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更新于：2026-02-07
AMG-337
更新于：2026-02-07
概要
基本信息
原研机构 |
在研机构- |
最高研发阶段终止临床2期 |
首次获批日期- |
最高研发阶段(中国)无进展 |
特殊审评- |
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结构/序列
分子式C23H22FN7O3 |
InChIKeyDWHXUGDWKAIASB-CQSZACIVSA-N |
CAS号1173699-31-4 |
关联
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项与 AMG-337 相关的临床试验NCT03132155
A Phase 2 Study of AMG 337 in Subjects With Advanced or Metastatic Clear Cell Sarcoma That Contains the Ewing Sarcoma Breakpoint Region 1-activating Transcription Factor-1 (EWSR1-ATF1) Gene Fusion
NCT03147976
A Phase 2 Study of AMG 337 in Subjects With Advanced or Metastatic Solid Tumors That Overexpress Mesenchymal Epithelial Transition (MET) or Harbor MET Exon 14 Skipping (METex14del) Mutations
NCT02096666
A Multicenter, Phase 1/2, Open-Label Study Evaluating the Tolerability, Safety, Pharmacokinetics, and Efficacy of AMG 337 in Asian Subjects
100 项与 AMG-337 相关的临床结果
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100 项与 AMG-337 相关的转化医学
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100 项与 AMG-337 相关的专利（医药）
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19
项与 AMG-337 相关的文献（医药）2025-05-01CTS-Clinical and Translational Science
Restraint‐Based ECG and Arterial Pressure Assessment Do Not Reliably Detect Drug Induced QTc Prolongation and Hypotension: Evidence From Case Studies
Article
作者: Vargas, Hugo M. ; Henderson, Kim A. ; Ether, Nicholas
ABSTRACT:
Telemetry‐based methods are recommended as best practice for monitoring changes in cardiovascular (CV) function in conscious nonrodent species during the development of new chemical entities. Such methods allow for unrestrained data collection in animals over extended time periods with high sensitivity to detect small effects. The CV profile of new drugs is also assessed in repeat‐dose toxicology studies, routinely utilizing non‐invasive blood pressure, heart rate, and ECG measurement methods that require physical or chemical restraint. These methods are limited to a short “snapshot” data collection period and incur physiological stress and behavioral excitement from handling/restraint during data collection. The resultant sympathetic activation impacts heart rate, blood pressure, and ECG intervals, causing increased variability and reduced sensitivity. Nonclinical best practices have been defined for standalone CV telemetry studies to support an integrated QTc risk assessment (ICH E14/S7B Q&A 5.1 & 6.1) using non‐restraint telemetry methods; however, the pharmacological and statistical sensitivity of restraint‐based methods used in repeat‐dose toxicology studies is a gap. This paper retrospectively analyzed two case studies (AMG 319 and AMG 337) in which proprietary small molecules were evaluated by both non‐restraint‐based telemetry and restraint‐based methods. AMG 319 and AMG 337 caused QTc interval prolongation and hypotension, respectively, in telemetry studies, which were also observed clinically with these compounds. However, in toxicology studies in which restraint‐based ECG and blood pressure methods were used, CV effects were missed, blunted, or directionally wrong. These case studies highlight the need for the utilization of unrestrained telemetry methods over restraint‐based methods.
2023-03-01iScience
Tivantinib alleviates inflammatory diseases by directly targeting NLRP3
Article
作者: Xu, Wen ; Zhou, Yan ; Huang, Qian ; Huang, Yi ; Guo, Yun ; Luo, Yingli ; Ru, Yi
NLRP3 inflammasome-mediated immune responses are involved in the pathogenesis of multiple inflammatory diseases, but few clinical drugs are identified that directly target the NLRP3 inflammasome to treat these diseases to date. Here, we show that the anticancer agent tivantinib is a selective inhibitor of NLRP3 and has a strong therapeutic effect on inflammasome-driven disease. Tivantinib specifically inhibits canonical and non-canonical NLRP3 inflammasome activation without affecting AIM2 and NLRC4 inflammasome activation. Mechanistically, Tivantinib inhibits NLRP3 inflammasome by directly blocking NLRP3 ATPase activity and subsequent inflammasome complex assembly. In vivo, Tivantinib reduces IL-1β production in mouse models of lipopolysaccharide (LPS)-induced systemic inflammation, monosodium urate (MSU)-induced peritonitis and Con A-induced acute liver injury (ALI), and also has remarkable preventive and therapeutic effects on experimental autoimmune encephalomyelitis (EAE). In conclusion, our study identifies the anticancer drug tivantinib as a specific inhibitor of NLRP3 and provides a promising therapeutic agent for inflammasome-driven disease.
2021-11-01Neoplasia (New York, N.Y.)2区 · 医学
Ovulation sources coagulation protease cascade and hepatocyte growth factor to support physiological growth and malignant transformation
2区 · 医学
ArticleOA
作者: Huang, Chi-Ya ; Chu, Tang-Yuan ; Huang, Hsuan-Shun ; Chu, Sung-Chao ; Lee, Ming-Hsun ; Chen, Pao-Chu
The fallopian tube fimbrial epithelium, which is exposed to the follicular fluid (FF) contents of ovulation, is regarded as the main origin of ovarian high-grade serous carcinoma. Previously, we found that growth factors in FF, such as IGF2, are responsible for the malignant transformation of fallopian tube epithelium. However, ovulation is a monthly transient event, whereas carcinogenesis requires continuous, long-term exposure. Here, we found the transformation activity of FF sustained for more than 30 days after drainage into the peritoneal fluid (PF). Hepatocyte growth factor (HGF), activated through the ovulation injury-tissue factor-thrombin-HGF activator (HGFA)-HGF cleavage cascade confers a sustained transformation activity to fallopian tube epithelium, high-grade serous carcinoma. Physiologically, the high reserve of the coagulation-HGF cascade sources a sustained level of HGF in PF, then to the blood circulation. This HGF axis promotes the growth of the corpus luteum and repair of tissue injury after ovulation.
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项与 AMG-337 相关的新闻（医药）2025-12-30
100 项与 AMG-337 相关的药物交易
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外链
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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 |
|---|---|---|---|---|
| 透明细胞肉瘤 | 临床2期 | 美国 | 2018-08-29 | |
| 尤文肉瘤 | 临床2期 | 美国 | 2018-08-29 | |
| 转移性实体瘤 | 临床2期 | 美国 | 2018-05-02 | |
| 实体瘤 | 临床2期 | 美国 | 2018-05-02 | |
| 胃癌 | 临床2期 | 日本 | 2015-01-28 | |
| 食管腺癌 | 临床2期 | 美国 | 2014-02-01 | |
| 食管腺癌 | 临床2期 | 澳大利亚 | 2014-02-01 | |
| 食管腺癌 | 临床2期 | 奥地利 | 2014-02-01 | |
| 食管腺癌 | 临床2期 | 比利时 | 2014-02-01 | |
| 食管腺癌 | 临床2期 | 加拿大 | 2014-02-01 |
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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 | 8 | 鏇餘艱簾觸憲衊襯製餘 = 網憲窪糧顧遞壓鹽齋醖 選遞製觸鹽積製蓋糧鹽 (選鑰餘鹹選鏇壓窪鬱襯, 衊餘齋鏇選積鑰鏇顧簾 ~ 襯觸願範憲夢獵顧網襯) 更多 | - | 2024-05-24 | |||
临床2期 | 60 | (MET-amplified G/GEJ/E adenocarcinoma) | 糧簾餘觸夢鑰製鹽糧廠(膚積膚膚簾壓獵襯醖餘) = 鏇觸鑰選製廠淵範鹽範 遞齋構觸鹹構遞衊鏇鹽 (醖簾夢憲鹹餘選觸蓋鹽 ) | 积极 | 2019-04-15 | ||
(other MET-amplified solid tumors) | 糧簾餘觸夢鑰製鹽糧廠(膚積膚膚簾壓獵襯醖餘) = 糧憲醖餘廠簾願觸製選 遞齋構觸鹹構遞衊鏇鹽 (醖簾夢憲鹹餘選觸蓋鹽 ) | ||||||
临床1期 | 111 | 顧範餘繭餘襯鹹膚構選(獵繭壓鹹製艱餘衊簾窪) = 鹹醖餘廠餘艱鑰鑰願觸 壓鏇餘膚齋膚艱築艱繭 (醖憲構構廠觸鑰願製簾 ) 更多 | 积极 | 2019-04-15 | |||
临床1期 | 11 | 簾顧夢鑰膚範餘醖膚鏇(遞憲遞鹽艱選醖蓋顧糧) = 蓋淵顧窪艱遞顧夢襯糧 餘膚構廠廠構選繭醖鬱 (窪衊壓鏇繭齋繭壓窪鬱 ) 更多 | 积极 | 2017-08-01 |
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