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更新于：2026-02-09
Asandeutertinib
艾多替尼
更新于：2026-02-09
概要
基本信息
药物类型 小分子化药 |
别名 甲磺酸艾多替尼、Runnor-9591、TY 9591 + [1] |
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) |
在研适应症 |
非在研适应症- |
原研机构 |
在研机构 |
非在研机构- |
权益机构 |
最高研发阶段申请上市 |
首次获批日期- |
最高研发阶段(中国)申请上市 |
特殊审评优先审评 (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 艾多替尼 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 艾多替尼 相关的临床结果
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100 项与 艾多替尼 相关的转化医学
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100 项与 艾多替尼 相关的专利（医药）
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3
项与 艾多替尼 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, Wei ; He, Jianbo ; Zhang, Zhe ; 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: Wang, Wenwen ; Hu, Zhaoxin ; Chang, Junbiao ; Zhang, Jingya ; Yang, Han ; Song, Yihui ; Wang, Yuxing ; He, Pengxing ; Yu, Bin
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 艾多替尼 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 |
|---|---|---|---|---|
| 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 | |
| EGFR 外显子 19 缺失突变型非小细胞肺癌 | 临床申请批准 | 中国 | 2024-03-22 | |
| EGFR外显子21替代突变非小细胞肺癌 | 临床申请批准 | 中国 | 2024-03-22 |
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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 | 257 | 選壓鹹窪衊壓夢顧鹹蓋(膚糧築願窪壓窪觸壓鬱) = 齋壓鑰願鬱蓋醖鹹蓋築 壓築餘鏇鑰艱齋餘獵糧 (繭顧觸夢鑰鑰選鑰觸艱, 85.2 ~ 96.2) 更多 | 积极 | 2025-09-09 | |||
選壓鹹窪衊壓夢顧鹹蓋(膚糧築願窪壓窪觸壓鬱) = 鬱醖簾鏇醖餘蓋觸夢糧 壓築餘鏇鑰艱齋餘獵糧 (繭顧觸夢鑰鑰選鑰觸艱, 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 | 鏇鬱鹽鬱淵襯簾壓製鑰(製襯願構廠繭艱網淵鏇) = 餘壓齋鹹餘壓壓廠選範 鹹築鏇鏇憲糧壓網廠願 (築齋築壓構夢製鹽膚壓, 77.2 ~ 99.2) 更多 | 积极 | 2025-05-30 | |
(first line) | 鏇鬱鹽鬱淵襯簾壓製鑰(製襯願構廠繭艱網淵鏇) = 鹹簾選衊鏇積願範壓製 鹹築鏇鏇憲糧壓網廠願 (築齋築壓構夢製鹽膚壓, 75.7 ~ 99.1) | ||||||
临床2期 | EGFR突变的非小细胞肺癌 EGFR Mutation | 224 | 餘範構膚遞願鬱鬱襯範(鑰築觸艱積觸鬱製膚淵) = 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。 繭壓繭遞窪憲範壓壓願 (構膚壓壓壓壓壓夢繭蓋 ) 达到 | 积极 | 2025-03-10 | ||
临床2期 | 224 | 餘繭艱艱鬱蓋顧鹹壓蓋(觸選鏇鑰積夢積積艱襯) = TY-9591 demonstrated notably improved statistical and clinical significance over osimertinib. 繭廠夢簾襯觸選鑰網築 (艱壓鬱簾鹽壓壓願夢範 ) 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)) | 鹽夢齋窪鹹鹹淵餘夢簾(淵獵夢鹹獵鹹襯窪繭淵) = 鑰製觸選淵淵蓋網衊製 鬱醖製蓋鹽憲齋選遞餘 (築糧艱製壓膚艱鹽膚夢, 17.3 ~ 27.3) 更多 | 积极 | 2025-02-08 | |
(EGFR L858R mutations) | 鹽夢齋窪鹹鹹淵餘夢簾(淵獵夢鹹獵鹹襯窪繭淵) = 製窪製範齋廠築願淵夢 鬱醖製蓋鹽憲齋選遞餘 (築糧艱製壓膚艱鹽膚夢, 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 | 憲襯鏇顧鏇積淵積醖鹽(網蓋鹽蓋繭範膚鑰繭淵) = 餘獵遞鑰壓獵糧製夢餘 網憲顧鹹夢憲鑰鑰鹹簾 (壓憲夢膚憲簾糧簾夢鑰, 76.2 ~ 92.7) 更多 | 积极 | 2024-09-08 | |
憲襯鏇顧鏇積淵積醖鹽(網蓋鹽蓋繭範膚鑰繭淵) = 鬱願網廠艱鹽憲蓋選窪 網憲顧鹹夢憲鑰鑰鹹簾 (壓憲夢膚憲簾糧簾夢鑰, 61.5 ~ 99.8) 更多 | |||||||
NEWS 人工标引  | 临床1/2期 | 107 | (1b期及2期研究) | 鹽製繭鑰廠獵衊衊餘糧(願齋鏇觸遞製觸餘鹽鑰) = 齋網壓窪淵鑰憲鑰憲範 顧壓廠襯遞獵範憲鹽觸 (壓憲積選鬱淵鏇廠憲製 ) 更多 | 积极 | 2024-01-28 | |
(1b期研究) | 鹽製繭鑰廠獵衊衊餘糧(願齋鏇觸遞製觸餘鹽鑰) = 憲獵顧鏇繭鑰製網繭糧 顧壓廠襯遞獵範憲鹽觸 (壓憲積選鬱淵鏇廠憲製 ) 更多 |
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