A Phase II Study Of Intravenous DX-8951f (EXATECAN MESYLATE) Administered Daily For Five Days Every Three Weeks To Pediatric Patients With Relapsed Or Refractory Rhabdomyosarcoma

RATIONALE: Drugs used in chemotherapy use different ways to stop tumor cells from dividing so they stop growing or die.
PURPOSE: Phase II trial to study the effectiveness of exatecan mesylate in treating children who have relapsed or refractory rhabdomyosarcoma.

开始日期2003-01-01

申办/合作机构

Daiichi Sankyo Co., Ltd.

NCT00055952

/ Completed临床2期

A Phase II Study Of Intravenous DX-8951f (EXATECAN MESYLATE) Administered Daily For Five Days Every Three Weeks To Pediatric And Young Adult Patients With Ewing's Sarcoma (ES), Primitive Neuroectodermal Tumor (PNET), Or Desmoplastic Small Round Cell Tumor (DSRCT)

RATIONALE: Drugs used in chemotherapy use different ways to stop tumor cells from dividing so they stop growing or die.
PURPOSE: Phase II trial to study the effectiveness of exatecan mesylate in treating patients who have relapsed or refractory Ewing's sarcoma or peripheral primitive neuroectodermal tumor or desmoplastic small round cell tumor.

开始日期2003-01-01

申办/合作机构

Daiichi Sankyo Co., Ltd.

NCT00045318

/ Completed临床1期IIT

A Phase I Study of DX-8951f (Exatecan Mesylate for Injection) in Patients With Renal Dysfunction

RATIONALE: Drugs used in chemotherapy use different ways to stop tumor cells from dividing so they stop growing or die.
PURPOSE: Phase I trial to study the effectiveness of exatecan mesylate in treating patients who have advanced solid tumors and kidney dysfunction.

开始日期2002-05-01

申办/合作机构

Jonsson Comprehensive Cancer Center

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100 项与依沙替康相关的临床结果

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100 项与依沙替康相关的转化医学

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100 项与依沙替康相关的专利（医药）

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170

项与依沙替康相关的文献（医药）

2026-04-30·JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Novel N-Linked Camptothecin Linker-Payloads to Access Antibody-Drug Conjugates with High Target-Mediated In Vivo Efficacy.

Article

作者: Kofman, Esther ; Hua, Zhong L ; Uyeoka, Alycia K ; Yang, Song ; Bacauanu, Vlad ; Bowman, Edward P ; Zepeda, Nancy ; Chastain, Olivia R ; Tomazela, Daniela M ; Fayadat-Dilman, Laurence ; Northrup, Alan B ; Quiroz, Ryan V ; Johnson, Rebecca E ; Geierstanger, Bernhard H ; Charati, Manoj ; Judo, Michael ; Barry, Evan R ; Seganish, W Michael ; Jia, Mengxuan ; Yan, Qingyun ; Knemeyer, Ian ; Chen, Si-Jie ; Akbari, Peyman ; Flygare, John A ; Morales, Christian L ; Zhang, Fan ; Lang, Simon B

Antibody-drug conjugates (ADCs) are transforming oncology by enabling targeted delivery of potent cytotoxic agents to tumors. However, challenges such as resistance and limited response to established ADCs highlight the need for improved linkers and novel payloads driven by rational multivariate design and extensive synthetic optimization. We describe a discovery chemistry campaign for novel camptothecin-based linker-payloads enabling high drug-to-antibody ratio (DAR) ADCs with good biophysical properties, good in vitro potency, and strong in vivo efficacy. Starting from exatecan, amine-containing cytotoxic analogs were synthesized and evaluated for potency and permeability. Optimization of protease-cleavable p-aminobenzyl carbamate (PABC) linkers with a focus on stability and polarity leads to the discovery of promising α-amino-isobutyramido-exatecan constructs. The corresponding high-DAR ADCs showed low aggregation, good in vitro potency, and robust target-mediated efficacy in vivo across two antibody-antigen pairs. These results demonstrate the potential of these linker-payloads and the broad applicability of this design strategy.

2026-04-02·MOLECULAR CANCER THERAPEUTICS

A Novel Dual-Payload ADC Platform Integrating Exatecan and Triptolide to Enhance Antitumor Efficacy and Overcome Resistance

Article

作者: Ren, Pengfei ; Qi, Lu ; Fan, Xinzou ; Guan, Menglong ; Zuo, Teng ; Lei, Gang ; Xu, Yanhua ; Yin, Shijun ; Chen, Jiao ; Li, Zhengping ; Ke, Xiao ; Zhao, Yonghao ; Yue, Ju ; Tang, Jiao

Abstract:

Antibody–drug conjugates (ADC) that utilize DNA topoisomerase I inhibitors, such as deruxtecan and SN-38, have significantly enhanced the efficacy of cancer treatment. However, the development of more effective ADCs to combat drug-resistant tumors remains a critical challenge. ADCs covalently link the topoisomerase I inhibitor exatecan and the RNA polymerase II inhibitor triptolide to the same antibody, thereby establishing a dual-killing mechanism against tumor cells. Through optimization of the linker design, this dual-payload ADC achieved precise drug delivery in vivo. Specifically, triptolide is initially released to downregulate the expression of the stress response protein heat shock protein 70 and the efflux pump P-glycoprotein in tumor cells, thereby significantly enhancing drug sensitivity and effectively overcoming resistance, followed by gradual exatecan release, further inhibiting tumor cell proliferation and survival. Experimental results demonstrated that this dual-payload ADC exhibits significant antitumor activity in both in vitro cell models and in vivo xenograft models, including cell line–derived xenograft and patient-derived xenograft models, successfully addressing the challenge of drug resistance encountered in traditional monotherapy. Additionally, non-Good Laboratory Practice–compliant toxicity studies have confirmed the favorable safety profile of this ADC. In summary, this study provides an innovative strategy for overcoming tumor resistance, demonstrating substantial potential for clinical translation, and offering promising therapeutic outcomes and prognosis for patients with cancer.

2026-04-02·MOLECULAR CANCER THERAPEUTICS

Preclinical Development of MGC028, an ADAM9-Targeted, Glycan-Linked, Exatecan-Based Antibody–Drug Conjugate for the Treatment of Solid Cancers

Article

作者: Li, Hua ; Jin, Linda ; Ford, Delta ; Bush, Curtis ; Son, Thomas ; Loo, Deryk ; Gorlatov, Sergey ; Brown, Jennifer G. ; Nam, Viktoriya ; Sharma, Neel K. ; Tamura, James ; Butler, Shelley ; Diedrich, Gundo ; Hav, Monirath ; Scribner, Juniper A. ; Zhang, Xiaoyan ; Quinonez, Dienis ; Bonvini, Ezio ; McKenzie, Carroll ; Summers, Antwanette

Abstract:

ADAM9, a member of the a disintegrin and metalloproteinase (ADAM) family of multifunctional type 1 transmembrane proteins, is an attractive target for cancer treatment owing to its overexpression in multiple tumors and its role in tumorigenesis and cancer progression. A maytansine-based ADAM9-targeting antibody–drug conjugate (ADC), IMGC936, was affected by dose-limiting ocular adverse events, including blurred vision and keratopathy, that were observed both preclinically and in a first-in-human clinical study. Ocular toxicity is a well-known adverse event associated with microtubule inhibitor–based ADC payloads and has been reported for several approved ADCs. Although IMGC936 ocular toxicity was dose-limiting and likely constrained its clinical activity, no other prominent safety signals were observed. To date, topoisomerase 1–inhibitor ADCs have shown good clinical activity without the dose-limiting ocular toxicities experienced with microtubule inhibitor payloads. Given the attractiveness of ADAM9 for targeted therapy, we sought to develop a topoisomerase 1–inhibitor ADAM9 ADC. Here, we report the preclinical evaluation of MGC028, an ADAM9-targeting ADC that incorporates the cleavable linker–payload, bicyclononyne carbamoyl sulfamide Val-Ala-PABC exatecan (SYNtecan E), site-specifically conjugated at asparagine 297 of the heavy chain through enzymatic glycan remodeling and metal-free click chemistry. MGC028 demonstrated in vitro cytotoxicity toward ADAM9-positive human tumor cell lines and mediated bystander killing. MGC028 exhibited specific, dose-dependent in vivo antitumor activity toward ADAM9-positive cell line–derived and patient-derived xenograft models and was well tolerated in a repeat-dose nonhuman primate toxicology study, with no evidence of the ocular toxicities observed with IMGC936. A first-in-human study of MGC028 in patients with advanced solid tumors has been initiated (NCT06723236).

1,052

项与依沙替康相关的新闻（医药）

2026-05-14

·全球好药资讯

【III期临床试验】第一三共ADC新药Ifinatamab deruxtecan（DS-7300a/I-DXd）招募含铂化疗和免疫治疗后疾病进展的晚期或转移性食管鳞癌！

#食管癌经治临床试验简要入排本临床药物为靶向B7-H3的ADC药物；目前招募晚期或转移性食管鳞癌（ESCC）患者；年龄≥18岁；接受铂类药物和免疫检查点抑制剂（ICI）治疗后出现疾病进展且既往接受针对不可切除的晚期或转移性ESCC最多一线全身治疗；受试者必须按照实验室手册的规定，提供足够数量和质量的基线肿瘤组织样本；排除既往接受过orlotamab 、enoblituzumab或其他B7-H3靶向药物治疗（包括IDXd）患者；排除接受过任何拓扑异构酶抑制剂治疗患者；排除组织学或细胞学确诊为腺鳞癌亚型的患者；脑转移患者需治疗后稳定4周以上；全国多中心。研究中心北京福建福州、厦门广西南宁湖北武汉四川成都天津山东济南、临沂、济宁江苏扬州、常州广东揭阳、汕头安徽合肥河南安阳、新乡、洛阳、郑州黑龙江哈尔滨吉林长春辽宁沈阳浙江杭州具体启动情况以后期咨询为准【研究中心若有更新请拉至文末查看】试验名称一项在经治的晚期或转移性食管鳞癌（ESCC）受试者中评价Ifinatamab Deruxtecan（I-DXd）的多中心、随机、开放性III期研究（IDeate-Esophageal01）。试验药物 Ifinatamab deruxtecan（代号：DS-7300a，简称：I-DXd）是第一三共利用其专有的DXd ADC技术设计，由人源化抗B7-H3 IgG1单克隆抗体通过可裂解四肽连接子与拓扑异构酶I抑制剂有效载荷（一种依喜替康衍生物，DXd）连接组成。当药物进入体内后，能够精准地靶向表达B7-H3的癌细胞，并释放细胞毒性载荷，从而实现对癌细胞的杀伤作用。 B7-H3是一种跨膜蛋白，属于B7蛋白家族，该家族与包括PD-1在内的CD28受体家族结合。其在多种癌症类型中均存在过度表达，包括食管鳞状细胞癌（ESCC），并已被证明其高表达与不良预后相关，因此B7-H3成为了一个有前景的治疗靶点之一。值得一提的是，2026年4月13日，默沙东和第一三共联合宣布ifinatamab deruxtecan（I-DXd）的生物制剂许可证申请（BLA）获得美FDA优先审评，用于治疗在铂类化疗期间或之后疾病进展的广泛期小细胞肺癌（ES-SCLC）成人患者。研究药物：Ifinatamab Deruxtecan（I-DXd）（III期）登记号：CTR20250583 试验类型：对照试验（VS 研究者选择的化疗）适应症：晚期或转移性食管鳞癌（二线）申办方：Daiichi Sankyo, Inc./第一三共（中国）投资有限公司/Daiichi Sankyo Propharma Co., Ltd. 延伸阅读第一三共（Daiichi Sankyo）是一家为社会可持续发展做贡献的创新型全球医疗保健公司，致力于发现、开发和提供新的标准疗法，以提高世界各地患者的生活质量。第一三共专注制药行业120余年，凭借其世界一流的科学和技术，为癌症、心血管疾病和其他医疗需求远未得到满足的疾病患者研发新的治疗方法和创新药物。备注：以上信息来源于药企官网注：上下滑动可查看全部内容用药周期 Ifinatamab Deruxtecan（简称：I-DXd；代号：DS-7300a）的规格：100mg；用法用量：12mg/kg；用药时程：每21天一个周期的第1天（Q3W）。对照组药物如下：多西他赛的规格：80mg/4mL；用法用量：第一天静脉注射75mg/m2；用药时程：每21天一次。紫杉醇的规格：300mg/50mL；用法用量：第一天静脉注射135-175mg/m2；用药时程：每21天一次。伊立替康的规格：300mg/15mL；用法用量：第1天和第8天静脉注射125mg/m2；用药时程：每21天一次。更多项目信息请参考： http://www.chinadrugtrials.org.cn/index.html 温馨提示：文章入排信息来源于国家临床试验官网公示信息，具体情况以实际咨询为准！报名方式参与临床试验，获取国际前沿新药新疗法使用机会！更有一线专家团队为你的治疗保驾护航！【印塔健康】目前有肺癌、肝癌、肾癌、胃癌、肠癌、胰腺癌、妇瘤、泌尿肿瘤、血液肿瘤......等几乎涵盖所有癌种的临床试验正在招募患者！扫描下方二维码添加医学运营一对一咨询或点击左下角“阅读原文”直接报名！我们将会在24小时内（工作日）与您电话或微信联系，请保持手机畅通！ #Ifinatamab—deruxtecan #DS—7300a #I—DXd #第一三共 #靶向B7—H3的ADC药物 #食管鳞癌ADC新药临床招募 #化疗免疫耐药的食管癌新药临床招募【重要提示】印塔健康旗下公众号【全球好药资讯】所有文章信息仅供参考，具体治疗谨遵医嘱！

2026-05-14

·探药新途

【肺癌】靶向Trop-2抗原的抗体偶联药物（ADC）注射用戈沙妥珠单抗招募广泛期小细胞肺癌

点击蓝字关注我们《临床试验信息》「READING」 01 试验题目　一项在既往接受过治疗的广泛期小细胞肺癌（ES-SCLC）参与者中比较戈沙妥珠单抗与标准治疗（SOC）的全球、多中心、随机、开放性、III期研究 02 适应症广泛期小细胞肺癌 03 研究药物　试验组：注射用戈沙妥珠单抗　对照组：托泊替康 04 药物介绍　　注射用戈沙妥珠单抗是一种靶向Trop-2抗原的抗体偶联药物（ADC），结合了抗体靶向性和细胞毒性药物的杀伤作用，其核心机制是通过抗体精准识别癌细胞表面的Trop-2蛋白，递送化疗药物至肿瘤内部，抑制癌细胞增殖并诱导凋亡。《主要入排标准》「READING」 01 满足年龄≥18 岁，男女不限 02 既往针对ES-SCLC接受1线含铂化疗（定义为至少2个治疗周期）联合或不联合抗程序性细胞死亡蛋白1（PD-1）或程序性细胞死亡配体1（PD-L1；下文将PD-1和PD-L1统称为PD-[L]1）治疗后 03 愿意并能够遵守本研究方案的要求和限制 04 具有存档肿瘤组织（福尔马林固定石蜡包埋[FFPE]组织块）或从可评估的粗针穿刺活检或切除活检中新获取的肿瘤组织 05 排除既往接受过伊立替康、托泊替康、SG、SN-38、依喜替康衍生物和类似的靶向拓扑异构酶I的药物治疗 06 排除无化疗间隔（从一线含铂化疗末次给药至出现疾病进展的时间）<30天（无论是否接受免疫疗法维持治疗）；未经治疗的脑转/癌性脑膜炎《患者权益》「READING」 1、提前获得前沿新药疗法 2、可能产生优于标准方案效果 3、相关检查和治疗药物免费 4、享受顶尖团队密切医疗照护 5、获得一定的交通补助长按下方二维码联系我们招募微信号丨19121190993 新浪微博丨探药新途 XINYAO ZHIJIA 招募微信号丨17349745256 抖音丨探药新途 XINYAO ZHIJIA 招募公众号丨tyxt158 小红书丨探药新途 XINYAO ZHIJIA TANYAOXINTU 　　上海药邦汇医疗科技有限公司（简称“药邦汇”）是一家专注于肿瘤、慢性病及罕见病领域临床试验患者招募的创新型医疗科技企业。公司立足上海，辐射全国，致力于搭建患者、医疗机构与新药研发企业之间的高效桥梁，加速创新药物和疗法的临床转化进程，为患者提供前沿治疗机会，助力中国医药产业高质量发展。探药新途——探寻生命健康的新可能。与我们一同，走在医药科技的最前沿。您的每一篇推送，都是一次通往新希望的路标。肿瘤疫苗、基因疗法、细胞疗法、免疫疗法、小分子抑制剂、AI制药等更多新药添加微信进行详细咨询微信：19121190993【电话同号】。

2026-05-13

·生物药观察

石药集团TF ADC SYS6051启动临床I期

2026年1月底，石药集团TF ADC SYS6051申报临床获受理，4月13日SYS6051获CDE默示临床许可，4月29日获FDA IND批准。 2026年5月13日，石药在CDE药物临床试验登记和信息公示平台登记了SYS6051的FIH临床I期研究（CTR20261816，SYS6051-001）。本项I期研究预计在中国入组114例经组织学或细胞学确诊的既往标准治疗失败的晚期实体瘤受试者。在剂量递增阶段，主要评估SYS6051治疗晚期实体瘤参与者的安全性和耐受性；队列扩展阶段，评估SYS6051在RP2D剂量下治疗晚期实体瘤的抗肿瘤活性。复旦肿瘤虞先濬博士为主要研究者。根据AACR2025的Abstract信息，SYS6051采用抗TF人源化IgG1抗体，偶联Exatecan，DAR6。SYS6051不影响凝血功能，快速内吞，具有显著的体内抗肿瘤活性。NHP毒性≤30mpk，未观察到凝血功能异常和皮疹，优于TF历史数据。竞争格局方面：2021年9月，首款靶向TF的ADC tisotumab vedotin（TV）获FDA加速批准上市，TV 在临床上出现较高频率的眼毒性和出血问题。此外，值得关注的是乐普生物的MRG004A和苏州信诺维的XNW28012已推进到临床3期。石药集团在ADC领域布局广泛，涵盖多款热门靶点点关注，不迷路

100 项与依沙替康相关的药物交易

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D01432	依沙替康	-	DB12185

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
胰腺癌	临床3期	美国	Daiichi Sankyo Co., Ltd.	2001-07-01
胰腺癌	临床3期	加拿大	Daiichi Sankyo Co., Ltd.	2001-07-01
促纤维增生性小圆细胞瘤	临床2期	美国	Daiichi Sankyo Co., Ltd.	2003-01-01
促纤维增生性小圆细胞瘤	临床2期	加拿大	Daiichi Sankyo Co., Ltd.	2003-01-01
外周性原始神经外胚层肿瘤	临床2期	美国	Daiichi Sankyo Co., Ltd.	2003-01-01
外周性原始神经外胚层肿瘤	临床2期	加拿大	Daiichi Sankyo Co., Ltd.	2003-01-01
复发性尤文肉瘤	临床2期	美国	Daiichi Sankyo Co., Ltd.	2003-01-01
复发性尤文肉瘤	临床2期	加拿大	Daiichi Sankyo Co., Ltd.	2003-01-01
食管癌	临床2期	美国	Daiichi Sankyo Co., Ltd.	2001-04-01
食管癌	临床2期	加拿大	Daiichi Sankyo Co., Ltd.	2001-04-01

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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


Pubmed \| Eur J Cancer	临床2期	局部晚期软组织肉瘤	-	Exatecan	製糧膚艱築範膚鏇鏇醖(膚製餘願蓋襯築膚衊構) = 顧網鏇窪網壓遞鏇壓鹽積壓鹽夢壓遞憲選鹽淵 (遞鑰蓋顧糧簾築廠廠網 ) 更多	不佳	2007-04-01
Pubmed \| J Clin Oncol	临床3期	晚期胰腺腺癌一线	349	Exatecan plus gemcitabine	膚鹽網積鹹獵鹽艱選壓(窪選構網構選餘顧製範) = 艱衊構壓餘糧淵憲願願襯鏇憲顧壓夢艱襯鹽簾 (襯簾淵鏇觸顧廠獵築廠 ) 更多	不佳	2006-09-20
Pubmed \| J Clin Oncol	临床3期	晚期胰腺腺癌一线	349	Gemcitabine alone	膚鹽網積鹹獵鹽艱選壓(窪選構網構選餘顧製範) = 鏇鏇淵鹽鏇製憲廠獵顧襯鏇憲顧壓夢艱襯鹽簾 (襯簾淵鏇觸顧廠獵築廠 ) 更多	不佳	2006-09-20
ASCO2004	临床3期	胰腺癌	349	DX-8951f (Exatecan Mesylate; DX) + Gemcitabine (GEM)	獵鹽鏇鑰鑰積醖願廠網(選願鬱齋壓膚鑰築齋艱) = 鏇顧遞築餘願選鬱網鹽觸糧築鹽鬱獵壓糧鏇遞 (艱獵顧鏇鹽構憲艱範襯 ) 更多	不佳	2004-07-15
ASCO2004	临床3期	胰腺癌	349	Gemcitabine (GEM)	獵鹽鏇鑰鑰積醖願廠網(選願鬱齋壓膚鑰築齋艱) = 網壓網鏇壓餘願願範蓋觸糧築鹽鬱獵壓糧鏇遞 (艱獵顧鏇鹽構憲艱範襯 ) 更多	不佳	2004-07-15
ASCO2004	临床2期	转移性胃癌	41	DX-8951f	窪膚鑰遞壓鬱顧廠獵衊(簾鹹窪網糧齋艱願膚鹹) = 繭糧廠築糧簾遞壓憲鹹鹹網壓鏇夢積鹹顧範鏇 (鬱築糧製選鹽鹽齋衊繭 )	-	2004-07-15
ASCO2004	临床3期	胰腺癌	339	Ensiv	鑰壓齋構廠艱窪選膚餘(積繭製憲窪鏇夢網獵製) = 築糧蓋廠選網壓觸鬱網製蓋憲遞製願鬱餘繭憲 (構鹹簾範糧淵願糧獵壓 ) 更多	-	2004-07-15
ASCO2004	临床3期	胰腺癌	339	Gemcitabine	鑰壓齋構廠艱窪選膚餘(積繭製憲窪鏇夢網獵製) = 簾壓鏇觸願夢鏇衊網夢製蓋憲遞製願鬱餘繭憲 (構鹹簾範糧淵願糧獵壓 ) 更多	-	2004-07-15
Pubmed \| Lung Cancer	临床2期	晚期非小细胞肺癌一线	39	Exatecan mesylate (DX-8951f)	範糧醖簾襯築淵鹽範範(壓窪選製簾遞願顧鏇繭) = 顧鹹積製積選範願艱顧膚襯廠簾襯鹹遞積壓膚 (觸積餘選鑰積醖糧鏇淵 ) 更多	不佳	2003-08-01