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更新于：2025-08-31
Tiotropium Bromide
噻托溴铵
更新于：2025-08-31
概要
基本信息
最高研发阶段批准上市 |
首次获批日期 英国 (2002-04-02), |
最高研发阶段(中国)批准上市 |
特殊审评孤儿药 (美国) |
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结构/序列
分子式C19H24BrNO5S2 |
InChIKeyMQLXPRBEAHBZTK-SEINRUQRSA-M |
CAS号411207-31-3 |
关联
372
项与 噻托溴铵 相关的临床试验CTRI/2025/05/087465
A Multicenter, Randomized, Assessor-Blind, Three period, Six-Sequence, Active- and Placebo- Controlled, Crossover, Single-Dose Study to Evaluatethe Bioequivalence (with Clinical Pharmacodynamic Endpoint) of Test Formulation Tiotropium Bromide Inhalation Powder 18 mcg/capsule with Reference Formulation Adult Patients with Chronic Obstructive Pulmonary Disease (COPD). - Nil
CTR20250934
噻托溴铵吸入粉雾剂随机、双盲、两周期、交叉设计的生物等效性研究
CTR20250548
噻托溴铵吸入粉雾剂单中心、随机、开放、双周期、双交叉设计的生物等效性试验
100 项与 噻托溴铵 相关的临床结果
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100 项与 噻托溴铵 相关的转化医学
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100 项与 噻托溴铵 相关的专利（医药）
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2,243
项与 噻托溴铵 相关的文献（医药）2025-09-02JOURNAL OF ASTHMA
Efficacy of tiotropium bromide on spirometric measurements and control of asthma in real life: data from a 1-year clinical follow-up
Article
作者: Aksu, Kurtuluş ; Çelik, Enes ; Akkale, Özgür ; Köycü Buhari, Gözde ; Aksu, Funda ; Dindar Çelik, Fatma ; Telli, Onur ; Çelik Tuğlu, Hatice ; Yağdıran, Melis ; Nazik Bahçecioğlu, Sakine
OBJECTIVE:
Real-life studies are needed to evaluate the clinical outcomes of add-on tiotropium therapy in patients with asthma. The effects of adding tiotropium bromide to the treatment of asthmatic patients on pulmonary functions and asthma control using real-life data.
METHODS:
In a retrospective study, spirometric measures and asthma control states were compared before and one year after of tiotropium treatment in asthmatic adults whose disease was not adequately controlled with a combination of inhaled corticosteroids and long-acting β2-agonists.
RESULTS:
One year after tiotropium treatment, mean FEV1, FEV1%, and FEV1/FVC ratio increased significantly compared to pretreatment values. Among 32 patients added tiotropium due to symptomatic asthma, 28 (87.5%) patients achieved well-controlled (ACT ≥ 20) end of the year and GINA treatment step-down in 4 (12.5%) patients. Monoclonal antibody therapies (mepolizumab or omalizumab) were initiated in 9 patients (28.1%). FEV1 values and FEV1/FVC ratios showed a statistically significant improvement from baseline measurements obtained prior to the initiation of tiotropium therapy, independent of monoclonal antibody use (p < .001 for each). The mean age of these patients was 48.78 ± 11.64 (range: 28-81) years, and 25 (78.1%) of them were female.
CONCLUSIONS:
Tiotropium bromide is an effective and reliable add-on therapy for symptomatic asthma when combined with ICS plus LABA, also leads to improvements in respiratory function and asthma control.
2025-09-01ENVIRONMENTAL POLLUTION
Validation of a large volume-solid phase extraction methodology for biotoxicity assessment of pharmaceuticals in aquatic organisms
Article
作者: Gómez-Canela, Cristian ; Moragrega-Knol, Emma ; Barata, Carlos ; Romero-Alfano, Irene
The growing scarcity of freshwater has intensified the need for alternative water sources, which often require advanced treatments to eliminate contaminants. Among emerging pollutants, pharmaceuticals have become a significant concern due to their persistence and potential impact, making their detection essential. However, analysing these contaminants is challenging due to the extremely low concentrations at which they are present. For chemical analysis, minimal or no sample enrichment is often necessary, while bioanalysis typically requires larger sample volumes and an enrichment factor to conduct comprehensive bioassays across various endpoints. Consequently, sample preconcentration techniques for large water volumes are necessary to improve the sensitivity of subsequent toxicological experiments. In this study, a novel large volume solid-phase extraction (LV-SPE) procedure was validated and evaluated for monitoring multiple pharmaceutical compounds in water samples, while maintaining the traditional solid-phase extraction (SPE) methodology using cartridges. This method proved effective extraction and preconcentration of significant amounts of water, with recoveries between 19 % and 109 % in spiked wastewaters (except for fluvoxamine, remdesivir, tamoxifen and tetracycline, with recoveries <10 %). Furthermore, the optimization of this approach covers an expansive chemical space, enabling the capture of a diverse range of pharmaceutical compounds and enhancing the validity of toxicological studies. Bioassays conducted with Daphnia magna juveniles and Danio rerio embryos validated the method's applicability regarding optimized exposure conditions, the absence of adverse effects from SPE blanks or solvent controls and sensitivity in detecting effects across field samples. Overall, the LV-SPE approach enhances sensitivity and reliability for evaluating pharmaceutical mixtures' risks under realistic conditions.
2025-07-14Journal of Chemical Information and Modeling
Adiabatic-Bias Molecular Dynamics Simulations Reveal the Impact of Mutations on Muscarinic Antagonist Unbinding Kinetics
Article
作者: Coricello, Adriana ; Bottegoni, Giovanni ; Elisi, Gian Marco ; Tehan, Benjamin Gerald ; Chiaravalle, Anna Lisa ; Musgaard, Maria
Ligand-target dissociation rates (koff) strongly correlate with efficacy and safety profiles, as well as with the therapeutic effect of drugs. As a prototypical example, muscarinic receptor antagonists used as bronchodilators show similar affinity profiles toward the muscarinic M3 receptors (M3R) and M2 receptors (M2R), whereas their kinetic selectivity toward M3R avoids the adverse effects that a prolonged inhibition of M2R would induce at the cardiac level. Previous studies on the dissociation kinetics of human M3R showed that the residence time and binding affinity of muscarinic antagonists are deeply affected by the presence of specific mutations. The aim of our work was to reproduce the rankings of these experimental kinetic rates through an approach based on the application of adiabatic-bias molecular dynamics (ABMD) simulations using Path Collective Variables (PCVs), PCV-ABMD. Employing this methodology, we simulated the translocation of tiotropium, a long-acting bronchodilator targeting M3R, from the orthosteric site to the extracellular vestibule, without considering the whole unbinding process. The estimated times necessary for translocation displayed a strong correlation with the experimental pkoff values. Moreover, a thorough analysis of protein-ligand contacts provided deeper insights into the mechanism of unbinding of muscarinic antagonists. The newly described PCV-ABMD protocol captured relevant metastable states and offered a reliable approach for the prediction of kinetic selectivity in sets of mutants.
100 项与 噻托溴铵 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 |
|---|---|---|---|
| 哮喘 | 日本 | 2014-11-18 | |
| 哮喘 | 日本 | 2014-11-18 | |
| 支气管痉挛 | 美国 | 2004-01-30 | |
| 慢性支气管炎 | 美国 | 2004-01-30 | |
| 肺气肿 | 美国 | 2004-01-30 | |
| 慢性阻塞性肺疾病 | 奥地利 | 2002-04-02 | |
| 慢性阻塞性肺疾病 | 比利时 | 2002-04-02 | |
| 慢性阻塞性肺疾病 | 保加利亚 | 2002-04-02 | |
| 慢性阻塞性肺疾病 | 塞浦路斯 | 2002-04-02 | |
| 慢性阻塞性肺疾病 | 捷克 | 2002-04-02 | |
| 慢性阻塞性肺疾病 | 丹麦 | 2002-04-02 | |
| 慢性阻塞性肺疾病 | 芬兰 | 2002-04-02 | |
| 慢性阻塞性肺疾病 | 法国 | 2002-04-02 | |
| 慢性阻塞性肺疾病 | 德国 | 2002-04-02 | |
| 慢性阻塞性肺疾病 | 希腊 | 2002-04-02 | |
| 慢性阻塞性肺疾病 | 匈牙利 | 2002-04-02 | |
| 慢性阻塞性肺疾病 | 冰岛 | 2002-04-02 | |
| 慢性阻塞性肺疾病 | 爱尔兰 | 2002-04-02 | |
| 慢性阻塞性肺疾病 | 意大利 | 2002-04-02 | |
| 慢性阻塞性肺疾病 | 拉脱维亚 | 2002-04-02 |
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 |
|---|---|---|---|---|
| 囊性纤维化 | 临床3期 | 美国 | 2010-09-01 | |
| 囊性纤维化 | 临床3期 | 澳大利亚 | 2010-09-01 | |
| 囊性纤维化 | 临床3期 | 奥地利 | 2010-09-01 | |
| 囊性纤维化 | 临床3期 | 比利时 | 2010-09-01 | |
| 囊性纤维化 | 临床3期 | 加拿大 | 2010-09-01 | |
| 囊性纤维化 | 临床3期 | 捷克 | 2010-09-01 | |
| 囊性纤维化 | 临床3期 | 法国 | 2010-09-01 | |
| 囊性纤维化 | 临床3期 | 德国 | 2010-09-01 | |
| 囊性纤维化 | 临床3期 | 匈牙利 | 2010-09-01 | |
| 囊性纤维化 | 临床3期 | 爱尔兰 | 2010-09-01 |
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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4期 | 80 | (Tiotropium Bromide & Salbutamol) | 構淵遞簾衊鹹鏇廠願餘(窪鏇襯築積鏇構獵窪範) = 壓遞醖顧築淵膚醖選窪 醖糧鏇積艱壓簾襯衊窪 (餘鬱網積憲繭衊憲鏇範, 構繭顧淵襯築選鏇鏇襯 ~ 鹹艱選網鏇衊繭夢壓艱) 更多 | - | 2024-09-19 | ||
(Fluticasone Propionate & Salbutamol) | 構淵遞簾衊鹹鏇廠願餘(窪鏇襯築積鏇構獵窪範) = 鹹淵鏇積築衊選顧齋網 醖糧鏇積艱壓簾襯衊窪 (餘鬱網積憲繭衊憲鏇範, 網衊選願廠繭壓夢鹹夢 ~ 衊壓夢艱鹽壓壓鬱廠襯) 更多 | ||||||
临床4期 | 771 | 獵壓窪齋構鏇餘糧憲積(繭簾鏇淵顧壓餘鹽繭製) = Significant reductions in CID risk were also observed in various subgroups, including patients with a CAT score <10, mMRC score <2, and mild COPD. 鹹鑰築夢醖衊簾願淵鬱 (構築淵顧廠選積壓網膚 ) 更多 | 积极 | 2024-02-01 | |||
Placebo | |||||||
临床4期 | - | 80 | Tiotropium bromide 5 µg + as-needed albuterol sulfate 0.2 mg | 齋鬱衊網構艱窪艱壓憲(淵遞膚簾鏇製鹹鏇鑰鬱) = 簾齋夢衊醖衊簾蓋鑰簾 築窪網鏇繭繭選遞餘廠 (艱網網範簾簾艱觸鬱鹹, 93 ~ 99) | 积极 | 2022-08-09 | |
Fluticasone propionate 125 µg + as-needed albuterol sulfate 0.2 mg | 齋鬱衊網構艱窪艱壓憲(淵遞膚簾鏇製鹹鏇鑰鬱) = 窪選艱齋壓製蓋鹹製窪 築窪網鏇繭繭選遞餘廠 (艱網網範簾簾艱觸鬱鹹, 78 ~ 93) | ||||||
N/A | - | 鬱襯廠遞憲遞簾壓糧構(選淵餘鏇鏇鏇膚鏇襯遞) = 繭襯網夢衊齋鑰窪鹽餘 憲觸選憲廠膚製簾蓋壓 (鹹鏇艱糧選淵繭憲鬱獵, 23 ~ 92) | 积极 | 2021-11-18 | |||
临床2期 | 2,080 | Placebo | 艱顧淵餘製憲淵淵製鹽(糧範遞獵觸選艱築醖獵) = 艱餘夢顧襯鏇獵獵餘糧 網繭觸齋鏇廠製餘鏇製 (鬱網蓋鬱齋繭醖艱窪窪, 0.010) 更多 | - | 2021-08-24 | ||
临床4期 | 40 | 淵獵簾願襯淵願壓廠網(鬱積鏇觸衊齋選糧鹽窪) = 繭憲製襯鏇願艱網獵窪 襯顧願餘淵選衊築醖蓋 (膚遞簾簾夢廠廠廠範壓, 25.2) 更多 | - | 2021-06-10 | |||
(Dry Powder Inhaler) | 淵獵簾願襯淵願壓廠網(鬱積鏇觸衊齋選糧鹽窪) = 遞窪糧糧壓築簾衊襯膚 襯顧願餘淵選衊築醖蓋 (膚遞簾簾夢廠廠廠範壓, 19.8) 更多 | ||||||
临床3期 | 9,942 | 壓鑰鹹襯鑰鬱製衊觸鏇(構鹹壓遞糧鹽鹽廠衊繭) = 艱積齋構遞艱簾壓選夢 窪簾願膚築築齋膚鑰廠 (廠觸壓選醖築鹹選繭鏇 ) | 积极 | 2020-08-10 | |||
壓鑰鹹襯鑰鬱製衊觸鏇(構鹹壓遞糧鹽鹽廠衊繭) = 鹹繭齋夢鬱糧獵鏇鹹範 窪簾願膚築築齋膚鑰廠 (廠觸壓選醖築鹹選繭鏇 ) | |||||||
N/A | - | 夢窪餘簾鑰遞衊遞遞淵(構憲顧壓艱積廠醖醖鹹) = 鹹餘艱餘顧餘簾夢願艱 簾衊鏇構艱製醖襯願構 (蓋鑰窪鹽鹹鹽夢簾淵製, 0.033 ~ 0.115) | - | 2020-08-01 | |||
临床3期 | 慢性阻塞性肺疾病 一线 | 1,078 | 襯遞鹹淵壓築廠餘鬱憲(網顧獵鏇壓淵觸齋製鏇) = 鹽鑰顧窪獵繭積鏇壓襯 鑰獵艱鬱製蓋憲網網觸 (襯鏇膚選鏇蓋壓網鏇壓, 0.033 ~ 0.079) | - | 2020-07-15 |
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