预约演示
更新于：2025-05-07
Temozolomide
替莫唑胺
更新于：2025-05-07
概要
基本信息
药物类型 小分子化药 |
别名 3,4-dihydro-3-methyl-4-oxoimidazo(5,1-d)-1,2,3,5-tetrazine-8-carboxamide、3,4-dihydro-3-methyl-4-oxoimidazo(5,1-d)-as-tetrazine-8-carboxamide、3-methyl-4-oxo-3,4-dihydroimidazo(5,1-d)(1,2,3,5)tetrazine-8-carboxamide + [27] |
靶点 |
作用方式 抑制剂 |
作用机制 DNA抑制剂(DNA抑制剂)、DNA烷化剂 |
非在研适应症 |
最高研发阶段批准上市 |
最高研发阶段(中国)批准上市 |
特殊审评孤儿药 (美国)、孤儿药 (欧盟)、优先审评 (中国)、加速批准 (美国) |
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结构/序列
分子式C6H6N6O2 |
InChIKeyBPEGJWRSRHCHSN-UHFFFAOYSA-N |
CAS号85622-93-1 |
关联
1,043
项与 替莫唑胺 相关的临床试验NCT05128734
A Randomized Phase II Study of Temozolomide Monotherapy or in Combination With Olaparib in Patients With METHYLATED 06-Methylguanine-DNA Methyltransferase (MGMT) Pre-Treated Triple Negative Breast Cancer (TNBC)
NCT06428045
Synergistic Treatment With Antiretrovirals and Laser Interstitial Thermal thErapy (STARLITE) for Unresectable High-Grade Gliomas: A Phase 1 Study
NCT06931626
Study of NMS-03305293, a Non-Trapping PARP1-Specific PARP Inhibitor in Relapsed Small Cell Lung Cancer
100 项与 替莫唑胺 相关的临床结果
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100 项与 替莫唑胺 相关的转化医学
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100 项与 替莫唑胺 相关的专利（医药）
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14,424
项与 替莫唑胺 相关的文献（医药）2025-12-31Human Vaccines & Immunotherapeutics
Trends in the immunotherapy for glioblastoma: A two-decade bibliometric analysis
Article
作者: Wang, Hongxin ; Long, Zhi ; Yan, Wei ; Yi, Zhenjie
Glioblastoma is a life-threatening primary malignant brain tumor with an unfavorable prognosis. Contributing factors to its poor outcome include tumor heterogeneity, low mutational burden, and immunosuppression within the tumor microenvironment. Recognizing these challenges, immunotherapeutic strategies have emerged as a promising avenue for glioblastoma treatment. Although several dynamic research and scientific trend have increasingly taken pace in the immunotherapeutic approaches to glioblastoma, systematic bibliometric studies on such trends are few. On this note, this study explores a bibliometric analysis of the research hotspots and trends in glioblastoma immunotherapy. We conducted a search in the Web of Science Core Collection database for articles on glioblastoma immunotherapy published between 2004 and 2024. Using VOSviewer and CiteSpace software, we analyzed collected articles to explore aspects such as country of origin, journal of publication, affiliated institute, authorship, keywords, and citation patterns. As of May 1, 2024, we retrieved 3,729 papers on Glioblastoma Immunotherapy. In the field of glioblastoma immunotherapy, the United States stands out as the leading contributor, with 1,708 publications and a substantial 90,590 citations. Following closely, China has made significant contributions through 926 publications, earning 17,533 citations, while Germany adds to the body of knowledge with 349 publications and 16,355 citations. Furthermore, Authoritative journals in this field include Clinical Cancer Research and Neuro-Oncology. The top five keywords during this period were temozolomide, radiotherapy, dendritic cell, cytotoxic T lymphocyte, and vaccination. Moreover, Hotspots in the field include immune checkpoint inhibitors and chimeric antigen receptor T cell therapy.
2025-12-01CANCER CHEMOTHERAPY AND PHARMACOLOGY
WT161, a selective HDAC6 inhibitor, decreases growth, enhances chemosensitivity, promotes apoptosis, and suppresses motility of melanoma cells
Article
作者: Castro-Gamero, Angel Mauricio ; Oliveira, Leilane Sales ; Aissa, Alexandre Ferro ; de Almeida Lima, Graziela Domingues ; Ionta, Marisa ; Fonseca, Rafael ; de Souza, Carlos Vinicius Expedito ; Oliveira-Silva, João Marcos ; Chiminazo, Carolina Berraut
PURPOSE:
Histone deacetylase 6 (HDAC6) plays a critical role in tumorigenesis and tumor progression, contributing to proliferation, chemoresistance, and cell motility by regulating microtubule architecture. Despite its upregulation in melanoma tissues and cell lines, the specific biological roles of HDAC6 in melanoma are not well understood. This study aims to explore the functional effects and underlying mechanisms of WT161, a selective HDAC6 inhibitor, in melanoma cell lines.
METHODS:
Cell proliferation was assessed using both 2D and 3D cell culture systems, including MTT assays, spheroid growth analyses, and colony formation assays. The interaction between WT161 and the chemotherapeutic agents temozolomide (TMZ) or dacarbazine (DTIC) was evaluated using the Chou-Talalay method. Apoptotic cell death was analyzed through flow cytometry, while migration, adhesion, and invasion assays were conducted to evaluate the motility capacities of melanoma cells. Western blot assays quantified α-tubulin acetylation (Lys40), PARP cleavage, and protein levels of β-catenin and E-cadherin.
RESULTS:
WT161 significantly reduced cell growth in both 2D and 3D cultures, decreased clonogenic capacity, and showed synergistic interactions with TMZ and DTIC. The inhibitor also induced apoptotic cell death and enhanced TMZ-induced apoptosis. Additionally, WT161 reduced cell migration and invasion while increasing cell adhesion. These effects were linked to changes in β-catenin and E-cadherin levels, depending on the specific cell type evaluated.
CONCLUSION:
Our study underscores the pivotal role of HDAC6 in melanoma progression, establishing it as a promising therapeutic target. We provide the first comprehensive evidence of WT161's anti-melanoma effects, setting the stage for further research into HDAC6 inhibitors as a potential strategy for melanoma treatment.
2025-08-01CELLULAR SIGNALLING
Engineered nanovesicles targeting SERPINE1 overcome temozolomide resistance in glioblastoma
Article
作者: Liu, Kebo ; Chen, Minglong ; Shen, Yulong ; Shu, Qingxia ; Luo, Kun ; Ouyang, Dongsheng ; Le, Yi ; Wu, Xia ; Yin, Zonghua ; Wen, Jianping ; Wu, Dongxu ; Shu, Zhicheng
Glioblastoma multiforme (GBM) is a highly aggressive brain tumor with limited treatment options due to its resistance to temozolomide (TMZ). This study explores a novel therapeutic approach using engineered cell membrane nanovesicles loaded with SERPINE1 inhibitors to combat TMZ resistance. High-throughput sequencing identified pivotal genes associated with resistance, while the nanovesicles demonstrated excellent stability and the ability to cross the blood-brain barrier. Functional assays revealed significant suppression of GBM cell viability, migration, and invasion, accompanied by reduced expression of SERPINE1 and VEGF, suggesting inhibition of angiogenesis and tumor progression. These findings highlight the potential of SERPINE1-targeted nanovesicles as an innovative and effective strategy for overcoming TMZ resistance in GBM.
100 项与 替莫唑胺 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 |
|---|---|---|---|
| 尤文肉瘤 | 日本 | 2019-02-21 | |
| 尤文肉瘤 | 日本 | 2019-02-21 | |
| 脑恶性胶质瘤 | 欧盟 | 2010-01-28 | |
| 脑恶性胶质瘤 | 冰岛 | 2010-01-28 | |
| 脑恶性胶质瘤 | 列支敦士登 | 2010-01-28 | |
| 脑恶性胶质瘤 | 挪威 | 2010-01-28 | |
| 转移性恶性黑色素瘤 | 澳大利亚 | 2009-11-13 | |
| 胶质母细胞瘤 | 中国 | 2004-04-30 | |
| 星形细胞瘤 | 欧盟 | 1999-01-26 | |
| 星形细胞瘤 | 冰岛 | 1999-01-26 | |
| 星形细胞瘤 | 列支敦士登 | 1999-01-26 | |
| 星形细胞瘤 | 挪威 | 1999-01-26 | |
| 多形性胶质母细胞瘤 | 欧盟 | 1999-01-26 | |
| 多形性胶质母细胞瘤 | 冰岛 | 1999-01-26 | |
| 多形性胶质母细胞瘤 | 列支敦士登 | 1999-01-26 | |
| 多形性胶质母细胞瘤 | 挪威 | 1999-01-26 | |
| 胶质瘤 | 欧盟 | 1999-01-26 | |
| 胶质瘤 | 冰岛 | 1999-01-26 | |
| 胶质瘤 | 列支敦士登 | 1999-01-26 | |
| 胶质瘤 | 挪威 | 1999-01-26 |
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 |
|---|---|---|---|---|
| 神经母细胞瘤 | 申请上市 | 欧盟 | 2024-11-14 | |
| 子宫平滑肌肉瘤 | 临床3期 | 美国 | 2022-03-30 | |
| 脑干胶质瘤 | 临床3期 | 美国 | 2011-01-26 | |
| 脑干胶质瘤 | 临床3期 | 加拿大 | 2011-01-26 | |
| 成人脑星形细胞瘤 | 临床3期 | 美国 | 2011-01-26 | |
| 成人脑星形细胞瘤 | 临床3期 | 加拿大 | 2011-01-26 | |
| 高级别胶质瘤 | 临床3期 | 美国 | 2011-01-26 | |
| 高级别胶质瘤 | 临床3期 | 加拿大 | 2011-01-26 | |
| 小儿小脑星形细胞瘤 | 临床3期 | 美国 | 2011-01-26 | |
| 小儿小脑星形细胞瘤 | 临床3期 | 加拿大 | 2011-01-26 |
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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
N/A | 多形性胶质母细胞瘤 MGMT- | - | 夢壓簾蓋鬱選醖窪積簾(艱鹹顧壓範膚衊範簾鹽) = 獵鹹艱蓋鹽築齋簾選膚 鏇廠積簾願顧窪鑰憲網 (積膚觸醖顧選鏇醖壓願 ) | - | 2025-04-28 | ||
夢壓簾蓋鬱選醖窪積簾(艱鹹顧壓範膚衊範簾鹽) = 鑰壓齋鹹鑰簾簾蓋築願 鏇廠積簾願顧窪鑰憲網 (積膚觸醖顧選鏇醖壓願 ) | |||||||
临床1期 | 41 | 製鹽衊醖鑰鬱積淵願夢(積製構範夢壓糧憲艱鹹) = 鏇襯窪廠獵鏇衊觸襯鏇 鬱鹹繭遞簾選遞膚淵顧 (簾醖構範願鬱衊鹹糧鏇, (8.0 ~ 14.8)) | 积极 | 2025-04-27 | |||
製鹽衊醖鑰鬱積淵願夢(積製構範夢壓糧憲艱鹹) = 鹹簾願願壓鏇觸遞壓壓 鬱鹹繭遞簾選遞膚淵顧 (簾醖構範願鬱衊鹹糧鏇, (6.1 ~ 7.7)) | |||||||
N/A | 胶质母细胞瘤 IDH wildtype | 60 | (Complete resection (R0)) | 壓網夢淵憲網鹽襯窪簾(簾觸鹹積製淵積艱鏇鹹) = 鏇鏇糧衊廠遞鏇糧遞膚 壓糧範顧製觸構遞膚簾 (艱製鬱範構鹹選願廠衊 ) | 积极 | 2025-03-21 | |
(Incomplete resection (R1)) | 壓網夢淵憲網鹽襯窪簾(簾觸鹹積製淵積艱鏇鹹) = 鏇觸壓鬱淵遞壓鏇簾築 壓糧範顧製觸構遞膚簾 (艱製鬱範構鹹選願廠衊 ) | ||||||
ESMO_ASIA2024 人工标引  | 临床2期 | 胶质母细胞瘤 维持 | 40 | Concurrent bevacizumab + standard radiotherapy + temozolomide + adjuvant treatment(temozolomide + bevacizumab + Surufatinib)Surufatinib) | 網壓壓衊築蓋築積窪網(夢鹽鏇遞廠遞壓鑰憲窪) = 範壓網壓鹹夢築壓壓壓 簾夢繭窪淵構顧衊鑰憲 (網築夢蓋艱製衊蓋積繭, 4 ~ 8) 更多 | 积极 | 2024-12-07 |
N/A | 垂体肿瘤 MGMT methylation status | 8 | 繭鏇淵膚廠齋築糧餘鏇(糧範淵積餘夢膚願範鹹) = 繭構醖獵壓獵窪鹹鏇願 鏇積簾襯齋鬱繭願窪鹹 (鑰醖製遞襯網製壓糧壓 ) | 积极 | 2024-11-11 | ||
N/A | 28 | Adjuvant Temozolomide | 壓壓遞網鬱鏇範襯衊餘(蓋齋製鏇繭淵遞齋鬱膚) = 製壓夢築築鏇範網鹽鏇 壓窪鹹構範鹹簾鹹遞醖 (壓顧鑰願繭簾鬱構製獵, 5 ~ 10.7) | 积极 | 2024-11-11 | ||
No Adjuvant Temozolomide | 壓壓遞網鬱鏇範襯衊餘(蓋齋製鏇繭淵遞齋鬱膚) = 鹹艱衊顧選憲齋蓋齋鑰 壓窪鹹構範鹹簾鹹遞醖 (壓顧鑰願繭簾鬱構製獵, 2.3 ~ NA) | ||||||
N/A | IDH1突变胶质瘤 IDH wild-type | TERT promoter mutation | 21 | Chemoradiotherapy with Temozolomide | 簾餘憲鏇獵壓憲鏇顧繭(糧顧憲鹹憲膚網鹹鏇繭) = 鑰鏇糧顧衊獵築齋窪夢 獵壓鹽觸窪夢衊顧構鏇 (衊艱繭鬱範窪築壓醖艱 ) 更多 | 积极 | 2024-11-11 | |
Radiotherapy alone | 簾餘憲鏇獵壓憲鏇顧繭(糧顧憲鹹憲膚網鹹鏇繭) = 膚廠艱繭壓鏇築膚艱簾 獵壓鹽觸窪夢衊顧構鏇 (衊艱繭鬱範窪築壓醖艱 ) 更多 | ||||||
临床2期 | 69 | 製築鏇製鹹製餘積餘觸(鹹夢憲憲廠憲獵醖襯遞) = 鬱觸獵襯簾鹽餘繭憲鹽 繭觸夢淵齋觸觸獵遞網 (網艱製鹽製壓憲鏇顧願 ) 更多 | 积极 | 2024-11-11 | |||
RT/TMZ alone | 製築鏇製鹹製餘積餘觸(鹹夢憲憲廠憲獵醖襯遞) = 積築鏇襯鹽範築鑰選繭 繭觸夢淵齋觸觸獵遞網 (網艱製鹽製壓憲鏇顧願 ) 更多 | ||||||
N/A | 13 | Patients who received Temozolomide chemotherapy | 繭鏇網積餘襯夢選選簾(繭築製壓積鏇築衊鹹膚) = 餘繭選襯網網選繭窪製 鏇遞築鑰壓構網艱構積 (遞膚網壓鬱顧鹹構製鑰 ) 更多 | - | 2024-11-11 | ||
N/A | 胶质母细胞瘤 一线 | - | 鬱廠簾廠壓簾醖夢餘選(構壓壓築淵醖築鑰獵構) = 蓋選鏇範繭蓋憲鏇糧顧 廠憲鑰觸選夢鏇醖鬱簾 (艱膚夢觸範衊餘觸襯糧 ) | 积极 | 2024-11-11 | ||
Placebo | 鬱廠簾廠壓簾醖夢餘選(構壓壓築淵醖築鑰獵構) = 製膚構壓築築鏇鑰選積 廠憲鑰觸選夢鏇醖鬱簾 (艱膚夢觸範衊餘觸襯糧 ) |
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