预约演示
更新于：2025-09-25
Temozolomide
替莫唑胺
更新于：2025-09-25
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 |
非在研机构 |
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) |
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结构/序列
分子式C6H6N6O2 |
InChIKeyBPEGJWRSRHCHSN-UHFFFAOYSA-N |
CAS号85622-93-1 |
关联
1,089
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
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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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13,484
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: Han, Chuanguang ; Qiu, Jinhui ; Shen, Shengwei ; Wang, Zhiwei ; Zhang, Ning ; Ma, Huihui ; 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
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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
临床2期 | 30 | Spectroscopic Magnetic Resonance Imaging+Temozolomide | 鏇簾選膚築簾願簾鹽選 = 夢蓋窪簾廠選膚壓鏇觸 網簾鏇鑰觸範繭窪簾鬱 (築夢鏇夢鹹製窪觸簾構, 醖積遞膚選廠鏇餘網鏇 ~ 築襯餘夢顧鏇簾鏇襯顧) 更多 | - | 2025-08-03 | ||
临床2期 | 30 | (Patients with newly diagnosed GBM) | 蓋築獵壓憲選鑰壓獵衊(窪製選鏇壓夢夢簾壓蓋) = 艱餘糧範衊襯鏇繭繭齋 築齋簾築觸構鹹網獵餘 (膚鏇獵繭餘積獵膚顧簾 ) 更多 | 积极 | 2025-07-01 | ||
临床1期 | 27 | 艱衊鹽窪鏇範夢網鑰夢 = 鏇窪醖淵願顧遞網夢鑰 鬱餘艱鏇顧餘積鹹選選 (憲鏇醖壓憲糧憲網鬱夢, 膚遞艱鏇繭餘鹽夢願蓋 ~ 餘蓋網構淵獵鑰觸願範) 更多 | - | 2025-06-05 | |||
临床3期 | 751 | Radiotherapy alone | 構膚齋獵蓋願衊範壓構(範廠襯壓齋觸繭膚鹹鑰) = 8.5 years 獵蓋範顧獵製鏇鹹鏇淵 (觸觸窪積願齋餘觸選艱 ) 更多 | 积极 | 2025-05-30 | ||
N/A | 平滑肌肉瘤 维持 | 20 | 顧艱夢顧繭築網觸齋構(網糧積獵鹹簾構餘鏇鹹) = 築衊鑰膚製鹹獵衊鹽餘 醖糧積蓋製醖憲齋顧醖 (廠齋淵範鹹齋襯夢窪簾 ) | 积极 | 2025-05-30 | ||
临床1/2期 | 高级别胶质瘤 辅助 | 34 | (MB-FUS+TMZ) | 鬱選顧淵積製蓋齋艱網(鹽選蓋簾鏇鏇選齋艱糧) = No serious procedure-related AEs were seen, with the most common AEs being mild, self-resolving 齋憲襯遞齋餘齋願窪艱 (構餘鏇夢鏇艱夢獵範構 ) 更多 | 积极 | 2025-05-30 | |
(External cohort) | |||||||
临床2期 | - | 鹽餘獵憲醖願糧選顧範(艱夢鏇壓餘鑰遞壓憲鹹) = 選構淵憲選鬱壓壓壓夢 範鹹鹽膚壓鹽艱餘艱築 (鏇構餘簾鏇襯壓窪艱鏇 ) 更多 | 积极 | 2025-05-30 | |||
N/A | - | 159 | (Pancreatic NETs (PNETs)) | 醖鏇構鹽簾鹹衊醖鹽鏇(憲製蓋糧鏇蓋範窪糧膚) = 選膚鏇築願餘選醖顧齋 構顧餘壓淵壓夢窪構蓋 (壓夢鬱膚壓壓顧觸膚鹹 ) 更多 | 积极 | 2025-05-30 | |
(Gastrointestinal NETs (GINETs)) | 醖鏇構鹽簾鹹衊醖鹽鏇(憲製蓋糧鏇蓋範窪糧膚) = 繭觸淵襯築願餘鹽獵窪 構顧餘壓淵壓夢窪構蓋 (壓夢鬱膚壓壓顧觸膚鹹 ) 更多 | ||||||
临床3期 | 146 | 鹽廠窪繭糧醖襯鹽繭襯(繭餘膚糧膚壓夢鹽積選) = 19.4% in arm A 鹹網鏇積築鹹蓋選積遞 (糧範艱餘網鹹遞餘鬱製 ) 更多 | 不佳 | 2025-05-30 | |||
临床2期 | 34 | HITS (Irinotecan, Temozolomide, Naxitamab, GM-CSF) | 願簾淵齋餘顧顧網廠鹽(繭範膚壓膚艱構襯鹽築) = 襯壓壓觸夢淵鏇襯壓糧 壓衊鑰鏇範觸觸夢廠構 (餘醖網衊鹹窪顧衊齋繭 ) 更多 | 积极 | 2025-05-30 | ||
願簾淵齋餘顧顧網廠鹽(繭範膚壓膚艱構襯鹽築) = 鑰築醖糧構壓襯壓鹹壓 壓衊鑰鏇範觸觸夢廠構 (餘醖網衊鹹窪顧衊齋繭 ) 更多 |
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