (intravenously), and work in different ways to stop the growth of tumor cells, either by killing the cells, by stopping them from dividing, or by stopping them from spreading. Another standard intravenous drug, bevacizumab, is in a class of medications called antiangiogenic agents. It works by stopping the formation of blood vessels that bring oxygen and nutrients to tumor. This may slow the growth and spread of tumor. Giving mitomycin via PIPAC in combination with the standard FOLFIRI regimen, with or without bevacizumab, may work better than standard FOLFIRI plus bevacizumab alone in treating patients with unresectable appendix or colorectal cancer with peritoneal metastases.

开始日期2026-10-01

申办/合作机构

City of Hope National Medical Center

[+1]

NCT07793942

/ Not yet recruiting临床2期

A Phase 2, Open-label Clinical Study to Evaluate the Safety and Efficacy of MK-2010 as Monotherapy and in Combination

Researchers are looking for new ways to treat certain types of advanced solid tumors. Solid tumors are cancers mostly in organs and tissues in the body, not in the blood or other fluids. Advanced means the cancer has spread nearby or to other parts in the body and cannot be removed with surgery.
In this trial, researchers want to learn if the trial medicine called MK-2010, given alone or with other treatments, can treat advanced solid tumors. MK-2010 is designed to help the immune system fight cancer.
The goals of this trial are to learn:
* About the safety of MK-2010 as monotherapy and in combinations and if participants tolerate them. Tolerate means participants will receive trial treatment unless they need to stop it due to health problems.
* How many participants who receive MK-2010 as monotherapy and in combination respond to treatment. Respond means the cancer gets smaller or goes away.

开始日期2026-09-29

申办/合作机构

Merck Sharp & Dohme LLC

100 项与氟尿嘧啶相关的临床结果

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100 项与氟尿嘧啶相关的转化医学

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100 项与氟尿嘧啶相关的专利（医药）

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62,080

项与氟尿嘧啶相关的文献（医药）

2027-01-01·JOURNAL OF ETHNOPHARMACOLOGY

Phytochemical basis and mechanistic insight of Swertia macrosperma in treating 5-fluorouracil-induced diarrhea

Article

作者: Ruan, Jingya ; Wang, Tao ; Yan, Wenjia ; Zhang, Yi ; Li, Huimin ; Cheng, Jiaming ; Geng, Qianqian ; Wu, Yijin ; Li, Fei ; Cao, Xiaoyan

ETHNOPHARMACOLOGICAL RELEVANCE:

5-Fluorouracil (5-FU)-induced diarrhea severely impacts chemotherapy outcomes. Swertia macrosperma (C. B. Clarke) C. B. Clarke in Hook. f. is traditionally used for diarrhea, yet its efficacy and mechanism remain unclear.

AIM OF THE STUDY:

This study first investigated the anti-diarrheal potential of 70% ethanol extract from S. macrosperma (SME).

MATERIALS AND METHODS:

In a 5-FU-induced mouse model, SME was evaluated for its effects on diarrhea severity, weight loss, intestinal histopathology, oxidative stress (MDA, SOD, GSH), inflammation (TNF-α, IL-6, COX-2, iNOS), and tight junction proteins (Claudin-1, Occludin). Phytochemical investigation (including isolation, structural elucidation, and UPLC-MS quantification), IEC-6 cell-based mechanistic studies, network pharmacology, and Western blot analysis (for PI3K-AKT pathway) were performed.

RESULTS:

SME significantly alleviated weight loss, diarrhea severity, and intestinal histopathological damage. It inhibited oxidative stress and inflammation while upregulating tight junction proteins, thereby protecting intestinal barrier integrity. Phytochemical investigation yielded 57 compounds, including three new isolates (swemacronosides A-C) and 37 first-time reports for this species. UPLC-MS quantification identified compounds 7, 8, and 23 as the predominant constituents. Mechanistic studies indicated that SME ameliorated diarrhea symptoms in mice via the PI3K-AKT signaling pathway. Western blot confirmed that compounds 7 and 23 significantly restored the 5-FU-induced downregulation of PI3K expression and the p-AKT/AKT ratio.

CONCLUSION:

S. macrosperma ameliorates 5-FU-induced diarrhea, and the mechanism potentially involves the PI3K-AKT pathway. However, under the present experimental conditions, it did not significantly reverse 5-FU-induced thymic and splenic atrophy. These findings provide a scientific basis for clinical application and offer potential chemical markers for future quality control studies of S. macrosperma.

2026-12-31·Gut microbes reports

Comparative preventive effects of probiotic and postbiotic preparations of Lacticaseibacillus rhamnosus L156.4 and GG in a 5-FU-induced mucositis model

Article

作者: Figueiredo Siqueira, Milca da Silva ; Pires, Luiz Octávio ; Elias Moreira Júnior, Renato ; Freitas, Andria dos Santos ; Cardoso, Valbert Nascimento ; Guimarães Sousa, Eduarda ; Lima Barroso, Fernanda Alvarenga ; Souza, Renan Pedra de ; Antunes Fernandes, Simone Odília ; Munis Campos, Gabriela ; Ferrary Américo, Monique ; Viegas Santos, Rhayane Cristina ; Santos, Tulio Marcos ; Brunialti Godard, Ana Lucia ; Azevedo, Vasco ; Silva Quaresma, Ludmila ; Gomes, Gabriel Camargos ; Guédon, Eric ; Carvalho, Rodrigo Dias de Oliveira ; Lima de Jesus, Luís Claúdio ; Ferreira, Enio ; Canário Viana, Marcus Vinícios ; Le Loir, Yves

Intestinal mucositis is a debilitating side effect of chemotherapy, characterized by epithelial damage, inflammation, and microbial dysbiosis, that significantly impairs patients' quality of life. This study evaluated the therapeutic potential of Lacticaseibacillus rhamnosus L156.4 in its live, heat-inactivated, and supernatant forms, compared to the reference strain L. rhamnosus GG (LGG), in a murine model of 5-fluorouracil (5-FU)-induced mucositis. Preventive treatment with live L156.4 significantly reduced mucositis-induced intestinal damage, preserving villus length, crypt depth, and goblet cell numbers, thereby supporting barrier integrity. In contrast, heat-inactivated and supernatant forms provided only limited protection. Both live L156.4 and LGG reduced myeloperoxidase activity and downregulated inflammatory markers such as Il1b and Nfkb1, confirming anti-inflammatory effects. They also modulated tight junction-related gene expression with L156.4 showing strong induction of Muc2, suggesting enhanced epithelial protection. Fecal microbiota analysis showed that, whereas LGG restored the loss of bacterial diversity and evenness induced by 5-FU, L156.4 primarily modulated microbiota composition by restoring the abundance of specific phyla and genera. Overall, our findings identify L156.4 as a promising probiotic candidate, with effects comparable to and complementarity with LGG, for mitigating chemotherapy-induced mucositis. Further studies are required to assess dose effects and long-term safety.

2026-12-31·ANNALS OF MEDICINE

Comparative efficacy of intralesional therapies for keloid scars: a network meta-analysis

Review

作者: Bentley, Alexa ; Romano, Candela ; Sanchez Cruz, Camila ; Perozo, Karla ; de Araujo, William Matheus ; Calderon Martinez, Ernesto ; Medina, Jose ; Magallanes Bajana, Angelo ; Ríos, Christopher Romero ; Mohamed Khalil, Malaz El Zubair

BACKGROUND:

Keloids are pathological scars causing pain, pruritus, and emotional distress. While common treatments exist, emerging options such as insulin and botulinum toxin A (BTX-A) are underrepresented in comparative analyses. This network meta-analysis (NMA) aimed to evaluate the efficacy and safety profiles of various intralesional therapies for keloid scars.

METHODS:

A PRISMA-guided search across seven databases was conducted on July 2025 and preregistered on PROSPERO (CRD420251088758). Included studies were randomized, non-randomized, and crossover trials of intralesional therapies. Pairwise and NMA were conducted for efficacy (keloid size/volume reduction), recurrence, and safety (adverse effects). Treatment rankings were based on surface under the cumulative ranking curve (SUCRA) scores. Statistical significance was set at (p < 0.05).

RESULTS:

From 51 studies (3234 participants, 23 interventions), 5-fluorouracil (5-FU) + corticoids significantly improved keloid reduction compared to corticoids alone (RR = 1.59; 95% CI: 1.31-1.92; p < 0.01), with 5-FU + corticoids + YAG:Laser (RR = 2.73; 95% CI: 1.36-5.48; p < 0.01) showing an even greater effect. SUCRA values indicated that 5-FU + corticoids + YAG:Laser (0.95), vitamin D + platelet rich plasma (0.83), and 5-FU + corticoids (0.78) had the highest probability of effectiveness. For recurrence, no significant differences were found across interventions, suggesting insufficient evidence. Regarding adverse effects, a significant risk reduction was found for BTX-A (RR = 0.29; 95% CI: 0.09-0.95; p = 0.04) and Verapamil (RR = 0.35; 95% CI: 0.14-0.84; p = 0.01) compared to corticoids; others showed no significant effects.

CONCLUSION:

This NMA provides a comparative overview, indicating that combination therapies, most notably 5-FU + corticoids + YAG:Laser, offer the greatest benefit. While data for novel agents (insulin and BTX-A) suggest potential, further research with standardized methodologies and longer-term follow-up is crucial to define optimal treatment algorithms.

3,738

项与氟尿嘧啶相关的新闻（医药）

2026-09-01

·BioBAY

研发动态丨盛迪亚：瑞康曲妥珠单抗单药或联合帕妥珠单抗一线治疗HER2阳性晚期乳腺癌III期临床研究达到主要终点

近日，BioBAY园内企业盛迪亚自主研发的以HER2为靶点的抗体药物偶联物瑞康曲妥珠单抗（SHR-A1811）用于HER2阳性复发或转移性乳腺癌一线治疗的关键Ⅲ期临床研究（研究代号：SHR-A1811-307）预设期中分析显示：两个试验组均达到主要终点PFS，与标准治疗相比显示出统计学显著且具有临床意义的改善。该研究结果表明，瑞康曲妥珠单抗联合或不联合帕妥珠单抗对比多西他赛联合曲妥珠单抗、帕妥珠单抗（THP方案），均可显著延长一线患者无进展生存期（PFS）。公司近期将向国家药品监督管理局药品审评中心递交上市前沟通交流申请。关于SHR-A1811-307研究 SHR-A1811-307研究为一项多中心、随机、开放、阳性对照Ⅲ期临床试验，旨在比较瑞康曲妥珠单抗（SHR-A1811）联合或不联合帕妥珠单抗对比多西他赛联合曲妥珠单抗、帕妥珠单抗（THP）方案在复发/转移阶段未接受过系统性抗肿瘤治疗的HER2阳性乳腺癌患者中的有效性和安全性。本研究由中国人民解放军总医院第五医学中心江泽飞教授、江苏省人民医院殷咏梅教授共同担任主要研究者，全国75家中心共同参与。 SHR-A1811-307研究入组868例受试者，按照1:1:1随机入组，分别接受瑞康曲妥珠单抗单药治疗，瑞康曲妥珠单抗联合帕妥珠单抗治疗，多西他赛联合曲妥珠单抗、帕妥珠单抗治疗。主要研究终点为盲态独立中心审查（BICR）基于RECIST v1.1评估的无进展生存期（PFS）。方案预设的期中分析结果表明，与对照组相比，瑞康曲妥珠单抗联合或不联合帕妥珠单抗均可显著降低患者疾病进展/死亡风险。关于HER2阳性乳腺癌乳腺癌位居全球女性恶性肿瘤发病率与死亡率前列，对女性健康造成了严重威胁。而HER2阳性乳腺癌约占所有乳腺癌的15-20%，抗HER2的药物问世以前，HER2阳性乳腺癌患者的平均生存期仅为阴性患者的一半。抗HER2药物的出现，改善了HER2阳性乳腺癌的病程和治疗结局。然而，在HER2阳性晚期乳腺癌一线治疗中，仍面临药物选择有限、早期耐药频发及不良反应限制用药等困境，临床亟需探索疗效优、耐受性良好的方案。关于瑞康曲妥珠单抗注射用瑞康曲妥珠单抗是恒瑞医药自主研发的以HER2为靶点的抗体偶联药物（ADC），可通过与HER2表达的肿瘤细胞结合并内吞，在肿瘤细胞溶酶体内通过蛋白酶剪切释放毒素，诱导细胞周期阻滞从而诱导肿瘤细胞凋亡。其释放的毒素具有高透膜性，可发挥旁观者杀伤效应。注射用瑞康曲妥珠单抗（商品名：艾维达®）已于2025年5月获批上市，适应症为用于治疗存在HER2（ERBB2）激活突变且既往接受过至少一种系统治疗的不可切除的局部晚期或转移性非小细胞肺癌（NSCLC）成人患者，是国内首个获批用于HER2突变NSCLC患者的中国自主研发抗体偶联药物。2026年3月，瑞康曲妥珠单抗新增乳腺癌适应症，用于治疗既往接受过一种或一种以上抗HER2药物治疗的局部晚期或转移性HER2阳性成人乳腺癌患者。2026年8月，瑞康曲妥珠单抗新增结直肠癌适应症，用于经奥沙利铂、氟尿嘧啶和伊立替康治疗失败的HER2阳性结直肠癌成人患者。截至目前，瑞康曲妥珠单抗已有11项适应症被纳入突破性治疗品种名单。此外，多项瑞康曲妥珠单抗临床研究正在进行，涵盖HER2表达的晚期实体瘤、非小细胞肺癌、乳腺癌、胃或胃食管结合部腺癌、结直肠癌、胆道癌、妇科恶性肿瘤等。 ▌文章来源：盛迪亚责编：于嘉敏审核：任旭推荐阅读研发动态丨茂行生物：靶向B7-H3通用型CAR-T获FDA快速通道认定，加速颅内实体瘤全球开发我国首个采用生物型人工血管重建外周动脉临床研究正式启动彩科生物单分子检测平台在多中心血液AD标志物头对头比较中实力登顶

2026-09-01

·微信

3000万美元落袋！一款国产双抗ADC出海印非7大市场

撰稿｜李秋萩 9月1日，正大天晴表示，其自主研发的潜在同类最佳（BIC）HER2双抗ADC药物TQB2102（rolditamig deuderuxtecan）在治疗HER2低表达复发/转移性乳腺癌中的Ⅲ期临床研究成功，达到预设的主要终点和关键次要终点。由此，其成为全球首个HER2双抗ADC在HER2低表达乳腺癌取得成功的Ⅲ期临床研究。据悉，正大天晴已获得CDE书面同意，将于近期递交该适应症的上市申请。就在8月31日，中国生物制药（01177）发布公告，集团子公司正大天晴与印度第三大制药公司Cipla就TQB2102签订独家授权与供应协议。根据协议，正大天晴授予Cipla在印度、南非及其他五个新兴市场（共计7大高增长国际市场）开发及商业化TQB2102的独家许可。正大天晴有权获得首付款、潜在开发、监管及销售里程碑付款，最高可达1.23亿美元，同时还将获得基于TQB2102年度净销售额的双位数的特许权使用费。这是TQB2102达成的第二项区域授权合作。截至目前，两项合作已累计带来约3000万美元的首付款和里程碑付款。中国生物制药方面向《每日经济新闻》记者表示，TQB2102的首次授权地区也是非欧美的广阔市场。正如中国生物制药执行董事、资深副总裁谢炘在接受动脉网访谈时所说，“BD不是买买买，自研才是根基”“很多时候我们不用主动‘敲门’，只需要让对的人知道我们在坚持做哪些赛道，优质的项目自然就会在合适的时机找上门来”。出海，驶向欧美以外的更广阔世界。 01. 本地化先行，填补新兴市场的需求缺口 2024年至2030年间，全球创新药市场规模将从约1.08万亿美元增长至1.5万亿美元，其中新兴市场的贡献率将有望突破35%。中国生物制药表示，高增长新兴市场区域凭借其庞大的人口基数、快速增长的医疗需求、持续完善的监管与支付体系，有望为创新药收入增长再添动能。底层逻辑上，新兴市场的癌症负担同样沉重，多数地区长期陷入“有市场、无产品、缺指南”的发展困境。从供需层面来看，庞大的人口基数催生了巨大的用药需求，但创新疗法与前沿药物的可及性却远落后于欧美国家。中国生物制药表示，其全球化布局将坚持精细化BD运营，走“高全球化、高本土化”并行的路线，布局东南亚、南亚、中东等广阔市场，携手深耕市场、根基深厚的合作伙伴，把国际先进的治疗理念、诊疗方案与创新产品落地当地，惠及更多患者。遵循这一路线，Cipla将负责授权区域内的本地临床开发、注册申报及商业化，正大天晴将继续负责TQB2102的生产及供应。作为印度第三大制药公司（IQVIA MAT 2026年6月）、南非处方药市场第二大药企（ IQVIA MAT 2026年5月）、按处方量在美国通用吸入剂及定量吸入器市场排名第二（IQVIA MAT 2026年6月），Cipla长期深耕印度、南非、北美及其他新兴市场，在多个协议覆盖国家建立了成熟的注册、医学、市场准入及商业化体系，并与当地医疗卫生专业人士及机构形成广泛合作网络。核心优势在于，Cipla在当地的卓越本地化能力，尤其是市场准入优势，将直接加快TQB2102在授权区域内的临床开发、注册和商业化进程。这意味着，“一次合作、多国辐射”。在南亚市场，印度可作为市场拓展的枢纽原点。印度的药品审批结果在斯里兰卡、尼泊尔、巴基斯坦等周边国家认可度较高、互认效力强，可依托这一优势实现注册资源快速外溢，辐射周边区域市场。同样，在非洲市场，南非生产了非洲约40%的药品，是南部非洲发展共同体（SADC）中唯一广泛符合WHO-GMP标准的国家。这也代表着中国创新药出海的一种新思路：在欧美走“FDA/EMA批准”的高价值路径，在新兴市场则走“借力区域枢纽”的高性价比路径。 02. 创新药及对外授权崛起，医药龙头双链并行作为一家老牌药企，正大天晴从仿制药起步，并成为国内率先向创新药转型的企业之一。2018年，公司自主研发的1类创新药盐酸安罗替尼胶囊上市，至今已获批11个适应症。截至3月底，正大天晴累计获批上市的创新产品已经有近20个，其中包括1类创新药11个。在自研方向，公司已连续4年保持研发投入占总营收超20%，在研项目130多个，其中创新药100多个，数量居于行业前列，形成了“上市一代、储备一代、研发一代”的良性格局。在BD方面，接连并购国内明星biotech药企礼新医药、赫吉亚生物。事实上，创新药对外授权已成为中国生物制药的重要增长引擎——2026年前6个月对外授权收入达9.8亿元，同比增长2101.9%。 2026年中期业绩公告显示，截至6月30日止六个月，中国生物制药录得收入约人民币194.4436亿元，较去年同期增长约10.6%。其中，创新药及对外授权是业绩增长的主要动力——创新药及对外授权之收入约人民币87.8940亿元，占本集团收入约45.2%，较去年同期增长约44.3%。年内，中国生物制药与赛诺菲就全球首创的JAK/ROCK抑制剂罗伐昔替尼达成15.3亿美元合作，后又将自主研发的慢阻肺创新药TQC3721以最高19亿美元授权给阿斯利康，创下近年呼吸领域单产品最高交易纪录。 03. 全球第一大癌症，对应的广泛未满足市场成立于1935年的Cipla，专注于复杂仿制药业务，在全球设有48处生产基地，依托前沿技术平台，生产50余种剂型、1500余款产品，在呼吸、抗逆转录病毒、泌尿、心血管、抗感染及中枢神经系统等治疗领域声誉卓著，业务覆盖全球70余个市场。九十年来，Cipla始终以改变患者生命为使命。2001年，Cipla在非洲率先推出针对HIV╱艾滋病的三联抗逆转录病毒疗法，将日治疗费用降至不足1美元。肿瘤领域，Cipla是印度首家推出常用癌症化疗药物长春碱（Vinblastine）和长春新碱（Vincristin）药物的公司（1984年），目前拥有32种以上药物（57种SKU）用于治疗各种癌症。同时，Cipla拥有印度首家获得FDA批准的肿瘤产品制造设施。对于Cipla而言，他们天然理解创新资产如何在弱支付能力、高需求的市场放量。去年10月，Cipla与礼来达成协议，获得其重磅减重药物穆峰达（Mounjaro，替尔泊肽）在印度的分销权，更新第二品牌 Yurpeak。类似合作模式是，礼来将为Cipla制造并供应Yurpeak，价格将与Mounjaro相同。存在一定差异的是，TQB2102在全球范围内尚未获批上市。1.23亿美元合作总额，足以见得Cipla对其商业化的信心。 TQB2102为一款新一代HER2双表位双特异性抗体药物偶联物（ADC），同时靶向HER2的ECD Ⅱ与ECD Ⅳ结构域，并采用可裂解连接子及拓扑异构酶I抑制剂载荷。基于差异化设计，TQB2102突破了传统HER2单克隆抗体或单靶点ADC的局限，双表位结合模式可增强受体交联及内吞效率，在治疗HER2低表达患者方面具有明确的差异化优势。 TQB2102已获得CDE的三项突破性疗法认定（HER2阳性早期或局部晚期乳腺癌的新辅助治疗；既往经奥沙利铂、伊立替康及氟尿嘧啶类药物治疗失败的HER2 IHC 3+晚期结直肠癌；既往未接受过化疗的不可切除或转移性HER2低表达乳腺癌），正在推进多项Ⅲ期临床研究，涵盖HER2低表达乳腺癌、HER2阳性乳腺癌、结直肠癌及胆道癌等多个癌种。 2025年美国临床肿瘤学会（ASCO）年会上，中国生物制药公布了TQB2102用于HER2低表达晚期乳腺癌的Ib期临床研究结果。在既往接受过多线治疗的患者中，总体客观缓解率（ORR）为53.4%(39/73）。即使在既往接受过ADC治疗并发生疾病进展的患者中，经TQB2102治疗后仍有44.4%达到缓解。安全性方面，间质性肺病（ILD）仅发生1例（2级），发生率为0.55%，远低于同类HER2 ADC。今日公开的多中心Ⅲ期临床研究，研究共纳入543例HER2低表达乳腺癌患者，主要终点为独立评估委员会（IRC）评估的无进展生存期（PFS）。期中分析结果显示，与研究者选择的化疗方案相比，TQB2102组可显著降低HER2低表达乳腺癌疾病进展或死亡风险，PFS在统计学意义和临床意义上均获得显著改善。另一重信心在于，广泛的未满足治疗需求市场。根据WHO国际癌症研究机构（IARC）发布的2020年全球最新癌症负担数据，2020年全球新发乳腺癌达到226万例，首次成为全球第一大癌症，约占每年全球新发癌症的12%。 2022年中国乳腺癌新发病例数约为35.7万例，死亡病例数约为7.5万例，严重危害女性健康。其中，约有45%—55%乳腺癌呈现HER2低表达状态（即HER2 IHC 1+或2+/FISH-）。这类乳腺癌患者构成一个新的亟待改善预后的异质性群体，当前姑息性化疗方案对其临床获益有限且毒性较大，亟需新的治疗手段改善治疗结局。 Nature Medicine发表的《全球185个国家乳腺癌发病率和死亡率的模式与趋势》显示，澳大利亚、新西兰发病率最高，北美和北欧地区次之；南亚地区、中非地区和东非地区最低。美拉尼西亚死亡率最高，年龄标准化发病率（ASMR）为26.8/10万人、西非地区其次，东亚地区死亡最低（6.5/10万人）。这反映了不同地区诊断和治疗之间的差距——乳腺癌终生死亡风险最高的是斐济（1/24）和非洲（1/47）。但死亡率与发病率比值（M:I），低人类发展指数国家高达56%，而极高人类发展指数国家仅为17%，这反映了不同地区诊断和治疗之间的差距。研究指出，在低人类发展指数国家，乳腺癌发病率低但死亡率高，这可归因于诊断延迟（导致晚期病例多）、治疗可及性差（医疗资源匮乏）。研究预测，到2050年，预计乳腺癌新发病例将增加38%，死亡病例将增加68%，在中低收入国家的增长最快。 * 参考资料：每日经济新闻《“有市场、无产品、缺指南”！中国生物制药回应为何牵手Cipla，到印度、南非等7个新兴市场卖抗癌药》动脉新医药《专访中国生物制药，拆解大药厂BD逻辑：买买买背后，自研能力才是根基》 END *封面来源：AI生成秒追创新医药产业动态 ⭐点赞、转发、在看一键三连⭐ 点亮动脉新医药星标不遗漏一手信息推送！专题推荐类器官与器官芯片｜CXO｜iPSC｜CGT｜核药｜上游工具｜多肽｜外泌体｜NASH｜蛋白降解剂｜合成生物学｜AI+新药｜VB思享会｜IPO-财报解读｜新医药对话往期推荐声明：动脉新医药所刊载内容之知识产权为动脉新医药及相关权利人专属所有或持有。未经许可，禁止进行转载、摘编、复制及建立镜像等任何使用。文中如果涉及企业信息和数据，均由受访者向分析师提供并确认。点点赞点分享点喜欢

2026-09-01

·研发客

正大天晴HER2双抗ADC低表达乳腺癌Ⅲ期临床成功，TQB2102上市进程迎重要里程碑

近日，中国生物制药（1177.HK）核心企业正大天晴宣布，其自主研发的HER2双抗ADC新药TQB2102治疗HER2低表达复发/转移性乳腺癌中的Ⅲ期临床研究已完成方案预设的期中分析。经独立数据监查委员会（IDMC）判定，研究成功达到预设的主要终点和关键次要终点。公司已获得国家药品监督管理局药品审评中心（CDE）书面同意，将于近期递交该适应症的上市申请。 PFS显著改善，实现精准治疗突破 TQB2102-III-01研究是一项随机、开放、阳性药物对照、多中心Ⅲ期临床研究，旨在评估注射用TQB2102对比研究者选择的化疗在HER2低表达复发/转移性乳腺癌中有效性和安全性。研究共纳入543例HER2低表达乳腺癌患者，主要终点为独立评估委员会（IRC）评估的无进展生存期（PFS）。期中分析结果显示，与研究者选择的化疗方案相比，TQB2102组可显著降低HER2低表达乳腺癌疾病进展或死亡风险，PFS在统计学意义和临床意义上均获得显著改善。研究成功达到预设的主要终点和关键次要终点。这是全球首个HER2双抗ADC在HER2低表达乳腺癌取得成功的Ⅲ期临床研究，实现了对该人群精准治疗的历史突破，为特定分子分型的乳腺癌患者提供全新的治疗选择。本研究的详细数据后续将在国际学术会议上公布。乳腺癌是全球最常见的女性恶性肿瘤之一。2022年中国乳腺癌新发病例数约为35.7万例，死亡病例数约为7.5万例，严重危害女性健康。其中，约有45%-55%乳腺癌呈现HER2低表达状态（即HER2 IHC 1+或2+/FISH-），这类乳腺癌患者构成一个新的亟待改善预后的异质性群体，当前姑息性化疗方案对其临床获益有限且毒性较大，亟需新的治疗手段改善治疗结局[1，2]。创新设计平衡有效性与安全性作为正大天晴首款ADC药物，TQB2102主要通过三大核心技术突破实现有效性与安全性的平衡优化。其一，双表位靶向：抗体端采用非对称型结构设计，可同时结合HER2的ECD II和ECD IV结构域。这种双表位协同作用不仅能显著提升对肿瘤细胞的选择性与亲和力，还能增强内吞效率，从而提升抗肿瘤活性。其二，可裂解连接子：采用酶裂解型连接子，在进入肿瘤细胞后能高效裂解释放毒素。这一设计保留了“旁观者效应”，扩大了对异质性肿瘤的杀伤范围。其三，适宜的DAR值调控：将药物抗体比（DAR）优化至5.8-6.0，并搭配拓扑异构酶I抑制剂毒素，在保证强效杀伤的同时降低了毒性。这种独特的药物设计突破了传统HER2单抗或单靶ADC的局限性，其受体交联和内吞作用更强，对HER2低表达肿瘤的治疗更具潜在优势。 2025年11月，TQB2102单药用于HER2阳性乳腺癌新辅助治疗的Ⅱ期临床研究结果在国际著名期刊《临床肿瘤学杂志》（Journal of Clinical Oncology，IF 43.4)发表[3]。该项研究由复旦大学附属肿瘤医院邵志敏教授团队领衔，为首个证实双抗HER2 ADC TQB2102在乳腺癌新辅助治疗阶段具有良好疗效和安全性的研究。 2026年5月，TQB2102用于晚期实体瘤的一项临床前及I期临床结果，在线发表于欧洲肿瘤内科学会（ESMO）旗舰期刊《肿瘤学年鉴》（Annals of Oncology，影响因子65.4）。该研究由中山大学肿瘤防治中心徐瑞华院士、王树森教授团队领衔，首次系统公布TQB2102在人体临床研究中的疗效与安全性数据，并同步公开其临床前研究结果，证实TQB2102作为双抗HER2 ADC的差异化特征[4]。多适应症布局惠及更多患者目前，正大天晴正在推进TQB2102的多项Ⅲ期临床研究，涵盖晚期未经化疗的HER2低表达乳腺癌、抗HER2治疗失败的晚期HER2阳性乳腺癌、新辅助治疗HER2阳性乳腺癌、一线治疗HER2阳性晚期乳腺癌、后线治疗HER2阳性晚期胆道癌，以及经奥沙利铂、伊立替康、氟尿嘧啶类药物治疗失败的HER2阳性晚期结直肠癌等。正大天晴将进一步加速该产品上市进程，早日为广大肿瘤患者群体带来全新的治疗选择。参考文献：[1] Louis Fehrenbacher, et al. NSABP B-47/NRG Oncology Phase III Randomized Trial Comparing Adjuvant Chemotherapy With or Without Trastuzumab in High-Risk Invasive Breast Cancer Negative for HER2 by FISH and With IHC 1+ or 2. J Clin Oncol. 2020 Feb 10;38(5):444-453.[2] Howard A Burris 3rd, et al. Phase II study of the antibody drug conjugate trastuzumab-DM1 for the treatment of human epidermal growth factor receptor 2 (HER2)-positive breast cancer after prior HER2-directed therapy. J Clin Oncol. 2011 Feb 1;29(4):398-405.[3] Li J, Zhang W, Zeng X, et al. Efficacy and Safety of Neoadjuvant TQB2102 in Locally Advanced or Early Human Epidermal Growth Factor Receptor 2-Positive Breast Cancer: A Randomized, Open-Label, Multicenter, Phase II Trial. J Clin Oncol. 2026 Jan;44(1):20-30.[4] Ruan DY, Lin SY, Huang JJ, et al. Preclinical characterization and phase 1 results of TQB2102, a first-in-class HER2 biparatopic antibody-drug conjugate, in patients with advanced solid tumors. Ann Oncol. 2026.

100 项与氟尿嘧啶相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D00584	氟尿嘧啶	L01BC02	DB00544

研发状态

批准上市

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
胰腺腺癌	美国	Avyxa Pharma LLC	2026-02-20
食管癌	日本	Kyowa Kirin Co., Ltd.	2021-11-25
肠肿瘤	日本	Kyowa Kirin Co., Ltd.	2018-09-21
胆道癌	巴西	Libbs Farmacêutica Ltda.	2007-01-22
膀胱癌	巴西	Libbs Farmacêutica Ltda.	2007-01-22
结肠癌	巴西	Libbs Farmacêutica Ltda.	2007-01-22
胆囊肿瘤	巴西	Libbs Farmacêutica Ltda.	2007-01-22
肝细胞癌	巴西	Libbs Farmacêutica Ltda.	2007-01-22
直肠癌	巴西	Libbs Farmacêutica Ltda.	2007-01-22
头颈部肿瘤	日本	Kyowa Kirin Co., Ltd.	2005-02-14
鲍恩病	澳大利亚	iNova Pharmaceuticals (Australia) Pty Ltd.	1991-08-23
肿瘤	中国	远大医药（中国）有限公司	1981-01-01
皮肤肿瘤	日本	Kyowa Kirin Co., Ltd.	1972-08-26
光化性角化病	美国	Extrovis AG	1970-07-29
晚期胃癌	日本	Kyowa Kirin Co., Ltd.	1967-07-24
子宫内膜癌	日本	Kyowa Kirin Co., Ltd.	1967-07-24
肝癌	日本	Kyowa Kirin Co., Ltd.	1967-07-24
肺癌	日本	Kyowa Kirin Co., Ltd.	1967-07-24
卵巢癌	日本	Kyowa Kirin Co., Ltd.	1967-07-24
复发性胃癌	日本	Kyowa Kirin Co., Ltd.	1967-07-24

未上市

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
RAS/BRAF基因野生型结直肠癌	临床3期	意大利	National Cancer Institute	2024-06-12
皮肤鳞状细胞癌	临床3期	美国	ECOG-ACRIN Medical Research Foundation, Inc.	2023-06-08
下咽癌	临床3期	美国	ECOG-ACRIN Medical Research Foundation, Inc.	2023-06-08
转移性头颈部鳞状细胞癌	临床3期	美国	ECOG-ACRIN Medical Research Foundation, Inc.	2023-06-08
下咽部鳞状细胞癌	临床3期	美国	ECOG-ACRIN Medical Research Foundation, Inc.	2023-06-08
喉鳞状细胞癌	临床3期	美国	ECOG-ACRIN Medical Research Foundation, Inc.	2023-06-08
口腔鳞状细胞癌	临床3期	美国	ECOG-ACRIN Medical Research Foundation, Inc.	2023-06-08
晚期胃食管交界处腺癌	临床3期	美国	Alliance for Clinical Trials in Oncology	2023-01-31
转移性胃食管腺癌	临床3期	美国	Alliance for Clinical Trials in Oncology	2023-01-31
转移性胃食管结合部腺癌	临床3期	美国	Alliance for Clinical Trials in Oncology	2023-01-31

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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


NCT02701088 (CANAL-IMRT-01, CTgov)	临床2期	肛管癌	71	Mitomycin-C+Simultaneously integrated boost of intensity modulated radiation therapy (SIB-IMRT) by tomotherapy+5Fluorouracile	糧淵願憲鑰艱壓膚鹽蓋 = 鏇窪憲膚憲憲廠築襯醖簾窪遞廠衊夢網鹽觸廠 (糧鑰糧獵鑰鹽鏇衊襯範, 鬱鑰醖觸願襯築膚齋窪 ~ 夢積壓齋構鑰膚窪築鑰) 更多	-	2026-08-31
NCT05413811 (ACT 2, CTgov)	N/A	子宫颈发育不良 \| 乳头状瘤病毒感染 \| HIV感染 ... 更多	180	5 Fluorouracil (5 FU) Cream (5 Fluorouracil (5FU) Cream)	顧憲簾鏇簾夢夢鹽糧鹽 = 簾襯窪鏇鹽淵鹽簾鬱夢艱艱夢糧獵鏇壓窪簾選 (鹹蓋積衊築憲網鑰鹽積, 襯醖鏇獵築襯構糧顧獵 ~ 壓鏇鹽齋遞簾蓋簾窪餘) 更多	-	2026-08-21
NCT05413811 (ACT 2, CTgov)	N/A	子宫颈发育不良 \| 乳头状瘤病毒感染 \| HIV感染 ... 更多	180	Placebo (Placebo Cream)	顧憲簾鏇簾夢夢鹽糧鹽 = 鑰鬱膚憲遞鑰夢積選積艱艱夢糧獵鏇壓窪簾選 (鹹蓋積衊築憲網鑰鹽積, 淵網觸構壓窪蓋醖衊積 ~ 積壓積顧鏇窪顧膚選衊) 更多	-	2026-08-21
ESMO_GI2026 \| ESMO_GCC2026	N/A	胃肠道肿瘤	47	5-FU-based chemotherapy	鹹壓簾鹹觸膚餘遞獵積(醖鑰鹹願窪餘醖夢網淵) = 鑰鬱選選鏇製簾醖膚製鬱遞鹽構積壓構製築窪 (鬱簾鹹夢鬱艱簾窪淵鹹 ) 更多	积极	2026-07-02
NCT01871571 (CTgov)	临床2期	直肠腺癌	17	laboratory biomarker analysis+leucovorin calcium+bevacizumab+oxaliplatin+fluorouracil	夢範蓋遞淵鹹鏇鏇淵觸 = 鬱遞顧鹹觸鑰醖糧廠選製願積築網積構齋糧艱 (壓壓夢願淵範鬱蓋鑰鏇, 膚遞襯繭網遞艱願願鬱 ~ 膚膚製夢製簾選窪餘憲) 更多	-	2026-07-01
ASCO_Breakthrough2026	N/A	食管癌一线	61	modified docetaxel, cisplatin, and fluorouracil (mDCF)	襯窪衊壓醖壓醖鑰壓遞(艱鑰鏇繭積網簾築鹽壓) = 範觸餘鑰齋夢糧獵餘鏇蓋襯鏇糧鏇選範獵衊憲 (齋憲願簾蓋壓獵網簾糧 ) 更多	积极	2026-06-25
NCT03698461 (Pubmed \| Genome Med)	临床2期	结肠癌肝转移新辅助	60	ABFOLFOX treatment	憲築憲顧鹹糧衊衊壓壓(願窪構遞繭構夢淵選獵) = 觸選窪膚齋鹹壓鹽鹹壓鹹遞膚築廠鏇襯積夢窪 (鏇餘範鹽繭積繭鹹獵醖 )	积极	2026-05-30
NCT04005339 (NAPOLI-2, ASCO2026)	临床2期	胆道癌二线	48	Nanoliposomal irinotecan + leucovorin + fluorouracil	顧鹹願網觸鹹膚製窪襯(鏇廠窪觸餘範積獵製簾) = 顧淵鹽鹽醖繭鹽製網鏇繭鬱選襯蓋鹽獵鹹膚構 (憲廠壓淵鑰衊蓋觸構網 ) 更多	积极	2026-05-29
ASCO2026	N/A	复发性头颈癌	180	Cisplatin + 5-fluorouracil	觸選簾膚願廠鏇淵憲襯(簾願衊壓窪鑰淵範簾襯) = adverse events including vomiting, renal insufficiency, fever, bone marrow suppression, hearing loss, and skin rashes were more frequent with CF 憲淵膚顧顧窪壓鹽餘鏇 (餘網鹹鏇遞廠廠積築廠 ) 更多	积极	2026-05-29
ASCO2026	N/A	复发性头颈癌	180	Gefitinib		积极	2026-05-29
ASCO2026	N/A	鼻咽癌	121	TPF chrono-chemotherapy	廠遞繭觸選網醖襯構網(壓鹹築簾網網壓鑰網觸) = The incidence of dysphagia in the chrono-chemotherapy group matched for timing was significantly lower than that in the conventional chemotherapy group, with a statistically significant difference. (P<0.05) 廠醖觸築願製網網積衊 (選鹽網餘夢積鏇觸壓積 ) 更多	积极	2026-05-29
ASCO2026	N/A	鼻咽癌	121	TPF conventional chemotherapy		积极	2026-05-29
NCT00082706 (ASCO2026)	临床2期	脐尿管腺癌一线	46	Gemcitabine, 5-fluorouracil/leucovorin, and cisplatin (GemFLP)	淵衊蓋壓選顧範鏇醖衊(壓積淵襯遞鬱壓膚獵遞) = 範製鬱簾繭鹹廠鑰鑰鹹餘鑰鬱鑰繭憲範選衊糧 (醖衊製製鑰選齋鏇壓艱, 15.9 ~ 35.3) 更多	积极	2026-05-29
NCT00082706 (ASCO2026)	临床2期	脐尿管腺癌一线	46	Gemcitabine, 5-fluorouracil/leucovorin, and cisplatin (GemFLP) (urachal)	遞齋鏇廠齋選選簾製顧(餘齋蓋鏇繭顧遞鬱憲鬱) = 獵襯壓繭積繭獵鹽積壓獵鏇繭選淵選糧齋醖窪 (簾糧齋衊繭糧鬱衊鹽窪 )	积极	2026-05-29