预约演示
更新于：2026-06-16
Tizetatug rezetecan
更新于：2026-06-16
概要
基本信息
药物类型 ADC |
别名 SHR A1921、SHR-1921、SHR-A1921 + [1] |
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 |
非在研适应症 |
原研机构 |
非在研机构 |
权益机构- |
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)、快速通道 (美国) |
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结构/序列
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Sequence Code 27958L
来源: *****
Sequence Code 774044794H
来源: *****
关联
19
项与 Tizetatug rezetecan 相关的临床试验NCT06470672
A Phase 2 Study of SHR-A1921 Combined Adebrelimab in Endocrine Therapy-failed HR-positive, HER2-negative Advanced Breast Cancer
NCT06649331
Platform Study of ADC Rechallenge in ADC-treated Metastatic Breast Cancer：A Prospective, Open-label, Phase 2 Trial
NCT06434103
An Open, Multicenter Phase I/II Trial of SHR-A1921 in Combination With Adebrelimab and SHR-8068 With or Without Carboplatin in the Treatment of Advanced NSCLC
100 项与 Tizetatug rezetecan 相关的临床结果
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100 项与 Tizetatug rezetecan 相关的转化医学
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100 项与 Tizetatug rezetecan 相关的专利（医药）
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4
项与 Tizetatug rezetecan 相关的文献（医药）2026-02-01CANCER TREATMENT REVIEWS
Clinical overview of trophoblast surface antigen 2 antibody-drug conjugates in non–small cell lung cancer
Review
作者: Naidoo, Jarushka ; Gadgeel, Shirish ; Mino-Kenudson, Mari ; Sethakorn, Nan ; Patel, Sandip Pravin
Lung cancer remains the leading cause of cancer-related death in the United States, with non-small cell lung cancer (NSCLC) accounting for most lung cancer cases. Improvements in first-line treatment with immuno-oncology and targeted therapies have been observed in patients with NSCLC, but benefits may be limited for those with advanced or metastatic NSCLC (mNSCLC). Following progression on frontline therapies, later-line therapies offer modest benefits and are associated with pronounced adverse effects. Accordingly, there is a need for new, more effective options to improve survival and quality of life. Trophoblast surface antigen 2 (TROP2) antibody-drug conjugates (ADCs) are a novel approach to address unmet treatment needs in NSCLC. There are 5 TROP2-directed ADCs currently under investigation for treatment of NSCLC: datopotamab deruxtecan, sacituzumab govitecan, sacituzumab tirumotecan, DB-1305, and SHR-A1921. Here, we provide an overview of the properties of each ADC as well as efficacy and safety data from clinical trials of patients with NSCLC with or without actionable genomic alterations (AGAs). The unique characteristics of each ADC and its components, particularly the linker chemistry and payload attributes, define the mechanism of action and subsequently influence dosing, efficacy, and safety. TROP2 ADCs have shown antitumor responses with a manageable safety profile in patients with mNSCLC in several ongoing and completed trials. Additional studies are required to understand how these agents can be effectively integrated into the treatment paradigm for lung cancer, taking into consideration sequential use of multiple ADCs, resistance mechanisms, combination therapies, and use in special populations.
2025-12-01CANCER CELL
TROP-2-targeted antibody-drug conjugate SHR-A1921 for advanced or metastatic solid tumors: A first-in-human phase 1 study
Article
作者: Yang, Yan ; Guo, Feng ; Liu, Caigang ; Yan, Min ; Li, Xingya ; Wang, Shuni ; Cui, Jiujie ; Zhang, Panpan ; Song, Zhengbo ; Zhong, Jia ; Dang, Qi ; Wang, Ce ; Han, Xinghua ; Chen, Liang ; Guo, Hongqian ; Zhong, Jincai ; Wu, Lin ; Wu, Shikai ; Li, Yong ; Fei, Kailun ; Xiao, Juxiang ; Wang, Jie ; Lin, Zhifei ; Tang, Dihong ; Xie, Qiushi ; Zhang, Shichuan ; Jiang, Shusuan ; Qu, Xiujuan ; Liu, Rongrui ; Liu, Tianshu ; Xu, Huiting ; Yuan, Chunxiu ; Xing, Nianzeng
This study is a first-in-human, three-stage, phase 1 trial (NCT05154604) designed to evaluate the trophoblast cell-surface antigen 2 (TROP-2)-targeted antibody-drug conjugate SHR-A1921 (1.5-6.0 mg/kg every 3 weeks) in 391 patients with pretreated advanced/metastatic solid tumors. Grade ≥3 treatment-related adverse events occurred in 132 patients (33.8%), with the most common being stomatitis, affecting 57 patients (14.6%). SHR-A1921 showed a low incidence of hematologic toxicities, with only 3.1% of patients experiencing grade ≥3 decreases in neutrophil count. The overall objective response rate was 24.8% (95% confidence interval [CI], 20.6-29.4), ranging from 18.2% to 43.1% across cohorts with platinum-resistant ovarian cancer, triple-negative breast cancer, small-cell lung cancer, non-small cell lung cancer, hormone receptor-positive breast cancer, cervical cancer, and biliary tract cancer. No significant correlation was found between TROP-2 expression and treatment efficacy. In summary, SHR-A1921 exhibited promising antitumor activity and a manageable safety profile, with 3.0 mg/kg every 3 weeks selected for further clinical development.
Frontiers in Pharmacology
Preclinical activity of SHR-A1921, a novel antibody-drug conjugate targeting trophoblast cell-surface antigen2 (Trop-2) in prostate cancer
Article
作者: Wang, Binyu ; Qiu, Xuefeng ; Huang, Haifeng ; Guo, Hongqian ; Xu, Qiuya ; Han, Zheng ; Peng, Shan
Background:
Despite advances in the 5-year survival rates for prostate cancer patients, progression to metastatic castration-resistant prostate cancer (mCRPC) remains a significant challenge following standard treatments. Antibody-drug conjugates (ADCs) are an emerging class of biopharmaceuticals that combine the specificity of monoclonal antibodies with the potency of cytotoxic drugs. Trophoblast cell surface antigen 2 (Trop-2) is overexpressed in prostate cancer, particularly in metastatic forms.
Methods:
Response to this, we developed a novel Trop-2-targeted antibody-drug conjugate (ADC), SHR-A1921, which incorporates a potent DNA topoisomerase I inhibitor,SHR9265. Its
in vitro
cytotoxicity was assessed across prostate cancer cell lines with differential Trop-2 expression. Subcutaneous xenograft models were established for
in vivo
tumor-suppressive activity evaluation, and patient-derived organoid models validated its potential clinical efficacy.
Results:
In preclinical models, SHR-A1921 specifically bound to Trop-2, followed by internalization into tumor cells and subsequent intracellular trafficking to lysosomes, where the release of SHR9265 occurred. This resulted in DNA damage and apoptosis in Trop-2-expressing tumor cells
in vitro
.
In vivo
, SHR-A1921 exhibited significant antitumor activity, inducing DNA damage in Trop-2-positive xenograft tumors. Additionally, SHR-A1921 demonstrated antitumor effects in Trop-2-expressing prostate cancer organoids. Safety assessments in rats indicated that SHR-A1921 had an acceptable safety profile.
Conclusion:
SHR-A1921 is a promising Trop-2-targeted ADC that leverages innovative technology to deliver potent antitumor activity against Trop-2-expressing prostate cancer cells, with an acceptable safety profile observed in preclinical studies. These results highlight the promising clinical potential of SHR-A1921 as a therapeutic option for prostate cancer patients with Trop-2-positive tumors.
294
项与 Tizetatug rezetecan 相关的新闻（医药）2026-06-06
·今日头条
2026-06-05
100 项与 Tizetatug rezetecan 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 |
|---|---|---|---|---|
| 铂耐药上皮性卵巢癌 | 临床3期 | 中国 | 2024-05-10 | |
| 铂耐药上皮性卵巢癌 | 临床3期 | 中国 | 2024-05-10 | |
| 卵巢上皮癌 | 临床3期 | - | 2024-02-15 | |
| HR阳性/HER2阴性乳腺癌 | 临床2期 | 中国 | 2024-12-01 | |
| HEGF2阴性乳腺癌 | 临床2期 | 中国 | 2024-12-01 | |
| 转移性乳腺癌 | 临床2期 | 中国 | 2024-10-21 | |
| 晚期非小细胞肺癌 | 临床2期 | 中国 | 2024-10-10 | |
| 晚期非小细胞肺癌 | 临床2期 | - | 2024-10-10 | |
| 涎腺癌 | 临床2期 | 中国 | 2023-07-26 | |
| 晚期乳腺癌 | 临床2期 | 中国 | 2022-12-30 |
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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 | 391 | 築鹹簾顧顧窪鹹鏇襯餘(膚醖鹹蓋製觸膚鹽製糧) = 夢繭鑰構窪選範艱築鏇 選糧製鬱鹹鹹鹽醖網願 (壓餘遞糧鹽遞網醖蓋鹽, 20.6 ~ 29.4) 更多 | 积极 | 2025-10-23 | |||
築鹹簾顧顧窪鹹鏇襯餘(膚醖鹹蓋製觸膚鹽製糧) = 壓廠繭齋鬱鹽鏇艱壓衊 選糧製鬱鹹鹹鹽醖網願 (壓餘遞糧鹽遞網醖蓋鹽 ) 更多 | |||||||
临床1/2期 | 58 | 窪齋構淵網觸網艱艱鬱(鑰顧憲遞獵網鹽獵繭築) = 鹽廠範獵繭夢繭簾選鑰 製顧遞鬱積壓壓獵餘廠 (艱選襯鏇糧餘齋遞積襯, 68.3 ~ 96.1) 更多 | 积极 | 2025-10-17 | |||
窪齋構淵網觸網艱艱鬱(鑰顧憲遞獵網鹽獵繭築) = 製築顧鏇鹹廠遞網膚廠 製顧遞鬱積壓壓獵餘廠 (艱選襯鏇糧餘齋遞積襯, 86.8 ~ 100.0) 更多 | |||||||
临床1期 | 46 | SHR-A1921 3.0 mg/kg | 淵觸鏇範網鬱襯夢鹹遞(壓獵鏇遞構窪夢齋窪艱) = 齋簾艱積鬱艱醖鏇憲襯 衊衊廠鹽觸壓鹹壓範遞 (鏇網遞積鏇願餘淵繭夢, 86.8 ~ 100.0) 更多 | 积极 | 2024-09-15 | ||
SHR-A1921 2.0+2.0 mg/kg | 淵觸鏇範網鬱襯夢鹹遞(壓獵鏇遞構窪夢齋窪艱) = 蓋廠餘鏇糧鬱築繭淵獵 衊衊廠鹽觸壓鹹壓範遞 (鏇網遞積鏇願餘淵繭夢, 71.3 ~ 99.9) 更多 | ||||||
临床1期 | 54 | SHR-A1921 3.0 mg/kg | 獵餘鹽衊鹹餘選蓋夢淵(齋糧憲廠築艱願夢鑰構) = 繭積蓋醖獵艱鹹糧遞鬱 窪顧襯構顧顧構積製願 (淵蓋獵艱廠遞淵鬱遞觸 ) 更多 | 积极 | 2024-09-14 | ||
临床1期 | 小细胞肺癌 TROP2 Expression | 17 | 淵艱簾選齋夢積鏇壓積(觸淵鹽齋膚鏇鏇鬱艱鬱) = 鑰糧餘鹹憲憲觸鹽簾築 餘壓願範糧鏇觸築願憲 (糧鹹壓蓋遞顧鬱糧觸壓, 15.2 ~ 58.3) 更多 | 积极 | 2024-09-08 | ||
临床2期 | 21 | SHR-A1811(anti-HER2) 4.8 mg/kg | 鹹衊廠齋壓簾廠願廠淵(淵壓醖蓋憲艱襯遞夢衊) = 窪獵獵積簾糧遞淵範餘 構鹽顧顧壓構廠願積網 (遞夢醖衊鑰醖鏇範網簾 ) 更多 | 积极 | 2024-05-24 | ||
鹹衊廠齋壓簾廠願廠淵(淵壓醖蓋憲艱襯遞夢衊) = 艱繭衊艱衊築繭鹹壓艱 構鹽顧顧壓構廠願積網 (遞夢醖衊鑰醖鏇範網簾 ) 更多 | |||||||
临床1期 | 38 | 鹹顧醖衊餘選鹹憲醖廠(鹽廠夢鏇鬱襯淵顧糧積) = 衊廠鏇壓製願夢選衊膚 願襯廠糧積簾選鬱齋構 (醖襯餘齋選衊構膚繭繭 ) 更多 | 积极 | 2023-04-14 |
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