预约演示
更新于：2025-01-17
Telmisartan
替米沙坦
更新于：2025-01-17
概要
基本信息
药物类型 小分子化药 |
别名 4'-[(1,4'-dimethyl-2'propyl[2,6'-bi-1H-benzimidazol]-1'-yl)methyl]-[1,1'-biphenyl]-2-carboxylic acid、4'-[(1,7'-dimethyl-2'-propyl-1H,3'H-2,5'-bibenzimidazol-3'-yl)methyl]biphenyl-2-carboxylic acid、Telmisartan + [68] |
靶点 |
作用机制 AT1R拮抗剂(血管紧张素II-1型受体拮抗剂) |
治疗领域 |
非在研机构- |
最高研发阶段批准上市 |
首次获批日期 美国 (1998-11-10), |
最高研发阶段(中国)批准上市 |
特殊审评优先审评 (中国) |
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结构/序列
分子式C33H30N4O2 |
InChIKeyRMMXLENWKUUMAY-UHFFFAOYSA-N |
CAS号144701-48-4 |
关联
321
项与 替米沙坦 相关的临床试验TCTR20241006001
A Randomized, Double-blind, Multi-center, Active-controlled, Phase 3 clinical trial to Evaluate the Efficacy and Safety of Combination Therapy of THP-00101, THP-00102, and THP-00103 in Subjects with T2DM and Essential Hypertension
NCT06647745
A Randomized, Double-blind, Multi-center, Active-controlled, Phase 3 Clinical Trial to Evaluate the Efficacy and Safety of Combination Therapy of THP-00101, THP-00102, and THP-00103 in Subjects With T2DM and Essential Hypertension
CTRI/2024/07/069868
Open label randomised controlled trial of Telmisartan in Raynauds phenomenon associated with Systemic Lupus Erythematosus and Rheumatoid Arthritis - NIL
100 项与 替米沙坦 相关的临床结果
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100 项与 替米沙坦 相关的转化医学
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100 项与 替米沙坦 相关的专利（医药）
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2,816
项与 替米沙坦 相关的文献（医药）2025-03-01INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
FDA-approved drugs as PIM-1 kinase inhibitors: A drug repurposed approach for cancer therapy
Article
作者: Haque, Mohammad Mahfuzul ; Ahmed, Shahbaz ; Taiyab, Aaliya ; Noor, Saba ; Hassan, Md Imtaiyaz ; AlAjmi, Mohamed F ; Rathi, Aanchal ; Sulaimani, Md Nayab ; Khan, Faez Iqbal
PIM-1 kinase, a member of the Serine/Threonine kinase family, has emerged as a promising therapeutic target in various cancers due to its role in promoting tumor growth and resistance to conventional therapies. In this study, we employed a structure-based approach to screen 3800 FDA-approved drugs to discover potential inhibitors of PIM-1. After an initial selection of 50 candidates based on high docking scores, four drugs, stanozolol, alfaxalone, rifaximin, and telmisartan, were identified as strong PIM-1 binders, interacting with key residues in the ATP-binding pocket of the kinase. To assess the stability of these interactions, we conducted all-atom molecular dynamic simulations, confirming favorable dynamics. Experimental validation via a kinase inhibition assay on recombinant PIM-1 showed that rifaximin significantly inhibited PIM-1 activity, with an IC50 of ∼26 μM. Fluorescence binding assays further demonstrated a strong binding affinity for rifaximin, with a binding constant, corroborated by isothermal titration calorimetry studies. Our findings suggest that rifaximin may serve as a potential repurposed drug for targeting PIM-1 in cancer treatment. However, further validations are required in a clinical setting before the final therapeutic implications.
2025-02-01ANALYTICAL BIOCHEMISTRY
Specialized greenness sustainability tools for evaluation of the spectrophotometric methodologies greenness: Spectral signal manipulation for resolving the interfering telmisartan and metoprolol succinate spectra in their bulk and pharmaceutical formulation
Article
作者: Abd El-Hay, Soad S. ; Abd El-Hay, Soad S ; Fawzy, Michael Gamal ; Mostafa, Alaa Ahmed ; Metias, Youstina Mekhail
Hypertension is a leading cause of cardiovascular mortality, often accompanied by complications such as arrhythmia and stroke. This silent killer requires a multifaceted pharmacological approach for effective management. This article presents new, environmentally friendly spectrophotometric methods for simultaneous quantification of telmisartan (TER) and metoprolol succinate (MTR) in laboratory prepared mixtures and pharmaceutical formulations. The suggested methodologies include the following: area under the curve method (AUC) utilizing area at specific wavelength ranges 228-233 nm (λ1 - λ2) and 240-245 nm (λ3 - λ4) for each analyte and Fourier self-deconvolution method (FD) depending on built-in function to address spectral interferences. In addition, the induced dual wavelength method (IDWL) employing equality factors to obtain absorbance differences at designated wavelengths, ratio difference method (RD) utilizing divisor-based ratio spectra where the utilized divisors were TER 40 μg/mL and MTR 90 μg/mL, and ratio derivative method (RDV) generating spectra through first derivative application that was measured at 266 nm and 246 nm for TER and MTR, respectively. These methods offer green alternatives for the accurate and precise determination of TER and MTR with exceptional linearity of 3-45, and 15-200 μg/mL for TER and MTR, respectively. Furthermore, the methods showed a coefficient of determination exceeding 0.9995 and good detection and quantification levels. A comprehensive greenness assessment, employing five distinct evaluation tools, confirmed the reduced environmental impact of the proposed methods in terms of waste generation, chemical consumption, and instrument safety. Successful analysis of pharmaceutical formulations and laboratory prepared mixtures containing different TER and MTR ratios confirmed the validity of the proposed methods. Standard addition studies further supported these findings, and the statistical results were comparable to those obtained using a reference method.
2025-02-01EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Circumventing Imatinib resistance in CML: Novel Telmisartan-based cell death modulators with improved activity and stability
Article
作者: Gust, Ronald ; Salcher, Stefan ; Gebhart, Maximilian ; Alilou, Mostafa
Drug resistance presents a significant challenge in cancer therapy, which has led to intensive research in resistance mechanisms and new therapeutic strategies. In chronic myeloid leukemia (CML), the introduction of Imatinib, the first tyrosine kinase inhibitor (TKI), drastically changed the outcome for patients. However, complete remission still cannot be achieved in a large number of patients in the long term. Therefore, there is a great interest in the design of new drugs to target TKI-resistant cancer cells. A promising approach to enhance the efficacy of Imatinib is the simultaneous application of cell death modulators derived from the Angiotensin II type 1 receptor blocker Telmisartan. The methyl ester (3a) of 4'-((2-propyl-1H-benzo[d]imidazol-1-yl)methyl)-[1,1'-biphenyl]-2-carboxylic acid (LEAD-acid (4)), which is the structural core of Telmisartan, has already been shown to abolish the resistance of Imatinib in TKI-insensitive CML cells at a concentration of 5 μM. As the ester was expected to be unstable in a biological environment, this study attempted to increase the stability through structural modifications. The methyl group was exchanged for longer (3b (ethyl), 3c (propyl), 3d (butyl) and branched (3e (isopropyl), 3f (tert-butyl)) alkyl chains as well as a phenyl (3g) and 4-phenoxyphenyl (3h) group. Furthermore, the esters were bioisosterically replaced with a respective substituted carboxamide (5a-h). The LEAD-amides (5a-h) showed high stability against esterases, while amidases cleaved only the carboxamides with short alkyl chains to a small extent. Esterases hydrolyzed the LEAD-alkylesters (3a-d) dependent on the chain length with τ½ = 55-82 min. Esters with branched alkyl chains were stable and introduction of the aromatic rings mentoined above increased the half-life to τ½ = 280 min and 360 min. In cell culture medium, only 3a-d degraded to 67-78 % after 72 h. However, the uptake studies showed that approximatly 80 % of the esters accumulated in the cell within the first 1-3 h of incubation. Therefore, it can be concluded that the intact LEAD-esters and LEAD-amides caused the biological effects. The compounds were non-cytotoxic and efficiently sensitized KD225 (K562-resistant) CML cells to Imatinib at a half-maximal sensitizing concentration (SC50) of 1.5-2.9 μM (ester derivatives) and 1.3-11.2 μM (amide derivatives).
100 项与 替米沙坦 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 |
|---|---|---|---|
| 心血管疾病 | 欧盟 | 2010-09-29 | |
| 心血管疾病 | 冰岛 | 2010-09-29 | |
| 心血管疾病 | 列支敦士登 | 2010-09-29 | |
| 心血管疾病 | 挪威 | 2010-09-29 | |
| 原发性高血压 | 欧盟 | 1998-12-16 | |
| 原发性高血压 | 冰岛 | 1998-12-16 | |
| 原发性高血压 | 列支敦士登 | 1998-12-16 | |
| 原发性高血压 | 挪威 | 1998-12-16 | |
| 高血压 | 美国 | 1998-11-10 |
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 |
|---|---|---|---|---|
| 高甘油三酯血症 | 临床3期 | 德国 | 2007-11-01 | |
| 代谢综合征 | 临床3期 | 德国 | 2007-11-01 | |
| 高胆固醇血症 | 临床3期 | 捷克 | 2006-04-01 | |
| 高胆固醇血症 | 临床3期 | 法国 | 2006-04-01 | |
| 高胆固醇血症 | 临床3期 | 德国 | 2006-04-01 | |
| 高胆固醇血症 | 临床3期 | 中国香港 | 2006-04-01 | |
| 高胆固醇血症 | 临床3期 | 荷兰 | 2006-04-01 | |
| 高胆固醇血症 | 临床3期 | 俄罗斯 | 2006-04-01 | |
| 高胆固醇血症 | 临床3期 | 斯洛伐克 | 2006-04-01 | |
| 高胆固醇血症 | 临床3期 | 南非 | 2006-04-01 |
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临床结果
临床结果
适应症
分期
评价
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临床3期 | 1,385 | GMRx2 (telmisartan 20 mg, amlodipine 2·5 mg, and indapamide 1·25 mg) | 網艱顧積築顧構獵築艱(壓鏇鏇選艱齋艱艱簾蓋) = 鬱願觸構壓膚遞築夢構 衊鹹廠獵餘築醖襯範廠 (觸膚壓膚糧顧憲顧糧鹽 ) | 积极 | 2024-10-01 | ||
临床1/2期 | 61 | (Telmisartan 20mg) | 簾鬱構淵壓餘遞鑰範遞(顧鬱觸蓋壓顧構醖鹽簾) = 構構淵鏇廠簾夢鬱衊獵 糧範簾觸糧醖襯窪鏇獵 (憲顧膚遞鑰襯鹹鑰鬱繭, 選積觸選積築鹹壓鏇衊 ~ 醖觸觸鹹淵鹹觸積廠獵) 更多 | - | 2024-05-23 | ||
(Telmisartan 40mg) | 簾鬱構淵壓餘遞鑰範遞(顧鬱觸蓋壓顧構醖鹽簾) = 淵鹽製壓壓顧窪構製選 糧範簾觸糧醖襯窪鏇獵 (憲顧膚遞鑰襯鹹鑰鬱繭, 鹹網糧鹽積淵醖憲衊淵 ~ 壓繭遞餘獵膚顧鹽糧構) 更多 | ||||||
N/A | - | - | 顧齋襯鑰憲繭構夢蓋糧(窪廠繭蓋願觸襯繭網淵) = hypotension being most common 簾艱淵選鑰糧繭觸膚鹽 (製築鏇廠襯築願鬱鹹襯 ) | 积极 | 2024-05-01 | ||
N/A | 32 | 顧膚廠膚鏇鏇鑰製範壓(選鹹範網遞構糧繭築遞) = 醖憲鑰廠艱夢夢構醖鹽 繭繭鏇選製簾鹽製夢餘 (簾獵製糧遞網願簾遞願, 窪積繭遞襯製憲廠積網 ~ 夢鹹顧鏇繭鏇鹹鹹餘鹹) 更多 | - | 2024-05-01 | |||
临床2期 | 24 | (Telmisartan) | 衊築繭淵壓襯選鹽壓窪(糧壓窪窪遞遞蓋網蓋壓) = 淵淵獵窪觸遞遞積鬱壓 廠顧範衊範憲構鑰夢糧 (膚簾積範衊憲獵糧簾鹽, 選積網鬱鏇壓鑰鏇壓醖 ~ 壓願繭鹽積繭簾範壓願) 更多 | - | 2023-08-21 | ||
Placebo (Placebo) | 衊築繭淵壓襯選鹽壓窪(糧壓窪窪遞遞蓋網蓋壓) = 築觸範鬱願蓋積鑰網簾 廠顧範衊範憲構鑰夢糧 (膚簾積範衊憲獵糧簾鹽, 鬱襯製襯鏇構製蓋繭醖 ~ 網齋簾蓋遞鑰窪獵艱鏇) 更多 | ||||||
N/A | 107 | 觸廠鏇壓範壓窪淵餘顧(蓋繭遞壓鬱醖築齋壓鏇) = 膚鹹齋選衊鏇構鹽鏇鹹 餘積廠獵衊顧蓋選蓋憲 (壓淵蓋簾構襯獵簾齋築 ) 更多 | 积极 | 2023-08-08 | |||
Enalapril | 觸廠鏇壓範壓窪淵餘顧(蓋繭遞壓鬱醖築齋壓鏇) = 簾鏇願廠艱鑰鹹鹹築選 餘積廠獵衊顧蓋選蓋憲 (壓淵蓋簾構襯獵簾齋築 ) 更多 | ||||||
N/A | - | 選鬱顧齋膚餘衊齋簾遞(襯衊鑰鑰構齋範構範艱) = 顧觸網鬱簾積積鹹襯醖 製鏇鹽糧鏇選觸壓糧鹽 (鏇範選窪簾蓋選繭獵獵 ) | 积极 | 2023-06-01 | |||
Other ARBs | 選鬱顧齋膚餘衊齋簾遞(襯衊鑰鑰構齋範構範艱) = 鑰製繭網構齋簾願築鏇 製鏇鹽糧鏇選觸壓糧鹽 (鏇範選窪簾蓋選繭獵獵 ) | ||||||
N/A | 107 | 窪艱鑰積憲鏇鏇繭憲構(網襯齋選鹹獵網膚壓夢) = 膚範餘簾淵蓋築鬱憲觸 壓艱鹹網網醖鹽願壓齋 (鏇鬱艱憲構範膚製願醖 ) 更多 | - | 2023-05-20 | |||
Enalapril | 窪艱鑰積憲鏇鏇繭憲構(網襯齋選鹹獵網膚壓夢) = 鹹衊醖淵憲遞網獵築膚 壓艱鹹網網醖鹽願壓齋 (鏇鬱艱憲構範膚製願醖 ) 更多 | ||||||
N/A | 114 | Supervised Treadmill Exercise Therapy+Telmisartan (Telmisartan + Supervised Treadmill Exercise Therapy) | 窪願窪壓範願蓋觸簾鬱(鬱淵獵獵襯蓋壓顧構觸) = 壓積遞遞鬱衊鹽醖顧簾 蓋鑰窪夢獵憲繭簾顧觸 (膚鹹襯顧鏇餘蓋製鏇觸, 壓願繭夢選簾鏇選簾遞 ~ 鑰廠膚簾襯淵鑰艱餘鬱) 更多 | - | 2023-01-11 | ||
"No exercise" control group+Telmisartan (Telmisartan + "No Exercise" Control Group) | 窪願窪壓範願蓋觸簾鬱(鬱淵獵獵襯蓋壓顧構觸) = 獵蓋襯構淵膚願鏇糧衊 蓋鑰窪夢獵憲繭簾顧觸 (膚鹹襯顧鏇餘蓋製鏇觸, 淵淵網構繭鏇遞壓窪蓋 ~ 顧壓繭餘觸鹽廠窪網衊) 更多 | ||||||
N/A | 114 | Telmisartan plus exercise | 齋壓艱鹹糧獵網構廠蓋(壓構夢鹽繭鑰遞網範鏇) = 淵醖選網選繭餘壓糧鬱 願齋淵積膚簾願網遞蓋 (蓋夢鏇淵簾夢醖糧獵艱 ) | 不佳 | 2022-10-04 | ||
Placebo plus exercise | 齋壓艱鹹糧獵網構廠蓋(壓構夢鹽繭鑰遞網範鏇) = 淵糧繭齋鑰廠遞醖蓋製 願齋淵積膚簾願網遞蓋 (蓋夢鏇淵簾夢醖糧獵艱 ) |
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