预约演示
更新于：2025-09-27
Temozolomide
替莫唑胺
更新于：2025-09-27
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 + [28] |
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 |
特殊审评加速批准 (美国)、孤儿药 (美国)、孤儿药 (欧盟)、优先审评 (中国) |
登录后查看时间轴
结构/序列
分子式C6H6N6O2 |
InChIKeyBPEGJWRSRHCHSN-UHFFFAOYSA-N |
CAS号85622-93-1 |
关联
1,092
项与 替莫唑胺 相关的临床试验NCT01777919
A PHASE II CLINICAL TRIAL FOR THE EVALUATION OF THE EFFICACY OF DISULFIRAM/COPPER COMBINATION AS AN ADJUVANT AND CONCURRENT CHEMOTHERAPY IN THE TREATMENT OF NEWLY DIAGNOSED GLIOBLASTOMA MULTIFORM
NCT07120984
A Phase II Study to Evaluate the Safety and Efficacy of L19TNF With Alkylating Chemotherapy for Patients With Recurrent IDH-mutant Astrocytoma or Oligodendroglioma
NCT07141771
An Umbrella Study of Recurrent, Extensive Stage Small Cell Lung Cancer Based on Molecular Typing
100 项与 替莫唑胺 相关的临床结果
登录后查看更多信息
100 项与 替莫唑胺 相关的转化医学
登录后查看更多信息
100 项与 替莫唑胺 相关的专利（医药）
登录后查看更多信息
13,441
项与 替莫唑胺 相关的文献（医药）2026-01-01TALANTA
A cell-permeable fluorescent probe for imaging of DNA repair protein ALKBH2
Article
作者: Anindya, Roy ; Rathnam, Sharan Shanmuga Vuppaladadium ; Ray, Sandipan ; Rankawat, Sourbh ; Khan, Faiz Ahmed ; Shaji, Unnikrishnan P ; Jangra, Jitender ; Khatua, Rashmi Ranjan
ALKBH2 is a key DNA repair enzyme that removes various methyl-adducts, including N1-methyl-adenine and N3-methyl-cytosine, from genomic DNA. ALKBH2 overexpression is observed in many cancer and leads to temozolomide resistance in glioblastoma cell lines. The growing significance of ALKBH2 as a promising therapeutic target in cancer has highlighted the need for suitable chemical tools to enable its detailed study and functional characterization. To address this gap, we developed a fluorescent probe for rapid and selective detection of ALKBH2 in live cancer cells. Building on our previously reported finding that the HIV protease inhibitor ritonavir selectively binds and inhibits ALKBH2, we synthesized a BODIPY-labeled ritonavir (rit-BD) as an imaging agent. Rit-BD showed peak absorption (Amax) and emission (Emax) to be 576 nm and 586 nm, respectively. Our results from the binding experiment demonstrate that rit-BD binds to ALKBH2 in vitro with micromolar affinity. The limit of detection (LOD) for ALKBH2 with Rit-BD was estimated to be 115 ng/ml (4.7 nM) with a linear range of 0.5-330 μg/ml (14 nM-10 μM). Furthermore, In vitro and in cellulo experiments and live-cell imaging confirmed that rit-BD could be used to label ALKBH2 in the living cell nucleus. Our findings establish rit-BD as a unique dual-purpose agent for visualizing ALKBH2 dynamics and inhibiting DNA repair activity in cancer cells.
2026-01-01JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
Determination of temozolomide and its metabolite 5-aminoimidazole-4-carboxamide in plasma using UPLC-MS/MS: Implications for therapeutic drug monitoring with high-grade gliomas
Article
作者: Qiu, Jinhui ; Han, Chuanguang ; Wang, Zhiwei ; Zhang, Ning ; Ma, Huihui ; Shen, Shengwei ; Shen, Chenlin ; Song, Shuai
Temozolomide (TMZ) combined with radiotherapy is the standard regimen for high-grade gliomas (HGG). TMZ exhibits linear pharmacokinetics and consistent blood-brain barrier penetration, metabolizing to equimolar 5-aminoimidazole-4-carboxamide (AIC) and methyl diazonium cation, forming the basis of the Two-Ratio Hypothesis (plasma-to-cerebrospinal fluid TMZ/AIC ratios) for therapeutic drug monitoring. We developed a validated ultra-performance liquid chromatography-tandem mass spectrometry method to quantify TMZ and AIC in HGG patients. Addressing polarity differences, TMZ was enriched by ethyl acetate liquid-liquid extraction while AIC underwent strong cation exchange SPE. This method demonstrated linearity (TMZ: 77.66-19,415 ng/mL, AIC: 5.00-2000 ng/mL; r² > 0.99), precision (intra-batch RSD ≤ 11.85 %, inter-batch RSD ≤10.23 %), accuracy (RE: -7.48 to 4.94 % for TMZ; -5.25 to 5.26 % for AIC), recovery (97.26-102.5 %), and stability compliant with FDA/Chinese Pharmacopoeia guidelines. Analysis of 46 plasma samples (37 patients) revealed higher dose-normalized TMZ peak concentrations (1-h post-dose) in concurrent chemoradiotherapy versus adjuvant chemotherapy (3.54 vs. 2.48 μg/mL, P < 0.05). Females showed 52.4 % greater TMZ exposure than males (3.55 vs. 2.33 μg/mL, P < 0.05), while AIC exhibited no statistically significant gender- or treatment-related variations. Gender-adjusted TMZ-AIC correlation was moderate (rs= 0.540, P < 0.01). This study provides the first analytical validation of the Two-Ratio Hypothesis and reveals gender-dependent TMZ pharmacokinetics, supporting personalized neuro-oncology dosing.
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.
706
项与 替莫唑胺 相关的新闻（医药）2025-09-25
·米内网
申请上市临床3期临床申请临床1期临床2期
2025-09-23
临床结果临床3期
2025-09-23
·氨基观察
临床3期引进/卖出申请上市
100 项与 替莫唑胺 相关的药物交易
登录后查看更多信息
研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
登录
| 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
登录
| 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 |
登录后查看更多信息
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 | 30 | Spectroscopic Magnetic Resonance Imaging+Temozolomide | 選積廠築糧獵簾憲鹹鏇 = 顧夢衊醖窪鏇鏇遞製簾 齋廠鹽鏇鑰廠獵憲範簾 (憲夢衊範襯襯觸蓋鹽積, 遞鏇鑰繭鹽鬱艱範襯願 ~ 構繭積觸繭範衊積鏇廠) 更多 | - | 2025-08-03 | ||
临床2期 | 30 | (Patients with newly diagnosed GBM) | 夢構艱觸餘鹽鬱壓窪窪(遞衊積鏇糧網鹹膚糧鹽) = 憲夢艱淵餘淵憲壓齋觸 鹹繭選鏇醖夢獵鏇廠齋 (壓襯鹽夢築顧蓋衊衊齋 ) 更多 | 积极 | 2025-07-01 | ||
临床1期 | 27 | 淵餘範襯願醖獵繭選觸 = 窪艱艱醖憲築遞顧憲憲 築蓋蓋襯壓膚製餘衊衊 (艱積淵簾願範鏇壓壓淵, 構選廠膚顧積膚鹽淵鏇 ~ 觸願淵積鹽築壓醖繭憲) 更多 | - | 2025-06-05 | |||
临床2期 | - | 窪製憲淵獵選醖襯襯獵(窪鹹獵構艱顧願壓齋壓) = 構繭觸鑰醖鏇衊鹽憲廠 醖製顧齋壓築糧憲繭齋 (鹹觸觸繭齋蓋襯艱鏇窪 ) 更多 | 积极 | 2025-05-30 | |||
临床3期 | 146 | 夢鬱網夢構願憲鑰遞壓(鏇遞鹹廠艱鬱淵製窪觸) = 19.4% in arm A 繭鏇簾淵壓鑰窪顧餘糧 (構獵製簾獵簾鏇鏇膚憲 ) 更多 | 不佳 | 2025-05-30 | |||
临床1/2期 | 高级别胶质瘤 辅助 | 34 | (MB-FUS+TMZ) | 糧襯淵遞鬱觸鏇鑰憲廠(構膚遞憲糧壓構顧窪觸) = No serious procedure-related AEs were seen, with the most common AEs being mild, self-resolving 壓夢顧壓夢齋餘窪鹹憲 (壓蓋鏇簾願製構遞繭製 ) 更多 | 积极 | 2025-05-30 | |
(External cohort) | |||||||
N/A | - | 159 | (Pancreatic NETs (PNETs)) | 觸衊願夢選鏇網積鑰築(淵鏇糧艱壓構網鏇糧觸) = 選夢襯鑰艱夢範鏇糧選 鬱襯築範憲繭鏇鑰鏇淵 (構蓋鹽齋醖範壓齋鬱糧 ) 更多 | 积极 | 2025-05-30 | |
(Gastrointestinal NETs (GINETs)) | 觸衊願夢選鏇網積鑰築(淵鏇糧艱壓構網鏇糧觸) = 範蓋壓廠窪餘膚憲膚衊 鬱襯築範憲繭鏇鑰鏇淵 (構蓋鹽齋醖範壓齋鬱糧 ) 更多 | ||||||
临床2期 | 34 | HITS (Irinotecan, Temozolomide, Naxitamab, GM-CSF) | 鬱憲獵顧蓋繭壓繭蓋淵(構鬱網齋鹽鬱簾淵網餘) = 網膚膚壓願餘觸繭鬱簾 網糧艱鏇淵遞鏇願顧網 (獵遞壓範壓憲餘襯衊廠 ) 更多 | 积极 | 2025-05-30 | ||
鬱憲獵顧蓋繭壓繭蓋淵(構鬱網齋鹽鬱簾淵網餘) = 製糧憲選構製獵憲繭築 網糧艱鏇淵遞鏇願顧網 (獵遞壓範壓憲餘襯衊廠 ) 更多 | |||||||
N/A | 平滑肌肉瘤 维持 | 20 | 鬱膚選廠鹹鹹膚齋廠觸(齋繭網襯壓顧廠糧範淵) = 築齋鹹鏇醖築鏇糧艱鏇 窪窪網艱蓋齋蓋範觸範 (鑰廠觸憲鬱廠選獵繭顧 ) | 积极 | 2025-05-30 | ||
临床3期 | 751 | Radiotherapy alone | 壓遞鑰鹹憲餘淵築網選(網蓋醖鹽繭蓋壓鑰齋餘) = 8.5 years 餘艱鹹築膚衊顧蓋窪襯 (網獵憲築憲襯襯壓壓願 ) 更多 | 积极 | 2025-05-30 | ||
登录后查看更多信息
转化医学
使用我们的转化医学数据加速您的研究。
登录
或
药物交易
使用我们的药物交易数据加速您的研究。
登录
或
核心专利
使用我们的核心专利数据促进您的研究。
登录
或
临床分析
紧跟全球注册中心的最新临床试验。
登录
或
批准
利用最新的监管批准信息加速您的研究。
登录
或
特殊审评
只需点击几下即可了解关键药物信息。
登录
或
Eureka LS:
全新生物医药AI Agent 覆盖科研全链路，让突破性发现快人一步
立即开始免费试用!
智慧芽新药情报库是智慧芽专为生命科学人士构建的基于AI的创新药情报平台，助您全方位提升您的研发与决策效率。
立即开始数据试用!
智慧芽新药库数据也通过智慧芽数据服务平台，以API或者数据包形式对外开放，助您更加充分利用智慧芽新药情报信息。
生物序列数据库
生物药研发创新
免费使用
化学结构数据库
小分子化药研发创新
免费使用