预约演示
更新于：2026-07-15
Tepotinib Hydrochloride Hydrate
盐酸特泊替尼
更新于：2026-07-15
概要
基本信息
药物类型 小分子化药 |
别名 Tepotinib、Tepotinib Hydrochloride(USAN)、EMD-1214063 + [6] |
靶点 |
作用方式 抑制剂 |
作用机制 c-Met抑制剂(肝细胞生长因子受体抑制剂) |
在研适应症 |
原研机构 |
非在研机构 |
最高研发阶段批准上市 |
首次获批日期 日本 (2020-03-25), |
最高研发阶段(中国)临床2期 |
特殊审评突破性疗法 (美国)、加速批准 (美国)、孤儿药 (美国)、特殊审批 (中国)、孤儿药 (日本)、孤儿药 (韩国)、孤儿药 (澳大利亚)、快速通道 (日本)、优先审评 (美国) |
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结构/序列
分子式C29H31ClN6O3 |
InChIKeyKZVOMLRKFJUTLK-UHFFFAOYSA-N |
CAS号1946826-82-9 |
关联
40
项与 盐酸特泊替尼 相关的临床试验JPRN-jRCT1031260225
JCOG2506: A randomized phase III trial comparing MET inhibitors versus immune checkpoint inhibitor with or without chemotherapy as first-line treatment for patients with advanced non-small cell lung cancer harboring MET exon.14 skipping mutation. (DECIDE-MET)
NCT07619339
A Pilot Study of Tepotinib + Ivonescimab in Patients With Advanced METex14 Skipping Positive NSCLC
CTR20255027
评估受试制剂盐酸特泊替尼片与参比制剂盐酸特泊替尼片（拓得康®）在餐后状态下作用于健康成年受试者的单中心、开放、随机、单剂量、交叉生物等效性研究
100 项与 盐酸特泊替尼 相关的临床结果
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100 项与 盐酸特泊替尼 相关的转化医学
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100 项与 盐酸特泊替尼 相关的专利（医药）
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303
项与 盐酸特泊替尼 相关的文献（医药）2026-12-31Lung Cancer Management
Cost-effectiveness analysis of tepotinib vs capmatinib as subsequent therapy in MET exon 14-mutated non-small-cell lung cancer
Review
作者: Zhong, Lu ; Liu, Tong ; Liu, Mengmeng
BACKGROUND:
This study evaluated the cost-effectiveness of Tepotinib versus Capmatinib in patients with advanced or metastatic non-small cell lung cancer (NSCLC) with MET Exon 14 Skipping Mutations in China.
METHODS:
An economic evaluation using a 3-state partitioned survival model assessed the cost-effectiveness of Tepotinib versus Capmatinib. The Kaplan-Meier (KM) curves for overall survival (OS) and progression-free survival (PFS) from two clinical trials were digitally extracted. The Exponential model with matching-adjusted indirect comparison (MAIC) was employed at the end of the trials to extrapolate the long-term survivals.
RESULTS:
The estimated cost and utility of Tepotinib treatment were higher than those of Capmatinib treatment, respectively (95,392.54 USD vs. 51,003.63 USD; 2.11 QALYs vs 1.38 QALYs). The incremental cost-effectiveness ratio (ICER) of Capmatinib treatment vs. Tepotinib treatment was calculated at 60,977.28 USD/QALY.
CONCLUSIONS:
Tepotinib was not cost-effective compared to Capmatinib as the second-line treatment for advanced or metastatic NSCLC patients with MET exon 14 skipping mutations in China.
2026-12-31RENAL FAILURE
A tri-scale in silico framework integrating pharmacovigilance and mechanistic modeling suggests tepotinib-associated acute kidney injury risk
Article
作者: Bai, Zhixun ; Wang, Qin ; Zheng, Rubin ; Lyu, Jiayi ; Han, Jinfen ; Lu, Jing ; Deng, Miao ; Chen, Jiaxi
Proactive safety evaluation of molecularly targeted therapies requires generalizable frameworks that integrate real-world evidence with mechanistic insights. As a case in point, tepotinib, a mesenchymal-epithelial transition (MET) inhibitor for non-small cell lung cancer, has a known pulmonary toxicity profile, but its link to acute kidney injury (AKI) and underlying mechanism remain unclear. We devised a tri-scale in silico strategy encompassing population-scale pharmacovigilance signal extraction from the FDA Adverse Event Reporting System (FAERS) (2020-2025) via disproportionality analysis (Reporting Odds Ratio, ROR, and Proportional Reporting Ratio, PRR), network toxicology-based multi-target exploration for shared target and hub gene identification, and mechanistic docking-based molecular plausibility assessment using the Cavity-detection guided Blind Docking (CB-Dock2) platform. Pharmacovigilance analysis identified a significant renal impairment signal (ROR = 20.60). Network toxicology suggested potential nephrotoxicity and revealed 173 shared targets and prioritizing six hub genes (HSP90AA1, AKT1, EGFR, CASP3, TNF, SRC). These genes were shown to be critically involved in PI3K-Akt and MAPK pathways. Molecular docking revealed high-affinity binding between tepotiniband all six hub targets (Vina scores: -8.0 to -10.6 kcal/mol), providing a structural basis for the postulated mechanistic link to AKI. These findings not only highlight the necessity for enhanced renal monitoring in tepotinib-treated patients but, more broadly, establish the FAERS-NetDock Pipeline as a reusable, generalizable and hypothesis-generating framework for evaluating tyrosine kinase inhibitors (TKIs)-induced nephrotoxicity; this framework is immediately applicable to profiling the safety of other TKIs (e.g. crizotinib, capmatinib, savolitinib, afatinib and osimertinib) and is readily adaptable for de-risking a wider spectrum of targeted therapies.
2026-09-01EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
A novel c-Met inhibitor containing chiral pyrrolidine side chain and its application as anti-tumor agents
Article
作者: Li, Jianxin ; Ren, Yuanyuan ; Yao, Han ; Li, Xingshu ; Cen, Xueping ; Hou, Puzhuang ; Jia, Xian ; Wen, Yuying ; Cao, Longcai ; Qin, Xiaojin ; Zhi, Haitao
c-Met inhibitors have demonstrated encouraging efficacy in the treatment of non-small cell lung cancer. However, some of these drugs are conditionally approved and still face certain limitations and challenges, primarily manifested as poor blood-brain barrier penetration, off-target toxicity, drug resistance, and low oral bioavailability. These factors restrict their clinical efficacy and widespread application. To discover novel c-Met inhibitors with high potency, minimal toxic side effects, and the ability to penetrate the blood-brain barrier, we designed and synthesized 33 new pyrimidine derivatives using Tepotinib as the lead, employing bioisosterism and conformational restriction strategies. Their anti-tumor activities were evaluated in vitro and in vivo. Among these derivatives, the optimal compound 11g exhibited IC50 values of 4.01 nM and 3.50 nM against MHCC97H and EBC-1 cells, respectively. In the EBC-1 xenograft mouse model, at a dose of 4 mg/kg, 11g achieved a tumor growth inhibition (TGI) rate of 64.9%, which was significantly higher than that of Tepotinib (33.5%) at the same dose. Pathological evaluation further confirmed that 11g possessed improved safety and reduced toxic side effects. In addition, 11g displayed superior blood-brain barrier permeability and metabolic stability compared with the lead compound. Mechanistic studies demonstrated that 11g effectively inhibits tumor cell proliferation and migration by binding to the c-Met protein and induces cell apoptosis. In summary, as a novel and highly potent c-Met inhibitor, 11g shows promising potential for the treatment of NSCLC, particularly in the prevention and treatment of tumor brain metastasis.
100 项与 盐酸特泊替尼 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 |
|---|---|---|---|
| MET外显子14跳变的非小细胞肺癌 | 韩国 | 2021-11-23 | |
| 非小细胞肺癌 | 美国 | 2021-02-03 | |
| c-Met阳性非小细胞肺癌 | 日本 | 2020-03-25 |
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 |
|---|---|---|---|---|
| RAS/BRAF基因野生型结直肠癌 | 临床2期 | 美国 | 2021-01-28 | |
| RAS/BRAF基因野生型结直肠癌 | 临床2期 | 比利时 | 2021-01-28 | |
| RAS/BRAF基因野生型结直肠癌 | 临床2期 | 捷克 | 2021-01-28 | |
| RAS/BRAF基因野生型结直肠癌 | 临床2期 | 法国 | 2021-01-28 | |
| RAS/BRAF基因野生型结直肠癌 | 临床2期 | 意大利 | 2021-01-28 | |
| RAS/BRAF基因野生型结直肠癌 | 临床2期 | 俄罗斯 | 2021-01-28 | |
| RAS/BRAF基因野生型结直肠癌 | 临床2期 | 西班牙 | 2021-01-28 | |
| RAS/BRAF基因野生型结直肠癌 | 临床2期 | 英国 | 2021-01-28 | |
| 晚期恶性实体瘤 | 临床2期 | 韩国 | 2020-01-16 | |
| 乳腺癌 | 临床2期 | 韩国 | 2020-01-16 |
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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 | MET外显子14跳变的非小细胞肺癌 MET exon 14 skipping | 26 | (MET exon 14 skipping NSCLC + Duration of Response >36 months) | 憲壓壓鹽獵醖襯獵糧繭(淵廠選遞簾齋淵襯齋製) = In 12 patients who discontinued treatment, reasons for discontinuation were: adverse events (5 patients [peripheral edema in 2 patients]), disease progression per investigator (3 patients), non-compliance (1 patient), consent withdrawal (1 patient), and other reasons (2 patients). 獵選糧窪鹽壓網餘醖簾 (繭艱築鏇廠餘選製壓範 ) 更多 | 积极 | 2026-05-29 | |
N/A | MET基因扩增非小细胞肺癌 MET gene copy number | 16 | 淵繭齋顧壓遞窪淵壓顧(觸廠獵顧鏇網顧簾醖遞) = 蓋窪鹽獵鑰觸顧窪鑰衊 醖鑰廠齋顧齋簾觸餘鏇 (壓醖壓醖簾糧製鹹製簾, 2 ~ 26) 更多 | 积极 | 2025-12-05 | ||
淵繭齋顧壓遞窪淵壓顧(觸廠獵顧鏇網顧簾醖遞) = 窪範廠鑰遞顧遞夢鑰艱 醖鑰廠齋顧齋簾觸餘鏇 (壓醖壓醖簾糧製鹹製簾, 3 ~ 24) 更多 | |||||||
N/A | MET外显子14跳变的非小细胞肺癌 MET exon 14 skipping mutations | 55 | 衊糧積衊鏇製餘鏇製壓(觸壓鬱觸鹹餘網憲遞鹹) = 糧鑰淵憲遞簾積選觸憲 簾鑰夢齋餘願構鑰廠顧 (鹹製艱壓艱醖壓製獵艱 ) 更多 | 积极 | 2025-12-05 | ||
(1L) | 衊糧積衊鏇製餘鏇製壓(觸壓鬱觸鹹餘網憲遞鹹) = 艱網餘壓鑰獵積網築鹽 簾鑰夢齋餘願構鑰廠顧 (鹹製艱壓艱醖壓製獵艱 ) 更多 | ||||||
N/A | MET外显子14跳变的非小细胞肺癌 MET exon 14 skipping | 62 | (Brain Metastases) | 鏇糧窪顧繭憲積簾鹹鑰(廠範構壓窪壓糧糧願醖) = 餘醖蓋齋憲選鏇餘襯築 顧衊衊鹽膚簾範憲遞衊 (製鹽膚遞衊範遞獵簾範 ) 更多 | 积极 | 2025-10-17 | |
(No Brain Metastases) | 獵簾顧膚齋醖築糧顧襯(蓋遞廠網艱窪範襯淵繭) = 積鬱製願廠築膚襯壓窪 構衊蓋艱構範鏇鹹鏇憲 (願網觸鹽餘憲窪艱憲遞, 1.7 ~ 12.1) 更多 | ||||||
N/A | 98 | 艱糧製淵壓製廠願醖鏇(壓壓醖艱襯範蓋憲淵醖) = Grade 3 or higher edema occurring in 12.9% of the patients 積壓範遞選鬱蓋餘蓋範 (鑰鑰製廠醖製膚艱構糧 ) | 积极 | 2025-05-30 | |||
Immune Checkpoint Inhibitors | |||||||
临床2期 | 313 | 製憲願淵廠顧鬱膚艱選(蓋觸鹽鹹願鑰憲鬱選夢) = 15.7% of pts discontinued treatment due to TRAEs 範製網獵獵顧襯襯遞範 (獵糧襯願糧廠鑰鑰襯鏇 ) 更多 | 积极 | 2025-03-26 | |||
临床2期 | 128 | (progression on first-line osimertinib) | 醖憲襯鏇範蓋衊艱艱鹹(憲襯鏇簾壓膚鹹遞蓋鹹) = 膚鹹繭鹽憲憲積壓網蓋 鹹壓醖顧醖鏇衊醖蓋簾 (鬱遞鹽鏇製蓋窪蓋積遞, 39.7 ~ 60.3) 更多 | 积极 | 2024-08-25 | ||
临床1期 | 18 | (Healthy Participants (Control)) | 網鹽艱醖築鹽繭願夢遞(簾鹽獵簾選齋膚鏇選築) = 簾網壓遞憲鬱鹹獵糧糧 齋糧醖積壓糧衊獵鏇鬱 (糧窪築衊繭選獵遞夢廠, 13.4) 更多 | - | 2024-08-12 | ||
(Mild Hepatic Impairment (Child-Pugh Class A)) | 網鹽艱醖築鹽繭願夢遞(簾鹽獵簾選齋膚鏇選築) = 艱獵顧鏇窪繭艱繭遞窪 齋糧醖積壓糧衊獵鏇鬱 (糧窪築衊繭選獵遞夢廠, 63.9) 更多 | ||||||
临床2期 | 140 | (Tepotinib Mono-therapy) | 構鏇簾遞艱糧鏇艱衊膚(夢構願壓製襯壓選襯壓) = 夢艱廠製餘膚構鑰築艱 蓋襯顧鬱鑰選構鏇壓齋 (範艱網廠壓築積蓋網範, 餘餘鑰醖簾鏇糧積蓋鏇 ~ 範簾鏇願範顧鏇簾範網) 更多 | - | 2024-06-04 | ||
(Tepotinib and Osimertinib) | 構鏇簾遞艱糧鏇艱衊膚(夢構願壓製襯壓選襯壓) = 網鑰憲鹽選願繭廠觸憲 蓋襯顧鬱鑰選構鏇壓齋 (範艱網廠壓築積蓋網範, 構窪鏇築獵鹽鹹餘鬱夢 ~ 鹹觸鏇憲觸艱鬱窪醖醖) 更多 | ||||||
临床2期 | 248 | (Brain metastases) | 選積憲窪壓鬱夢構製壓(糧餘鹹觸繭糧襯膚鬱淵) = 齋鑰網蓋選鬱鏇糧窪糧 鏇憲獵鹽築餘糧鏇獵願 (夢遞積遞壓淵願廠鬱製, 2.41) 更多 | 积极 | 2024-05-24 | ||
(Liver metastases) | 選積憲窪壓鬱夢構製壓(糧餘鹹觸繭糧襯膚鬱淵) = 鑰獵淵夢觸餘壓鏇網鑰 鏇憲獵鹽築餘糧鏇獵願 (夢遞積遞壓淵願廠鬱製, 2.27) 更多 |
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