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更新于：2026-06-29
ESG-401
更新于：2026-06-29
概要
基本信息
药物类型 ADC |
别名 Humanized anti-Trop2-SN-38 antibody conjugate、Humanized mAb anti-TROP-2 program、重组人源化抗Trop2单抗-SN38偶联物 (诗健生物) + [6] |
作用方式 抑制剂 |
作用机制 TOP1抑制剂(DNA拓扑异构酶I抑制剂)、Trop-2抑制剂(肿瘤相关钙信号传感器2抑制剂) |
在研适应症 |
在研机构 |
最高研发阶段临床3期 |
首次获批日期- |
最高研发阶段(中国)临床3期 |
特殊审评突破性疗法 (中国) |
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结构/序列
分子式C22H20N2O5 |
InChIKeyFJHBVJOVLFPMQE-QFIPXVFZSA-N |
CAS号86639-52-3 |
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Sequence Code 27958L
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Sequence Code 319372635H
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关联
4
项与 ESG-401 相关的临床试验NCT06732323
A Randomized, Open-label, Phase III Study of ESG401 Versus Investigator's Choice Chemotherapy as First-line Treatment in Patients With Unresectable Recurrent or Metastatic Triple-Negative Breast Cancer
NCT06383767
A Open-label, Randomized, Multicenter Phase III Study of ESG401 Versus Investigator's Choice Chemotherapy in Patients With Locally Advanced or Metastatic HR+/HER2- Breast Cancer Who Had Failed at Least One Line of Chemotherapy
NCT05060276
A Phase 1B, Dose-Escalation Study of the Safety and Preliminary Efficacy of an Anti-Trop2 Antibody Drug Conjugate (STI-3258) in Patients With Relapsed or Refractory Solid Tumors
100 项与 ESG-401 相关的临床结果
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100 项与 ESG-401 相关的转化医学
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100 项与 ESG-401 相关的专利（医药）
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1,924
项与 ESG-401 相关的文献（医药）2026-02-18ACS bio & med chem Au
Blue Fluorescent Siloxytecans Exhibit Potent Anticancer Activity and Enable Direct Real-Time Quantification of Intracellular Uptake
Article
作者: Menta, Lekhya ; Chen, Rebecca ; Njoo, Edward ; Wang, Terry ; Parvin, Jessica ; Kwok, Olivia ; Yamamoto, Akira ; Sadagopan, Sripathy ; Li, Katelyn ; Vaidya, Sanika ; D’souza, Zane ; Sanchez, Thomas ; Zhang, Jenny ; Pazzi, Joseph ; Xie, Yining ; Baratoff, Isa ; Mo, Ashley ; Somani, Shreya ; Chia, Alyssa Yee-Xin ; Lo, Isabella
Notwithstanding the natural abundance of silicon on Earth, silicon-containing compounds comprise relatively few pharmaceutical drugs, though several silylated natural products have demonstrated greater bioavailability and lipophilicity. Here, we apply this strategy in the preparation and biological evaluation of synthetic camptothecin analogs involving a C-10 silyl ether on SN-38, which not only blocks a site of metabolism but also enhances bright-blue fluorescence properties in such compounds. These siloxytecans exhibit comparable dose- and time-dependent antiproliferative activity in a broad panel of cancer cells. Uniquely, we demonstrate that the enhanced fluorescence of these compounds enables real-time, quantitative visualization of the dynamics and selectivity of intracellular uptake through fluorescence microscopy without the need for extensive sample preparation or installation of auxiliary fluorophores. We further demonstrate that the kinetics of cellular uptake observed by fluorescence microscopy are consistent with time-course washout experiments with subtle differences in anticancer potency in several cell lines. Further cell cycle analysis by flow cytometry and cell-free topoisomerase inhibition studies suggests that these siloxytecans retain the topoisomerase-inhibiting properties of camptothecin and other related topoisomerase I inhibitors. Collectively, these studies highlight the utility of quantitative fluorescence microscopy in investigating mechanisms of biological transport and the anticancer activity of such siloxytecans.
2025-12-01ADVANCED MATERIALS
Rational Design of Metal–Organic Frameworks for Pancreatic Cancer Therapy: from Machine Learning Screening to In Vivo Efficacy
Article
作者: Jon Ostolaza-Paraiso ; Dhruv Menon ; João Conde ; Sergio Mercado ; Jhenifer Oliveira ; Xu Chen ; Bárbara B. Mendes ; David Fairen-Jimenez ; Francesca Melle ; João Conniot
Abstract:
Despite improvements in cancer survival rates, metastatic and surgery‐resistant cancers, such as pancreatic cancer, remain challenging, with poor prognoses and limited treatment options. Enhancing drug bioavailability in tumors, while minimizing off‐target effects, is crucial. Metal–organic frameworks (MOFs) have emerged as promising drug delivery vehicles owing to their high loading capacity, biocompatibility, and functional tunability. However, the vast chemical diversity of MOFs complicates the rational design of biocompatible materials. This study employed machine learning and molecular simulations to identify MOFs suitable for encapsulating gemcitabine, paclitaxel, and SN‐38, and identified PCN‐222 as an optimal candidate. Following drug loading, MOF formulations are improved for colloidal stability and biocompatibility. In vitro studies on pancreatic cancer cell lines have shown high biocompatibility, cellular internalization, and delayed drug release. Long‐term stability tests demonstrated a consistent performance over 12 months. In vivo studies in pancreatic tumor‐bearing mice revealed that paclitaxel‐loaded PCN‐222, particularly with a hydrogel for local administration, significantly reduced metastatic spread and tumor growth compared to the free drug. These findings underscore the potential of PCN‐222 as an effective drug delivery system for the treatment of hard‐to‐treat cancers.
2025-09-01INTERNATIONAL JOURNAL OF PHARMACEUTICS
Structure-guided dual modification prodrug strategy for optimizing camptothecin delivery in pancreatic cancer chemotherapy
Article
作者: Wang, Yijie ; Li, Xiaoyan ; Wang, Hangxiang ; Chen, Xiaolong ; Zhu, Hengyan
Pancreatic ductal adenocarcinoma (PDAC) remains one of the most lethal malignancies, exacerbated by the limited efficacy and significant adverse effects associated with current chemotherapies. Thus, there is an urgent need for more effective and less toxic treatment options. Irinotecan, the water-soluble prodrug of 7-ethyl-10-hydroxycamptothecin (SN38), is clinically used for cancer treatment but the efficacy has been compromised by insufficient conversion to its active metabolite SN38. To address these challenges and to expand the repertoire of our previous prodrug chemical engineering, we here developed a dual-modification prodrug strategy to re-constitute this potent DNA topoisomerase I inhibitor SN38 for PDAC treatment. Polyunsaturated fatty acids (PUFAs) were employed as pro-moieties to synthesize mono- or dual-engineered SN38 prodrugs through covalent conjugation to its hydroxyl groups. These prodrugs were then assembled with biodegradable amphiphilic block polymers to form intravenously injectable cytotoxic nanoparticles. The dual-engineered prodrugs demonstrated improved compatibility with the polymer matrices compared to their mono-modified counterparts, leading to enhanced stability and sustained drug release. These optimized nanotherapeutics exhibited markedly higher cytotoxic activity against PDAC cells in vitro than irinotecan. In a preclinical subcutaneous PDAC mouse model, these nanoparticles showed high antitumor activity and were well tolerated. Furthermore, compared to the clinically approved drugs (e.g., Irinotecan and nanoliposomal irinotecan), this prodrug formulation had superior pharmacokinetic property and in vivo antitumor efficacy in an orthotopic PDAC model. Our findings contribute valuable insights into refining prodrug strategies and nanoparticle formulations to potentially overcome existing delivery barriers and enhance the clinical translatability of therapies for PDAC.
100 项与 ESG-401 相关的药物交易
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研发状态
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 晚期三阴性乳腺癌 | 临床3期 | 中国 | 2025-08-27 | |
| HR阳性/HER2阴性乳腺癌 | 临床3期 | 中国 | 2024-06-25 | |
| HR阳性/HER2阴性乳腺癌 | 临床3期 | 中国 | 2024-06-25 | |
| 膀胱癌 | 临床2期 | 中国 | 2021-09-14 | |
| 结直肠癌 | 临床2期 | 中国 | 2021-09-14 | |
| 非小细胞肺癌 | 临床2期 | 中国 | 2021-09-14 | |
| 卵巢癌 | 临床2期 | 中国 | 2021-09-14 | |
| 胃癌 | 临床2期 | 中国 | 2021-09-14 | |
| 三阴性乳腺癌 | 临床2期 | 中国 | 2021-09-14 | |
| 实体瘤 | 临床2期 | 中国 | 2021-09-09 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
临床1期 | 转移性HER2阴性乳腺癌 HER2 Negative | 17 | 蓋築鏇積壓範獵鏇築構(膚鏇艱餘夢壓齋淵選顧) = 範糧窪鹹顧選衊淵觸築 製壓鏇鏇齋壓鹹廠製觸 (築簾窪構鑰醖願淵衊壓, 27.8 ~ 77.0) 更多 | 积极 | 2025-05-13 | ||
临床1期 | 150 | (previously untreated TNBC) | 範醖範鏇膚壓衊鑰壓積(觸淵願壓鹽獵襯觸築夢) = 範觸構淵構積糧壓簾鹽 餘繭築淵遞構觸築簾鹹 (遞繭繭鹹鹽繭齋淵製淵 ) 更多 | 积极 | 2025-01-29 | ||
(late-stage TNBC) | 範醖範鏇膚壓衊鑰壓積(觸淵願壓鹽獵襯觸築夢) = 願觸鏇齋鬱齋鏇繭製夢 餘繭築淵遞構觸築簾鹹 (遞繭繭鹹鹽繭齋淵製淵 ) 更多 | ||||||
临床1期 | 117 | ESG401tage HR+/HER2-BC 12 mg/kg | 壓衊鏇廠醖淵顧膚齋憲(鬱窪製膚襯觸鬱鑰襯鏇) = 襯製齋膚鑰窪壓襯鹹簾 積餘築獵範顧獵壓製範 (蓋遞淵齋憲築夢壓膚範, 64.7 ~ 87.5) 更多 | 积极 | 2024-09-16 | ||
ESG401tage TNBC 12 mg/kg | 壓衊鏇廠醖淵顧膚齋憲(鬱窪製膚襯觸鬱鑰襯鏇) = 範繭壓遞選夢網壓鬱醖 積餘築獵範顧獵壓製範 (蓋遞淵齋憲築夢壓膚範, 44.8 ~ 77.5) 更多 | ||||||
临床1期 | 16 | ESG401 12 mg/kg | 遞襯廠積淵衊遞簾願製(顧鹽窪構餘觸鹹繭選網) = 餘積鹽淵壓觸膚鹽觸築 網獵膚網願顧製憲鹹蓋 (壓願顧窪選鹹網餘鹹衊, 15.2 ~ 64.6) 更多 | 积极 | 2024-09-15 | ||
临床1期 | 40 | 鬱選艱醖齋醖衊願膚鹽(鹽壓顧簾鬱壓製簾鏇壓) = 餘築製遞鑰網衊鑰鹹鹽 鑰顧鏇壓鬱構淵獵範願 (鏇憲壓製襯淵壓觸顧淵 ) 更多 | 积极 | 2024-08-30 | |||
(TRD) | 鬱選艱醖齋醖衊願膚鹽(鹽壓顧簾鬱壓製簾鏇壓) = 淵選襯夢選鹽夢壓窪壓 鑰顧鏇壓鬱構淵獵範願 (鏇憲壓製襯淵壓觸顧淵 ) 更多 | ||||||
临床1期 | 三阴性乳腺癌 一线 | 19 | 範襯餘願網顧廠艱醖鏇(選壓製遞廠廠餘鏇選獵) = 醖鏇鑰餘繭願鬱餘獵壓 衊膚糧鏇艱範醖鏇膚積 (積醖鹹廠廠鏇醖鏇積醖 ) 更多 | 积极 | 2024-08-09 | ||
临床1期 | 23 | ESG401 (16 mg/kg IV) | 壓築糧繭艱膚壓網鹹顧(壓衊廠壓廠鏇夢築壓鏇) = 憲鬱構膚襯蓋獵築壓壓 膚觸顧顧築醖鹽鬱艱糧 (繭鹹憲鑰艱鑰憲範淵獵 ) 更多 | 积极 | 2024-05-24 | ||
临床1/2期 | 35 | (triple negative breast cancer) | 淵遞艱淵願獵鹽鏇願範(簾醖願夢顧廠鬱艱鏇餘) = 願醖膚獵選鏇遞窪鏇壓 襯選製壓製簾糧襯製廠 (窪顧壓觸齋糧蓋簾蓋窪 ) 更多 | 积极 | 2023-05-26 | ||
(HR+/HER2- breast cancer) | 淵遞艱淵願獵鹽鏇願範(簾醖願夢顧廠鬱艱鏇餘) = 鹽鏇窪襯觸襯遞淵獵鏇 襯選製壓製簾糧襯製廠 (窪顧壓觸齋糧蓋簾蓋窪 ) 更多 | ||||||
临床1/2期 | - | 衊鹹築顧廠顧鏇構製觸(獵積糧艱壓淵齋廠醖鹹) = 血液毒性（白细胞和中性粒细胞降低、贫血）和消化道毒性（严重腹泻）出现的频率和程度均大幅度降低。 蓋窪憲築網糧鑰積壓襯 (憲獵窪顧構憲廠鏇襯蓋 ) | 积极 | 2022-09-21 |
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