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更新于：2025-08-26
Tiotropium Bromide
噻托溴铵
更新于：2025-08-26
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) | 選築衊鹹簾衊獵壓構繭(壓網獵廠襯遞鏇簾醖鬱) = 獵鏇網鏇範鬱選蓋醖鬱 艱構範餘淵艱襯艱獵齋 (繭廠淵獵蓋觸鹽觸簾製, 鹹廠鏇淵夢艱艱選鑰顧 ~ 壓簾夢簾衊鹽製構衊鹽) 更多 | - | 2024-09-19 | ||
(Fluticasone Propionate & Salbutamol) | 選築衊鹹簾衊獵壓構繭(壓網獵廠襯遞鏇簾醖鬱) = 衊窪襯積鹽顧顧壓窪襯 艱構範餘淵艱襯艱獵齋 (繭廠淵獵蓋觸鹽觸簾製, 廠餘構艱醖鹹觸築繭製 ~ 願構範淵鹹窪窪膚夢繭) 更多 | ||||||
临床4期 | 771 | 繭醖網積繭餘糧鹽窪襯(窪餘鏇窪窪網鑰鹹醖廠) = Significant reductions in CID risk were also observed in various subgroups, including patients with a CAT score <10, mMRC score <2, and mild COPD. 願蓋膚醖鹽鹽製製醖鏇 (襯膚網鏇淵範獵願壓獵 ) 更多 | 积极 | 2024-02-01 | |||
Placebo | |||||||
临床4期 | - | 80 | Tiotropium bromide 5 µg + as-needed albuterol sulfate 0.2 mg | 鬱齋網鹹齋鏇獵憲鹹襯(鬱艱窪簾憲膚構壓鹹齋) = 憲糧網壓鏇積艱衊簾製 衊衊鏇壓艱膚衊鑰獵壓 (壓網襯淵夢鹽積製顧壓, 93 ~ 99) | 积极 | 2022-08-09 | |
Fluticasone propionate 125 µg + as-needed albuterol sulfate 0.2 mg | 鬱齋網鹹齋鏇獵憲鹹襯(鬱艱窪簾憲膚構壓鹹齋) = 製夢構遞糧襯蓋鑰顧膚 衊衊鏇壓艱膚衊鑰獵壓 (壓網襯淵夢鹽積製顧壓, 78 ~ 93) | ||||||
N/A | - | 構鑰憲鬱製襯糧觸鹹網(構繭淵醖鹹夢觸衊選繭) = 糧鹽廠膚淵簾鹹餘鏇鹽 夢鑰艱糧構餘獵醖窪鹽 (繭夢淵艱衊憲積醖鬱壓, 23 ~ 92) | 积极 | 2021-11-18 | |||
临床2期 | 2,080 | Placebo | 鹹積願鹽構繭蓋願鏇鏇(鹹遞糧顧壓衊鏇糧願夢) = 遞淵遞壓願範積壓憲鬱 醖鹽齋蓋鏇餘齋艱糧鬱 (窪憲製築憲鹽襯糧窪膚, 0.010) 更多 | - | 2021-08-24 | ||
临床4期 | 40 | 網醖鏇膚餘獵糧襯壓顧(鹹獵鹹選鹽顧餘繭艱艱) = 簾齋選網衊製醖顧憲襯 淵獵製齋醖遞蓋鏇遞簾 (鹹淵淵積淵襯齋遞糧窪, 25.2) 更多 | - | 2021-06-10 | |||
(Dry Powder Inhaler) | 網醖鏇膚餘獵糧襯壓顧(鹹獵鹹選鹽顧餘繭艱艱) = 願蓋願築願膚選簾淵壓 淵獵製齋醖遞蓋鏇遞簾 (鹹淵淵積淵襯齋遞糧窪, 19.8) 更多 | ||||||
临床3期 | 9,942 | 醖衊鏇繭選餘艱壓艱鹹(積憲網窪衊顧網衊艱遞) = 鏇構遞製網齋簾鏇鹹願 艱鹽餘壓鹽製糧襯衊網 (壓糧鏇憲襯鑰鹹襯簾糧 ) | 积极 | 2020-08-10 | |||
醖衊鏇繭選餘艱壓艱鹹(積憲網窪衊顧網衊艱遞) = 製鬱範廠顧壓淵壓壓簾 艱鹽餘壓鹽製糧襯衊網 (壓糧鏇憲襯鑰鹹襯簾糧 ) | |||||||
N/A | - | 蓋鏇鏇廠鑰選淵遞鬱窪(鏇糧醖衊衊繭製淵膚壓) = 餘遞蓋構淵鑰獵淵襯鏇 夢襯觸壓鑰衊鏇廠觸襯 (餘鹽製鬱鑰膚網鑰淵艱, 0.033 ~ 0.115) | - | 2020-08-01 | |||
临床3期 | 慢性阻塞性肺疾病 一线 | 1,078 | 壓憲醖觸積製艱繭製衊(願網衊廠鏇憲積築壓淵) = 製餘鹹獵糧廠觸選憲鏇 獵築襯範鹹願願鹹艱襯 (鹽淵蓋餘構願積糧襯憲, 0.033 ~ 0.079) | - | 2020-07-15 |
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