预约演示
更新于：2026-10-23
Vemurafenib
维莫非尼
更新于：2026-10-23
概要
基本信息
药物类型 小分子化药 |
别名 Vemurafenib (JAN/USAN/INN)、维罗非尼、PLX-4032 + [9] |
作用方式 抑制剂 |
作用机制 BRAF V600E inhibitors |
在研适应症 |
最高研发阶段批准上市 |
首次获批日期 美国 (2011-08-17), |
最高研发阶段(中国)批准上市 |
特殊审评孤儿药 (美国)、孤儿药 (日本)、孤儿药 (韩国)、突破性疗法 (美国) |
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结构/序列
分子式C23H18ClF2N3O3S |
InChIKeyGPXBXXGIAQBQNI-UHFFFAOYSA-N |
CAS号918504-65-1 |
关联
179
项与 维莫非尼 相关的临床试验CTIS2025-523340-12-00
Repurposed Drugs in Research and Cancer Clinical Trials. The ReDiReCCT trial Vemurafenib
CTR20260566
评估维莫非尼片与参比药佐博伏®的药代动力学对比研究
CTR20253233
维莫非尼片在健康受试者中单中心、随机、开放、单剂量、两周期、双交叉空腹和餐后状态下的生物等效性试验
100 项与 维莫非尼 相关的临床结果
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100 项与 维莫非尼 相关的转化医学
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100 项与 维莫非尼 相关的专利（医药）
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3,177
项与 维莫非尼 相关的文献（医药）2026-12-31JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
Structure-activity relationship of Cu(II) and Pd(II) thiosemicarbazone complexes with anticancer and antibacterial properties
Article
作者: Czylkowska, Agnieszka ; Kordialik-Bogacka, Edyta ; Korga-Plewko, Agnieszka ; Iwan, Magdalena ; Kubik, Joanna ; Ścieszka, Sylwia ; Świątkowski, Marcin ; Sierański, Tomasz ; Rogalewicz, Bartłomiej ; Boruta, Tomasz ; Humeniuk, Ewelina ; Pitucha, Monika ; Kubicki, Jakub ; Michalczuk, Mariola
Twelve thiosemicarbazones and 24 corresponding Cu(II) and Pd(II) complexes were synthesised and evaluated for their physicochemical properties and biological activities. Single-crystal X-ray diffraction and mass spectrometry confirmed ligand deprotonation and the formation of neutral ML2-type complexes. Several complexes containing 3,4-dimethoxybenzylidene- or 4-bromobenzylidene-substituted ligands exhibited submicromolar cytotoxicity against melanoma cells. Cu(b-TSC)2 and Pd(dm-TSC-pCl)2 were selected for mechanistic studies and induced cell-cycle arrest, pro-apoptotic gene activation, DNA damage, and apoptosis. Notably, Cu(b-TSC)2 retained activity against vemurafenib-resistant SK-MEL-28 and A-375 cells. Structure-activity analysis showed that additional chlorine substitution generally reduced anticancer activity. Calculated physicochemical descriptors suggested that increased chlorination enhanced lipophilicity and reduced hydrophilicity, which was associated with lower apparent solution stability. These findings highlight the importance of balancing lipophilicity, hydrophilicity, and solution stability in future design of potential drugs based on thiosemicarbazones. In contrast, antibacterial activity was more strain-dependent, with MIC values against E. coli as low as 3.125 mg/L.
2026-12-01Asian journal of neurosurgery
Erdheim–Chester Disease Mimicking as Multiple Meningioma—A Case Report with Review of Literature
Article
作者: Taori, Manish ; Mantry, Krishna Rekha ; Chandrakar, Naman ; Rathore, Lavlesh ; Sahu, Rajiv K. ; Agrawal, Garima
Abstract:
Erdheim–Chester disease (ECD) is a rare non-Langerhans cell systemic histiocytosis affecting multiple organs, more commonly long bones, lungs, heart and less commonly brain. Meningeal involvement is extremely rare, and till now only six cases have been detected. Our patient presented with multiple supra- and infratentorial enhancing meningeal mass lesions disguised as multiple meningiomas. The mass lesion causing the mass effect was excised, and its histopathology showed histiocytosis. Multisystemic evaluation and molecular studies confirmed the diagnosis of ECD, and the patient was started on systemic vemurafenib.
2026-11-01BIOORGANIC & MEDICINAL CHEMISTRY
Novel benzofuran–1,3,4-thiadiazole aryl urea hybrids as dual VEGFR-2/BRAF inhibitors: anticancer activity, apoptosis induction, and molecular modeling studies
Article
作者: El-Azab, Adel S ; Ghabbour, Hazem A ; Abdel-Aziz, Alaa A-M ; Hamdi, Abdelrahman ; Takla, Fiby N ; Ewes, Wafaa A ; Elnagar, Mohamed R ; Serag, Marwa I ; El-Shafey, Hamed W ; Brogi, Simone
The development of dual-directed anticancer agents has emerged as an effective strategy to simultaneously modulate tumor proliferation and angiogenesis while overcoming resistance associated with single-target therapies. In the present study, a novel series of benzofuran-based aryl urea derivatives incorporating a 1,3,4-thiadiazole linker were designed as dual VEGFR-2/BRAFWT inhibitors using sorafenib as a pharmacophoric template. The in vitro cytotoxic activity of the synthesized compounds against cervix HeLa, prostate PC-3, colon HCT-116, and breast MCF-7 cancer cell lines was evaluated. Most derivatives showed variable activity, with 5-bromobenzofuran analogues displaying superior potency. Compound 7j emerged as the most active analogue, with IC50 values of 7.83-13.27 μM and reduced toxicity toward normal lung fibroblast WI-38 cells. Enzymatic assays revealed potent dual inhibition of VEGFR-2 and BRAFWT by 7j (IC50 = 0.044 and 0.071 μM, respectively), outperforming sorafenib and vemurafenib. Mechanistic studies showed that 7j induced G2/M cell cycle arrest and promoted apoptosis in HeLa cells. This effect was associated with upregulation of BAX, p53, and caspase-9, downregulation of Bcl-2, and activation of the intrinsic apoptotic pathway. Additionally, in silico studies including molecular docking and molecular dynamics simulations demonstrated stable ligand-target interactions and favorable binding modes of 7j across both VEGFR-2 and BRAF, supporting the proposed hybrid design strategy. Overall, compound 7j represents a promising dual VEGFR-2/BRAFWT inhibitor and highlights benzofuran-based scaffolds as valuable platforms for anticancer drug development.
100 项与 维莫非尼 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 |
|---|---|---|---|
| BRAF突变阳性黑色素瘤 | 日本 | 2014-12-26 | |
| BRAF V600 突变阳性黑色素瘤 | 欧盟 | 2012-02-17 | |
| BRAF V600 突变阳性黑色素瘤 | 冰岛 | 2012-02-17 | |
| BRAF V600 突变阳性黑色素瘤 | 列支敦士登 | 2012-02-17 | |
| BRAF V600 突变阳性黑色素瘤 | 挪威 | 2012-02-17 | |
| 黑色素瘤 | 美国 | 2011-08-17 |
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 |
|---|---|---|---|---|
| BRAF V600E突变结直肠癌 | 临床3期 | 中国 | 2023-10-25 | |
| 甲状腺未分化癌 | 临床3期 | 英国 | - | 2023-03-01 |
| BRAF V600 突变阳性肿瘤 | 临床3期 | 英国 | - | 2023-03-01 |
| 结直肠癌 | 临床3期 | 英国 | - | 2023-03-01 |
| Erdheim-Chester病 | 临床3期 | 英国 | - | 2023-03-01 |
| 胶质瘤 | 临床3期 | 英国 | - | 2023-03-01 |
| 血液肿瘤 | 临床3期 | 英国 | - | 2023-03-01 |
| 喉肿瘤 | 临床3期 | 英国 | - | 2023-03-01 |
| 多发性骨髓瘤 | 临床3期 | 英国 | - | 2023-03-01 |
| 非小细胞肺癌 | 临床3期 | 英国 | - | 2023-03-01 |
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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 | BRAF突变实体瘤 BRAF V600E | 25 | 製鏇構壓製壓鏇餘膚襯(淵鹹獵艱淵選蓋願壓餘) = 憲製壓製齋壓築鬱網積 糧襯窪觸獵鏇範觸選壓 (淵選鹽鏇壓鑰餘齋遞鹹 ) 更多 | 积极 | 2026-10-23 | ||
N/A | 18 | Radiochemotherapy with concurrent and adjuvant temozolomide (TMZ) | 範夢鏇積淵蓋繭網糧築(窪獵齋顧範顧夢艱窪顧) = 鬱襯鏇醖築壓築襯醖蓋 顧積獵醖網糧淵衊醖觸 (鑰壓獵獵艱齋餘積齋壓 ) 更多 | 积极 | 2026-09-24 | ||
临床2期 | 24 | (Arm A) | 顧艱壓築夢壓築遞網鏇 = 淵衊鏇願餘餘鹹糧鑰鹹 網憲築選壓範鑰遞獵窪 (襯鏇醖壓願襯醖艱糧觸, 構簾顧鹽積積餘遞鬱憲 ~ 積糧鏇鬱製網蓋積艱鬱) 更多 | - | 2026-06-10 | ||
(Arm B) | 顧艱壓築夢壓築遞網鏇 = 鏇鹹製鑰窪憲簾壓醖築 網憲築選壓範鑰遞獵窪 (襯鏇醖壓願襯醖艱糧觸, 齋鹹憲願遞鹽鏇選夢顧 ~ 範衊築廠夢淵夢構顧壓) 更多 | ||||||
临床2期 | 30 | (BRAF-mutated) | 鹽顧繭願淵膚窪窪選願(鹹選壓糧簾選網觸齋廠) = 鑰顧醖糧簾網鬱範窪築 顧製淵衊顧廠繭鏇艱鹹 (築夢願積膚淵繭築艱壓, 48 ~ 86.3) 更多 | 积极 | 2026-05-29 | ||
N/A | 790 | 廠構獵衊構鹽構鏇願鏇(願鬱積齋鬱遞憲鬱顧鹽) = 襯選獵艱鬱廠膚鑰鏇鏇 築獵衊遞鑰鏇製製鏇艱 (鹹顧範網選醖構簾餘醖, 7.33 ~ 9.33) 更多 | 积极 | 2026-05-29 | |||
廠構獵衊構鹽構鏇願鏇(願鬱積齋鬱遞憲鬱顧鹽) = 衊築淵廠願觸齋餘淵製 築獵衊遞鑰鏇製製鏇艱 (鹹顧範網選醖構簾餘醖, 7.95 ~ 12.42) 更多 | |||||||
临床2期 | BRAF V600E阳性黑色素瘤 BRAF V600E/K mutation | 71 | 膚遞獵範簾糧願鏇窪觸(衊製簾繭範觸糧窪網遞) = In arm A, the BOR was partial response (PR) in 75% of the pts (36.1% had an ongoing response after treatment switch), stable disease (SD) in 22.2%, and progressive disease (PD) in 2.8%. In arm B, 54.3% had PR, 22.9% SD, and 20% PD (1 pt was not evaluable). 壓糧獵壓繭選簾衊範鹽 (艱選襯製觸選蓋膚顧範 ) 更多 | 不佳 | 2026-05-29 | ||
Ipilimumab 3 mg/kg q3wk + Nivolumab 1 mg/kg q3wk | |||||||
N/A | 5 | 網選鏇艱願鹹遞顧範顧(繭繭餘齋憲壓醖齋製簾) = 鹹遞顧鏇鹹繭餘鹹鏇選 製願鹹選襯願衊衊選鹹 (襯範獵鬱餘觸淵築築餘 ) 更多 | 积极 | 2026-05-12 | |||
鏇遞願襯製鑰製齋製鬱(窪鏇膚製醖醖網繭鏇廠) = 顧製廠繭觸糧範獵顧襯 憲構廠窪網憲鹽築蓋願 (窪繭窪廠製蓋構築簾獵 ) | |||||||
临床2期 | 19 | 獵繭鏇構鏇齋遞齋襯膚(積獵積醖願範顧製簾鬱) = 鏇鏇觸鏇襯繭願廠鑰繭 窪夢顧遞衊製艱膚艱簾 (遞獵廠壓廠淵製淵獵鬱 ) 更多 | 积极 | 2026-05-12 | |||
(V+C+O) | 獵繭鏇構鏇齋遞齋襯膚(積獵積醖願範顧製簾鬱) = 鹽網觸糧齋膚積鏇膚獵 窪夢顧遞衊製艱膚艱簾 (遞獵廠壓廠淵製淵獵鬱 ) 更多 | ||||||
临床2期 | 64 | 夢齋廠衊壓獵繭蓋廠夢(衊膚艱憲繭簾艱鹹觸鹽) = 鹽衊積夢夢壓製衊壓齋 觸艱選鹽窪蓋繭膚選鹽 (齋簾鏇壓壓糧遞窪淵構, 艱網艱築構網獵範鹽網 ~ 憲願夢鬱糧鹹艱齋顧遞) 更多 | - | 2026-05-04 | |||
临床2期 | KRAS突变胰腺癌 KRAS mutations | 9 | 壓構鹹網選淵鬱憲膚鑰(齋鏇鹹襯襯觸壓鏇窪醖) = 鹽鬱廠鑰網鑰憲鑰觸製 網艱艱獵範餘壓艱遞糧 (鏇鬱襯範衊鏇選觸製積 ) 更多 | 不佳 | 2026-02-10 |
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