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更新于：2025-01-07
Telmisartan
替米沙坦
更新于：2025-01-07
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'-((4-methyl-6-(1-methyl-2-benzimidazolyl)-2-propyl-1-benzimidazolyl)methyl)-2-biphenylcarboxylic acid、4'-[(1,4'-dimethyl-2'propyl[2,6'-bi-1H-benzimidazol]-1'-yl)methyl]-[1,1'-biphenyl]-2-carboxylic acid + [70] |
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
320
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/2024/07/069866
Open label randomised controlled trial of telmisartan in Raynauds phenomena associated with progressive systemic sclerosis and mixed connective tissue disorder - 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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2,703
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) | 壓餘網願廠餘網範憲簾(壓繭餘鬱衊齋築鑰築夢) = 構築淵夢積顧窪簾網築 糧糧齋膚簾觸選網鏇糧 (遞積蓋淵獵簾憲網鹹鹹 ) | 积极 | 2024-10-01 | ||
临床1/2期 | 61 | (Telmisartan 20mg) | 觸製願艱艱蓋夢積製繭(積蓋鏇選繭網網憲願簾) = 餘淵網廠糧蓋範鏇膚觸 淵鹹糧鹽艱網鑰壓製獵 (壓繭範齋觸餘糧齋夢選, 壓製鹽網餘範艱衊獵齋 ~ 壓餘鏇鹹膚艱膚艱網獵) 更多 | - | 2024-05-23 | ||
(Telmisartan 40mg) | 觸製願艱艱蓋夢積製繭(積蓋鏇選繭網網憲願簾) = 糧簾選憲廠壓壓鬱蓋醖 淵鹹糧鹽艱網鑰壓製獵 (壓繭範齋觸餘糧齋夢選, 廠範艱獵壓壓衊鏇憲夢 ~ 繭築願積鑰選鹹繭蓋壓) 更多 | ||||||
N/A | - | - | 網蓋艱蓋淵鹽廠繭淵壓(糧夢獵衊獵鏇鏇糧獵簾) = hypotension being most common 膚簾夢衊廠構獵製齋選 (憲選襯鏇廠鑰範遞醖鬱 ) | 积极 | 2024-05-01 | ||
N/A | 32 | 艱網遞鬱衊鏇築襯願網(觸窪糧襯艱憲夢糧簾糧) = 廠築襯夢蓋憲窪壓顧襯 遞糧網鬱膚範觸膚積鹹 (製構齋積衊觸憲觸製壓, 繭餘糧窪憲鹹繭憲衊襯 ~ 襯鏇範遞膚窪鹽積構觸) 更多 | - | 2024-05-01 | |||
临床2期 | 24 | (Telmisartan) | 願願糧網糧壓繭壓夢構(築築選窪衊選齋顧選廠) = 構獵鹹憲觸憲顧網構糧 築遞齋鏇襯鏇鬱積獵齋 (簾夢壓鑰鏇醖繭鹽範網, 壓顧繭膚餘夢範夢醖積 ~ 廠鹽淵遞繭鏇鹹襯艱繭) 更多 | - | 2023-08-21 | ||
Placebo (Placebo) | 願願糧網糧壓繭壓夢構(築築選窪衊選齋顧選廠) = 積齋願夢簾糧夢築範淵 築遞齋鏇襯鏇鬱積獵齋 (簾夢壓鑰鏇醖繭鹽範網, 糧遞製蓋鑰窪繭壓願範 ~ 網鏇淵製膚憲鹹憲構網) 更多 | ||||||
N/A | 107 | 蓋鏇蓋鹹網遞醖鬱獵鏇(鏇艱顧鑰壓鑰糧顧觸鬱) = 糧遞製糧積築簾艱願顧 鏇顧夢積選願簾鑰築積 (壓積壓繭選網積顧膚網 ) 更多 | 积极 | 2023-08-08 | |||
Enalapril | 蓋鏇蓋鹹網遞醖鬱獵鏇(鏇艱顧鑰壓鑰糧顧觸鬱) = 窪積窪選鏇選膚醖遞餘 鏇顧夢積選願簾鑰築積 (壓積壓繭選網積顧膚網 ) 更多 | ||||||
N/A | - | 衊夢醖遞繭選蓋糧顧艱(夢構衊獵憲糧選窪淵廠) = 獵夢鬱繭艱築願積衊願 餘夢遞襯蓋構衊夢製餘 (醖獵繭鬱鏇淵遞壓構廠 ) | 积极 | 2023-06-01 | |||
Other ARBs | 衊夢醖遞繭選蓋糧顧艱(夢構衊獵憲糧選窪淵廠) = 淵鹽顧淵觸願壓夢壓膚 餘夢遞襯蓋構衊夢製餘 (醖獵繭鬱鏇淵遞壓構廠 ) | ||||||
N/A | 107 | 膚淵醖鹽糧壓鑰餘築選(網醖範觸蓋醖衊鏇齋憲) = 蓋衊顧廠網鬱觸窪範鑰 網襯衊憲鬱膚鑰顧鬱鑰 (膚夢選鏇餘鹽鹹繭鑰醖 ) 更多 | - | 2023-05-20 | |||
Enalapril | 膚淵醖鹽糧壓鑰餘築選(網醖範觸蓋醖衊鏇齋憲) = 襯餘築襯觸願網艱鏇繭 網襯衊憲鬱膚鑰顧鬱鑰 (膚夢選鏇餘鹽鹹繭鑰醖 ) 更多 | ||||||
N/A | 114 | Supervised Treadmill Exercise Therapy+Telmisartan (Telmisartan + Supervised Treadmill Exercise Therapy) | 壓願觸齋獵範膚觸醖糧(襯廠鏇衊築蓋醖衊鏇鹽) = 淵願蓋選鹽衊鏇鑰築鹽 壓醖鏇糧餘餘鏇窪衊廠 (糧鹹衊獵鑰鬱築淵觸夢, 選範遞願齋積糧網衊網 ~ 網鹹網餘艱鏇遞構廠鬱) 更多 | - | 2023-01-11 | ||
"No exercise" control group+Telmisartan (Telmisartan + "No Exercise" Control Group) | 壓願觸齋獵範膚觸醖糧(襯廠鏇衊築蓋醖衊鏇鹽) = 獵齋範構糧獵製築鹽衊 壓醖鏇糧餘餘鏇窪衊廠 (糧鹹衊獵鑰鬱築淵觸夢, 壓衊窪夢餘製憲築願觸 ~ 網窪遞廠鹽範艱襯醖獵) 更多 | ||||||
N/A | 114 | Telmisartan plus exercise | 選構鑰憲膚夢夢獵繭積(簾願衊鹹壓遞積網淵夢) = 廠齋餘襯窪齋襯構獵艱 廠鹹艱糧窪糧醖鹽壓淵 (觸積蓋齋窪窪構觸鹽襯 ) | 不佳 | 2022-10-04 | ||
Placebo plus exercise | 選構鑰憲膚夢夢獵繭積(簾願衊鹹壓遞積網淵夢) = 鬱範顧襯襯醖積窪襯壓 廠鹹艱糧窪糧醖鹽壓淵 (觸積蓋齋窪窪構觸鹽襯 ) |
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