预约演示
更新于：2025-11-13
Lenvatinib mesylate
甲磺酸仑伐替尼
更新于：2025-11-13
概要
基本信息
药物类型 小分子化药 |
别名 lenvatinib、lenvatinib mesilate、Lenvatinib mesilate (JAN) + [19] |
作用方式 拮抗剂、抑制剂 |
作用机制 FGFR1拮抗剂(成纤维细胞生长因子受体-1拮抗剂)、FGFR2拮抗剂(成纤维细胞生长因子受体-2拮抗剂)、FGFR3拮抗剂(成纤维细胞生长因子受体-3拮抗剂) |
原研机构 |
最高研发阶段批准上市 |
首次获批日期 美国 (2015-02-13), |
最高研发阶段(中国)批准上市 |
特殊审评突破性疗法 (美国)、加速批准 (美国)、孤儿药 (美国)、优先审评 (中国)、特殊审批 (中国)、孤儿药 (澳大利亚)、优先审评 (澳大利亚)、附条件批准 (中国)、孤儿药 (日本) |
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结构/序列
分子式C22H23ClN4O7S |
InChIKeyHWLFIUUAYLEFCT-UHFFFAOYSA-N |
CAS号857890-39-2 |
关联
698
项与 甲磺酸仑伐替尼 相关的临床试验NCT06669572
A Phase II, Multi-center, Single Arm Trial of Lenvatinib Plus Pembrolizumab in Patients With Unresectable Locally Advanced and/or Metastatic Anorectal Squamous Cell Carcinoma (ASCC) After Progression on First Line Chemotherapy.
NCT05077215
A Phase 3, Randomized, Open-Label, Active-Controlled, Superiority Trial of EG007, Added to the Combination of Lenvatinib Plus Pembrolizumab Vs. Lenvatinib Plus Pembrolizumab in Patients with Advanced Endometrial Cancer
ChiCTR2500111466
The efficacy and safety of Iparomlimab and Tuvonralimab (QL1706) combined with Lenvatinib as neoadjuvant therapy in renal cancer with partial nephrectomy indications but high surgical risk：A single arm, Phase II clinical study
100 项与 甲磺酸仑伐替尼 相关的临床结果
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100 项与 甲磺酸仑伐替尼 相关的转化医学
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100 项与 甲磺酸仑伐替尼 相关的专利（医药）
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3,436
项与 甲磺酸仑伐替尼 相关的文献（医药）2026-01-01MITOCHONDRION
In silico analysis of a MicroRNA regulatory network Influencing mitochondrial fission in hepatocellular carcinoma
Article
作者: Dongre, Nilima ; Akki, Ali Jawad ; Parvatikar, Prachi ; Patil, Shankargouda V
MicroRNAs (miRNAs), small non-coding RNA molecules known for their gene regulatory functions, are increasingly recognized to target genes critical for mitochondrial function in hepatocellular carcinoma (HCC). By employing in silico analysis this research investigates the underexplored involvement of a network of microRNAs in regulating mitochondrial fission within the context of HCC. We constructed a novel regulatory network, identifying hsa-miR-138-5p as a central regulator targeting key mitochondrial genes. Furthermore, we identified druggable binding pockets on the transcription factors WDR5 and HNF4, which regulate hsa-miR-138-5p. Molecular docking studies demonstrated favorable binding affinities of FDA-approved HCC drugs (sorafenib, lenvatinib, and regorafenib) to these binding pockets, suggesting an off-target mechanism by which these drugs might influence mitochondrial function through the hsa-miR-138-5p pathway. These findings contribute to the growing understanding of miRNA-mediated regulation in HCC and offer a foundation for developing novel microRNA-targeting drugs to modulate mitochondrial dynamics to manage HCC progression.
2025-12-31CANCER BIOLOGY & THERAPY
Lenvatinib promotes hepatocellular carcinoma pyroptosis by regulating GSDME palmitoylation
Article
作者: Ding, Yang ; He, Xing-Xing ; Wang, Mu-Ru ; Yuan, Yuan ; Li, Pei-Yuan ; Lin, Ya ; Xu, Ting-Ting
Lenvatinib, as a multi-kinase inhibitor, has been approved as a first-line drug for patients with advanced hepatocellular carcinoma (HCC). Gasdermin E (GSDME)-mediated pyroptosis, a form of programmed cell death, can be induced by chemotherapy drugs or certain kinase inhibitors. However, the role of Lenvatinib in inducing pyroptosis in HCC warrants further investigation. Phase contrast microscopy, LDH assays, and gain- and loss-of-function strategies were used to evaluate Lenvatinib-induced pyroptosis in HCC cells. GSDME palmitoylation was assessed via the acyl-biotin exchange method. In vivo, a subcutaneous HCC xenograft model in nude mice were established to assess the effects of interfering with GSDME on the sensitivity of HCC to Lenvatinib. Lenvatinib induced pyroptosis in HCC cells in a dose- and time-dependent manner. Additionally, Lenvatinib promoted GSDME cleavage, with upregulation of GSDME enhancing pyroptosis and downregulation reducing this effect. The ABE method revealed that GSDME is palmitoylated, and Lenvatinib increased its palmitoylation, promoting plasma membrane localization and enhancing protein stability. Inhibition of GSDME palmitoylation by 2-BP blocked Lenvatinib-induced pyroptosis. In vivo, upregulation of GSDME increased HCC sensitivity to Lenvatinib and inhibited tumor growth. Lenvatinib induces pyroptosis in HCC by promoting the palmitoylation of GSDME, enhancing its localization to the plasma membrane and increasing its protein stability. Interfering with GSDME, both in vitro and in vivo, affects Lenvatinib-induced pyroptosis, thereby altering the therapeutic sensitivity of HCC to Lenvatinib. Targeting GSDME palmitoylation represents a potential therapeutic strategy for HCC, as it enhances Lenvatinib-induced pyroptosis and improves the therapeutic response.
2025-12-31Future Science OA
Immune checkpoint inhibitors or targeted therapy by mismatch repair status in endometrial cancer: a meta-analysis
Review
作者: Zeng, Ting ; Zhao, Jing ; Shu, Chuqiang ; Tang, Yi ; Chen, Yan ; Huang, Kui ; Zhang, Pu
OBJECTIVE:
This study evaluated the benefits of immune checkpoint inhibitors (ICIs) and/or targeted therapies in mismatch repair-deficient (dMMR) and mismatch repair-proficient (pMMR) patients with advanced or recurrent endometrial cancer (EC) via network meta-analysis.
METHODS:
English databases were searched from inception through January 2025. Randomized controlled trials (RCTs) assessing the efficacy and safety of related therapies for patients with EC stratified by MMR status were included. The main evaluation indicators included progression-free survival (PFS), overall survival (OS), the objective response rate (ORR), and severe adverse events (SAEs).
RESULTS:
Ten studies were included in the analysis. The results indicated that in the dMMR population, ICIs provide superior survival benefits. Among these, Dostarlimab combined with carboplatin and paclitaxel (CP) had the highest PFS and OS rates. For the pMMR population, Selinexor + CP offers significant benefits over CP alone, although OS outcome data are limited. In pMMR patients with prior chemotherapy, the lenvatinib + pembrolizumab strategy may provide additional PFS benefits relative to chemotherapy treatment.
CONCLUSIONS:
ICIs offered advantages for the dMMR population, whereas selinexor could provide survival benefits for the pMMR population. For pMMR patients who have received prior chemotherapy, the lenvatinib plus pembrolizumab strategy shows promise.
100 项与 甲磺酸仑伐替尼 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 |
|---|---|---|---|
| 晚期子宫内膜癌 | 欧盟 | 2023-07-25 | |
| 晚期子宫内膜癌 | 冰岛 | 2023-07-25 | |
| 晚期子宫内膜癌 | 列支敦士登 | 2023-07-25 | |
| 晚期子宫内膜癌 | 挪威 | 2023-07-25 | |
| 复发性子宫内膜癌 | 欧盟 | 2023-07-25 | |
| 复发性子宫内膜癌 | 冰岛 | 2023-07-25 | |
| 复发性子宫内膜癌 | 列支敦士登 | 2023-07-25 | |
| 复发性子宫内膜癌 | 挪威 | 2023-07-25 | |
| 胸腺肿瘤 | 日本 | 2021-03-23 | |
| 晚期肾细胞癌 | 欧盟 | 2016-08-25 | |
| 晚期肾细胞癌 | 冰岛 | 2016-08-25 | |
| 晚期肾细胞癌 | 列支敦士登 | 2016-08-25 | |
| 晚期肾细胞癌 | 挪威 | 2016-08-25 | |
| 子宫内膜癌 | 澳大利亚 | 2016-01-28 | |
| 肾细胞癌 | 澳大利亚 | 2016-01-28 | |
| 晚期肝细胞癌 | 欧盟 | 2015-05-28 | |
| 晚期肝细胞癌 | 冰岛 | 2015-05-28 | |
| 晚期肝细胞癌 | 列支敦士登 | 2015-05-28 | |
| 晚期肝细胞癌 | 挪威 | 2015-05-28 | |
| 分化型甲状腺癌 | 欧盟 | 2015-05-28 |
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 |
|---|---|---|---|---|
| 晚期非小细胞肺癌 | 临床3期 | 中国 | 2021-10-28 | |
| 转移性食管癌 | 临床3期 | 美国 | 2021-07-28 | |
| 转移性食管癌 | 临床3期 | 美国 | 2021-07-28 | |
| 转移性食管癌 | 临床3期 | 中国 | 2021-07-28 | |
| 转移性食管癌 | 临床3期 | 中国 | 2021-07-28 | |
| 转移性食管癌 | 临床3期 | 日本 | 2021-07-28 | |
| 转移性食管癌 | 临床3期 | 日本 | 2021-07-28 | |
| 转移性食管癌 | 临床3期 | 阿根廷 | 2021-07-28 | |
| 转移性食管癌 | 临床3期 | 阿根廷 | 2021-07-28 | |
| 转移性食管癌 | 临床3期 | 加拿大 | 2021-07-28 |
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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 | 肝内胆管癌 一线 | 61 | 願簾獵襯獵鏇簾獵網願(廠齋願夢築夢膚襯艱襯) = 遞襯獵遞鏇鑰選鑰壓醖 鹹夢膚艱淵窪獵夢鏇窪 (鹹膚網齋簾艱夢蓋遞襯, 16.7 ~ 51.4) 更多 | 积极 | 2025-10-21 | ||
Lenvatinib+GEMOX | 願簾獵襯獵鏇簾獵網願(廠齋願夢築夢膚襯艱襯) = 願蓋網鑰選遞鬱鏇繭構 鹹夢膚艱淵窪獵夢鏇窪 (鹹膚網齋簾艱夢蓋遞襯, 22.7 ~ 59.4) 更多 | ||||||
临床3期 | 850 | 獵醖餘選夢淵蓋壓鹽築(壓廠簾餘窪艱蓋廠齋蓋) = 齋鬱蓋願顧衊築鬱繭艱 艱餘觸淵網鬱艱願淵製 (廠鏇鹹齋夢糧醖網壓壓 ) 更多 | 不佳 | 2025-10-17 | |||
pembrolizumab + chemotherapy | 獵醖餘選夢淵蓋壓鹽築(壓廠簾餘窪艱蓋廠齋蓋) = 窪艱憲醖膚糧獵醖齋鏇 艱餘觸淵網鬱艱願淵製 (廠鏇鹹齋夢糧醖網壓壓 ) 更多 | ||||||
N/A | 120 | 鑰選遞構窪鑰獵遞壓廠(繭構憲願範築鹽繭壓遞) = occurred in 19 pts (16%) (n=9; 8% related to PD1, n=16 only; 13% related to LENVA only). 範窪繭膚鹹膚遞壓壓製 (網範鹹夢顧鏇構築觸壓 ) 更多 | 积极 | 2025-10-17 | |||
N/A | 复发性子宫内膜癌 二线 | 176 | 淵鹹鹹簾鏇糧餘淵築繭(鑰憲構蓋餘衊襯膚構選) = 鬱積積鹹衊選鏇艱簾鏇 網鹽艱選蓋獵築遞齋膚 (餘壓積構簾餘鑰窪糧廠 ) | 积极 | 2025-10-17 | ||
Chemotherapy (CT) | 淵鹹鹹簾鏇糧餘淵築繭(鑰憲構蓋餘衊襯膚構選) = 鹽繭積蓋廠鹽鏇鹹鹽網 網鹽艱選蓋獵築遞齋膚 (餘壓積構簾餘鑰窪糧廠 ) | ||||||
临床2期 | 32 | 鏇繭鹹簾膚淵願積衊觸(膚製積艱簾艱齋網獵廠) = 鑰築積壓選糧鬱鏇構鏇 製淵夢衊選鬱膚衊夢繭 (壓製簾顧選構鹽淵廠積 ) 更多 | 不佳 | 2025-10-17 | |||
N/A | 46 | 構選淵鏇選淵鬱夢糧鑰(衊齋淵構簾鹽鬱鏇齋觸) = Among pts with PFS >12 months (26%), ARID1A (p=0.02) and PTEN mutations (p=0.03) were more frequent. 艱獵製遞築範製簾餘繭 (簾顧廠築憲襯顧鑰衊廠 ) 更多 | 积极 | 2025-10-17 | |||
N/A | 25 | 觸膚鑰鹹願窪夢築鑰糧(獵製範艱顧製齋膚齋齋) = 製繭夢觸醖襯壓願鏇衊 糧鏇夢獵餘製鏇膚蓋鬱 (範簾遞獵願襯鬱衊衊構 ) 更多 | 积极 | 2025-10-17 | |||
临床2期 | 29 | 築襯鹹繭鬱構襯簾膚艱(衊觸淵築範簾觸膚遞選) = 網簾鏇廠鏇鬱簾淵鏇網 糧醖壓繭製餘遞鹽鏇襯 (醖網鏇夢窪糧顧願觸衊 ) 更多 | 积极 | 2025-10-17 | |||
(ctDNA clearance or persistently negative) | 築襯鹹繭鬱構襯簾膚艱(衊觸淵築範簾觸膚遞選) = 淵選築鏇壓膚蓋鬱鹽獵 糧醖壓繭製餘遞鹽鏇襯 (醖網鏇夢窪糧顧願觸衊 ) 更多 | ||||||
临床2期 | 24 | 積築襯積鑰窪遞簾鏇窪(憲膚鹹窪鬱觸艱選齋襯) = 築糧製繭糧觸觸餘廠艱 製鹽廠齋鹽遞顧網獵觸 (選廠憲願遞願鹹願鹹簾 ) 更多 | 积极 | 2025-10-17 | |||
临床1期 | 47 | Belzutifan 120 mg PO QD | 願築醖醖鹽窪構鬱網憲(鑰鏇顧築構觸獵襯顧鬱) = 製壓鏇觸繭齋鏇淵膚窪 艱廠淵鏇網廠鹹憲夢餘 (鏇餘壓廠壓艱積簾醖齋, 29 ~ 71) 更多 | 积极 | 2025-10-17 |
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