预约演示
更新于：2026-09-09
Asandeutertinib Mesylate
甲磺酸氘申艾替尼
更新于：2026-09-09
概要
基本信息
药物类型 小分子化药 |
别名 Asandeutertinib、氘申艾替尼、甲磺酸氘申艾替尼 + [5] |
作用方式 抑制剂 |
作用机制 EGFR T790M抑制剂(表皮生长因子受体T790M抑制剂) |
非在研适应症- |
原研机构 |
在研机构 |
非在研机构- |
权益机构 |
最高研发阶段批准上市 |
首次获批日期 中国 (2026-08-25), |
最高研发阶段(中国)批准上市 |
特殊审评附条件批准 (中国)、优先审评 (中国) |
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结构/序列
分子式C28H33N7O2 |
InChIKeyDUYJMQONPNNFPI-VPYROQPTSA-N |
CAS号1638281-46-5 |
关联
7
项与 甲磺酸氘申艾替尼 相关的临床试验NCT06672068
To Evaluate the Efficacy and Safety of TY-9591 Tablets Combined With Chemotherapy as First-line Treatment in Patients With Locally Advanced or Metastatic Non-small Cell Lung Cancer (NSCLC) Harboring EGFR Mutation
NCT05948813
A Phase II Study of TY-9591 Tablets in Patients With EGFR-Mutated Non-small Cell Lung Cancer With Brain Metastases
NCT05871905
[14 C] Study on Mass Balance of TY-9591 in Healthy Chinese Adult Male Subjects
100 项与 甲磺酸氘申艾替尼 相关的临床结果
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100 项与 甲磺酸氘申艾替尼 相关的转化医学
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100 项与 甲磺酸氘申艾替尼 相关的专利（医药）
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3
项与 甲磺酸氘申艾替尼 相关的文献（医药）2025-06-01Journal of Thoracic Oncology
Old Wine in New Bottles? Deuterium Switch (Replacing Hydrogen With Deuterium) Comes to Thoracic Oncology as Deuterated Lorlatinib (Deulorlatinib, TGRX-326) and Deuterated Osimertinib (Asandeutertinib, TY-9591) in ALK+ NSCLC and EGFR+ NSCLC, Respectively
作者: Park, Cathleen June ; Li, Molly Siu-Ching ; Ou, Sai-Hong Ignatius
2025-06-01Journal of Thoracic Oncology
Safety, Pharmacokinetics, and Efficacy of Asandeutertinib in Advanced EGFR-mutated NSCLC: A Phase 1 Dose-Escalation and Dose-Expansion Study
Article
作者: Shi, Jianhua ; Chen, Xiugui ; Zhang, Zhe ; Zhang, Wei ; He, Jianbo ; Chen, Bolin ; Liu, Yanqing ; Han, Baohui ; Liu, Jie ; Zhao, Yanqiu ; Wu, Yusheng ; Wu, Lin
INTRODUCTION:
This phase 1 study evaluated the safety, pharmacokinetics, and preliminary efficacy of TY-9591 (asandeutertinib), a deuterated osimertinib derivative.
METHODS:
Patients with advanced EGFR-mutated (most commonly exon 19 deletions or L858R) NSCLC were enrolled. In the dose-escalation phase, TY-9591 was administered from 20 to 200 mg once daily to assess dose-limiting toxicities and the maximum tolerated dose. In the dose-expansion phase, patients were treated with 80, 120, or 160 mg doses to further evaluate safety, pharmacokinetics, and preliminary efficacy.
RESULTS:
A total of 105 patients were enrolled (dose-escalation: n = 19; dose-expansion: n = 86). During the dose escalation phase, no dose-limiting toxicities were observed, and the maximum tolerated dose was not reached. Treatment-related adverse events (TRAEs) were reported in 100 patients (95.2%). The most common TRAEs were decreased white blood cell count (54.3%), decreased neutrophil count (46.7%), increased blood creatine phosphokinase (39.0%), and anemia (39.0%). Of these patients, 32 (30.5%) experienced grade 3 or higher TRAEs. Pharmacokinetic analysis found that TY-9591 had a favorable profile with reduced levels of active metabolites. During the dose-expansion phase (n = 79), the median progression-free survival for first-line EGFR-mutated (exon 19 deletions or L858R) NSCLC was 21.5 months (95% confidence interval [CI]: 17.3-27.3), whereas the confirmed objective response rate was 85.9% (95% CI: 76.2-92.7). In patients with L858R mutations (n = 36), the median progression-free survival was 19.3 months (95% CI: 13.1-23.5), and the confirmed objective response rate was 86.1% (95% CI: 70.5-95.3).
CONCLUSION:
TY-9591 reported a favorable safety profile and substantial efficacy in treating EGFR-mutated NSCLC, particularly in patients with L858R mutations.
2025-03-13JOURNAL OF MEDICINAL CHEMISTRY
Structure-Based Design of New LSD1/EGFRL858R/T790M Dual Inhibitors for Treating EGFR Mutant NSCLC Cancers
Article
作者: Bin Yu ; Han Yang ; Junbiao Chang ; Yihui Song ; Zhaoxin Hu ; Yuxing Wang ; Pengxing He ; Wenwen Wang ; Jingya Zhang
Epigenetic changes, such as LSD1 dysregulation, contribute to acquired resistance in EGFR mutant NSCLCs and reduce the effectiveness of current therapeutics. To address the challenges, we herein reported the structure-based design of new LSD1/EGFR dual inhibitors, of which ZJY-54 represents the shortlisted lead compound with high potency, selectivity, and unique dual modes of action (namely irreversibly binding to EGFR but reversibly binding to LSD1). ZJY-54 effectively inhibited growth in both parent- and TKI-resistant NSCLC cells. In H1975 cells, ZJY-54 induced accumulation of H3K4me2 and H3K9me2, as well as inhibited phosphorylation of EGFR signaling. ZJY-54 showed favorable PK profiles and effectively inhibited tumor growth in the H1975 xenograft model. ZJY-54 represents the best-in-class LSD1/EGFR dual inhibitor and warrants further preclinical development for treating NSCLCs. These findings highlight the therapeutic potential of LSD1/EGFR dual inhibitors in drug-resistant cancers where EGFR and LSD1 were dysregulated.
100 项与 甲磺酸氘申艾替尼 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| EGFR 外显子 19 缺失突变型非小细胞肺癌 | 中国 | 2026-08-25 | |
| EGFR外显子21替代突变非小细胞肺癌 | 中国 | 2026-08-25 |
未上市
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 |
|---|---|---|---|---|
| 局部晚期非小细胞肺癌 | 临床3期 | 中国 | 2022-06-08 | |
| EGFR突变的非小细胞肺癌 | 临床3期 | 中国 | 2022-05-30 | |
| 转移性非小细胞肺癌 | 临床3期 | 中国 | 2022-05-30 | |
| 非鳞状非小细胞肺癌 | 临床2期 | - | 2025-02-20 | |
| 脑转移瘤 | 临床2期 | 中国 | 2022-04-02 | |
| 软脑膜转移性恶性肿瘤 | 临床2期 | 中国 | 2022-04-02 |
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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2期 | 224 | 願觸艱壓窪壓艱遞蓋網(齋憲醖糧網艱齋鬱構膚) = 選醖範網醖遞選鹽蓋鹹 選膚餘壓範築鹽簾鹹襯 (獵衊遞鹽積範繭醖選糧, 89.8 ~ 98.5) 更多 | 积极 | 2026-05-29 | |||
願觸艱壓窪壓艱遞蓋網(齋憲醖糧網艱齋鬱構膚) = 壓壓衊範衊鬱願鏇醖築 選膚餘壓範築鹽簾鹹襯 (獵衊遞鹽積範繭醖選糧, 71.0 ~ 86.6) 更多 | |||||||
临床2期 | 257 | 範餘蓋製鬱繭願醖憲膚(襯壓網襯淵願鹽憲襯鏇) = 窪齋齋壓廠壓鬱齋製簾 餘艱積觸製壓網餘壓鹽 (鹹簾網鏇鹽窪夢獵遞鹹, 85.2 ~ 96.2) 更多 | 积极 | 2025-09-09 | |||
範餘蓋製鬱繭願醖憲膚(襯壓網襯淵願鹽憲襯鏇) = 齋構遞衊獵襯製製顧遞 餘艱積觸製壓網餘壓鹽 (鹹簾網鏇鹽窪夢獵遞鹹, 67.2 ~ 83.6) 更多 | |||||||
临床2期 | EGFR阳性非小细胞肺癌 EGFR Mutation | 29 | Asandeutertinib 160 mg once daily | 窪鏇範鏇遞襯遞醖範製(獵遞願醖廠鬱網構築獵) = 鬱壓觸憲窪簾積鏇構網 襯壓壓構顧糧遞遞廠廠 (壓醖鏇選構築鏇鹽製醖, 77.2 ~ 99.2) 更多 | 积极 | 2025-05-30 | |
(first line) | 窪鏇範鏇遞襯遞醖範製(獵遞願醖廠鬱網構築獵) = 鏇鏇遞簾窪鹹淵齋鹹餘 襯壓壓構顧糧遞遞廠廠 (壓醖鏇選構築鏇鹽製醖, 75.7 ~ 99.1) | ||||||
临床2期 | EGFR突变的非小细胞肺癌 EGFR Mutation | 224 | 獵膚鬱簾醖簾願蓋壓鹽(繭醖艱鹽鹹鹹蓋願構遞) = TY-9591在颅内客观缓解率（iORR）达到预期，对比奥希替尼显示出统计学意义和临床意义的明显改善。 願餘鏇醖餘憲餘構鏇鬱 (範膚醖夢遞廠廠夢簾衊 ) 达到 | 积极 | 2025-03-10 | ||
临床2期 | 224 | 繭鹽顧蓋遞觸願夢鬱鹹(選簾簾鑰齋鏇築繭蓋積) = TY-9591 demonstrated notably improved statistical and clinical significance over osimertinib. 淵夢艱衊壓簾壓鹹鏇願 (網顧構蓋鏇鹹夢築顧艱 ) 达到 | 积极 | 2025-03-09 | |||
临床1期 | EGFR突变的非小细胞肺癌 EGFR Exon 19 Deletion | EGFR Mutation | EGFR L858R | 105 | (first-line EGFR-mutated (exon 19 deletions or L858R)) | 遞壓構憲夢鹹壓夢選醖(糧築壓餘糧繭積廠衊製) = 構遞觸膚齋積願築窪膚 構膚顧製糧鏇構鹽憲艱 (繭簾壓鹽繭遞願築窪醖, 17.3 ~ 27.3) 更多 | 积极 | 2025-02-08 | |
(EGFR L858R mutations) | 遞壓構憲夢鹹壓夢選醖(糧築壓餘糧繭積廠衊製) = 積製鏇簾願膚範築顧壓 構膚顧製糧鏇構鹽憲艱 (繭簾壓鹽繭遞願築窪醖, 13.1 ~ 23.5) 更多 | ||||||
临床1期 | EGFR阳性非小细胞肺癌 EGFR Positive | 105 | TY-9591 20mg | 顧觸膚襯壓選築構衊夢(鬱艱鏇淵餘醖醖觸糧糧) = 積醖獵淵憲蓋鑰鏇繭糧 淵廠襯鑰窪壓鬱壓獵築 (鑰觸襯觸衊鹹繭簾鹹壓, 76.2 ~ 92.7) 更多 | 积极 | 2024-09-08 | |
顧觸膚襯壓選築構衊夢(鬱艱鏇淵餘醖醖觸糧糧) = 鹹鏇範鬱艱膚願鏇製選 淵廠襯鑰窪壓鬱壓獵築 (鑰觸襯觸衊鹹繭簾鹹壓, 61.5 ~ 99.8) 更多 | |||||||
NEWS 人工标引  | 临床1/2期 | 107 | (1b期及2期研究) | 築觸廠繭選願遞衊鏇艱(願艱積鑰鹽夢鹽糧襯遞) = 築憲鹹艱鬱築艱觸願齋 觸構鹹淵獵鹽鬱醖壓糧 (憲壓蓋繭願齋鏇壓夢淵 ) 更多 | 积极 | 2024-01-28 | |
(1b期研究) | 築觸廠繭選願遞衊鏇艱(願艱積鑰鹽夢鹽糧襯遞) = 醖觸窪衊衊淵糧窪齋鏇 觸構鹹淵獵鹽鬱醖壓糧 (憲壓蓋繭願齋鏇壓夢淵 ) 更多 |
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