预约演示
更新于：2026-10-28
Glycopyrrolate/Indacaterol Maleate
茚达特罗/格隆溴铵
更新于：2026-10-28
概要
基本信息
药物类型 小分子化药 |
别名 Glycopyrrolate/indacaterol、Glycopyrronium bromide/indacaterol maleate、Indacaterol Maleate and Glycopyrronium Bromide + [23] |
作用方式 拮抗剂、激动剂 |
作用机制 mAChRs拮抗剂(毒蕈碱型乙酰胆碱受体家族拮抗剂)、β2-adrenergic receptor激动剂(β2-肾上腺素能受体激动剂) |
最高研发阶段批准上市 |
首次获批日期 欧盟 (2013-09-18), |
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C43H56BrN3O6 |
InChIKeyGCUZFFAPBPDIFM-IKXQUJFKSA-M |
CAS号1262431-94-6 |
关联
77
项与 茚达特罗/格隆溴铵 相关的临床试验NCT07896252
Randomized, Double-Blind, Placebo-Controlled, 14-Day Treatment, 2-Period Crossover Trial Evaluating the Lung Function Response After Treatment With Inhaled LABA and LAMA Monotherapies and Their Combination AERO-007 Administered Via Nebulization in Participants With Chronic Obstructive Pulmonary Disease (COPD) (AERODUO-2 Trial)
CTR20261764
评估受试制剂茚达特罗格隆溴铵吸入粉雾剂与参比制剂茚达特罗格隆溴铵吸入粉雾剂（杰润®，Ultibro®）在健康成年试验参与者中的生物等效性研究
CTR20260229
茚达特罗格隆溴铵吸入粉雾剂在健康试验参与者中空腹状态下的单中心、开放、随机、单剂量、两周期、两序列、交叉生物等效性试验
100 项与 茚达特罗/格隆溴铵 相关的临床结果
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100 项与 茚达特罗/格隆溴铵 相关的转化医学
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100 项与 茚达特罗/格隆溴铵 相关的专利（医药）
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86
项与 茚达特罗/格隆溴铵 相关的文献（医药）2026-06-01THORAX
Disproportionate increase in COPD exacerbation risk for 3 months after discontinuing LAMA or ICS: insights from the FLAME trial
Article
作者: Sivapalan, Pradeesh ; Mathioudakis, Alexander G ; Bakerly, Nawar Diar ; Chatzimavridou-Grigoriadou, Victoria ; Bate, Sebastian ; Vestbo, Jørgen ; Jensen, Jens-Ulrik Stæhr ; Singh, Dave
Background:
In real-world chronic obstructive pulmonary disease (COPD) care, poor adherence often leads to treatment discontinuations. Discontinuing inhaled corticosteroids (ICS) can trigger withdrawal effects transiently increasing exacerbation risk; but evidence for long-acting muscarinic antagonists (LAMA) withdrawal remains limited.
Methods:
We performed a post hoc analysis of the 52-week, double-blind, Effect of Indacaterol Glycopyrronium versus Fluticasone Salmeterol on COPD Exacerbations trial that compared long-acting beta-2 agonist (LABA)+LAMA with LABA+ICS in 3362 patients with moderate-to-severe COPD and exacerbation history. Potential withdrawal effects after discontinuing LAMA or ICS were suggested by monthly exacerbation incidence plots during the first quarter of follow-up. Participants were stratified by their baseline use of these therapies, and outcomes were compared between the first and subsequent quarters among those who continued versus discontinued each treatment. Multivariable mixed-effects models assessed differences in exacerbation rates, with temporal variation in treatment effects interpreted as indicative of withdrawal effects.
Results:
Discontinuing LAMA was associated with a marked, transient increase in moderate-to-severe exacerbations during the first versus subsequent quarters (p=0.001; rate ratio up to 2.2 (95% CI 1.2 to 4.1) in the subgroup least influenced by concomitant ICS use). This observation was not confirmed for severe exacerbations, likely due to low event count. In contrast, discontinuing ICS was associated with a significant early rise in severe exacerbations (p=0.023), though the difference for moderate-to-severe events did not reach statistical significance. Importantly, ICS withdrawal effects appeared consistent regardless of baseline blood eosinophil count.
Conclusion:
Our findings suggest potent LAMA and ICS treatment withdrawal effects on exacerbations, highlighting the importance of treatment adherence and accounting for withdrawal effects in clinical trials.
Trial registration number:
NCT01782326
.
2025-10-01Journal of Thoracic Disease
Efficacy, pharmacokinetics, and safety of nebulized HL231 inhalation solution in patients with chronic obstructive pulmonary disease: a randomized trial
Article
作者: Bian, Tao ; Xiong, Hao ; Li, Fangqiong ; Yue, Yun ; Xie, Lihua ; Li, Yaming ; Xiao, Zuke ; Hu, Qingyuan ; Yang, Guoping ; Zhao, Li ; Chen, Feng ; Wen, Fuqiang ; Luo, Zhu ; He, Qing ; Luo, Lin
Background:
Long-acting beta-agonist (LABA) plus long-acting muscarinic antagonist (LAMA) is superior to monotherapy or corticosteroid/LABA in terms of improving lung function, alleviating symptoms and educe chronic obstructive pulmonary disease (COPD) exacerbations. This study aimed to establish optimal dosage of nebulized HL231 inhalation solution (HL231), comparable to Ultibro® (110 µg indacaterol maleate/50 µg glycopyrronium bromide), for bronchodilatation, pharmacokinetics, and safety in COPD.
Methods:
This study employed a multicenter, randomized, single-dose, single-blind, crossover design and featured two parts. The randomization schedule was generated by the statistical team using the block randomization procedure in SAS software. Chinese adults aged 40 years or older who were diagnosed with moderate-to-severe COPD using the Global Initiative for Chronic Obstructive Lung Disease (GOLD) criteria were eligible for the study. Blinding was implemented for the personnel conducting pulmonary function tests. In Part A, patients were randomized to receive a single dose of HL231 (132 µg/72 µg, 261 µg/141 µg, or 516 µg/279 µg), Ultibro®, or placebo in a randomized sequence with a washout period of at least 14 days between two visits. The primary efficacy endpoint was the change in the area under the curve (AUC) of FEV1 from baseline to 12 h after administration (ΔFEV1 AUC0-12h). In Part B, patients were randomized to receive a single dose of HL231 (261 µg/120 µg and 261 µg/141 µg), or Ultibro® in a randomized sequence. The primary endpoints were pharmacokinetic parameters, including the AUC from time 0 to the last detectable time point (AUC0-t), AUC from time 0 to infinity (AUC0-∞), and peak concentration (Cmax). Safety was evaluated in both parts.
Results:
The study was initiated and completed between December 2021 and May 2023, with 173 and 29 patients screened in Part A and Part B respectively, resulting in 84 and 18 randomized patients, of whom 83 and 18 completed at least one treatment cycle. In Part A, the least squares (LS) mean differences in ΔFEV1 AUC0-12h for HL231 doses (132 µg/72 µg, 261 µg/141 µg, and 516 µg/279 µg) and Ultibro® versus placebo were 2.30, 2.58, 2.68, and 2.33 L·h (all P<0.001), respectively, while compared to Ultibro®, differences were -0.04 (P=0.83), 0.24 (P=0.14), and 0.35 L·h (P=0.04), respectively. Moreover, the LS means of ΔFEV1 AUC0-12h for these doses were 2.30, 2.58, and 2.69 L·h, indicating a dose-response relationship. In Part B, HL231 261 µg/141 µg demonstrated peak concentration (Cmax) of indacaterol and glycopyrronium at 86% and 54% of Ultibro®, with comparable AUC0-t. Safety was acceptable, with most treatment-emergent adverse events (TEAEs) being grade 1-2.
Conclusions:
HL231 (261 µg/141 µg) is highly comparable to Ultibro® in bronchodilatation, pharmacokinetics, and safety, making it a potential alternative for COPD patients.
Trial Registration:
This study was registered at Chinese Clinical Trials Registration (ChiCTR2300068316) and clinicaltrials.gov (NCT06619210, retrospectively registered).
2024-02-01International journal of pharmaceutics
Mixing energy as an adjustment tool for aerodynamic behaviour of an inhaled product: In-vitro and in-vivo effects
Article
作者: Merja Kirjavainen ; Ann-Marie Lyberg ; Laura Matilainen ; Stefan Göransson ; Kyrre Thalberg ; Elina Heinonen ; Satu Lähelmä ; Johanna Husman-Piirainen ; Maiju Autio ; Patrik Eriksson
This paper describes the development of a fixed dose dry powder combination of indacaterol maleate (Inda) and glycopyrronium bromide (Glyco) in Easyhaler® inhaler for a comparative pharmacokinetic (PK) study, as well as the outcome of such a study. The development aim was to produce formulations with three different in vitro dispersibility profiles for both Inda and Glyco. This so-called 'rake' approach allows for quantitation of the candidate formulations relative to the reference product Ultibro® Breezhaler® in terms of the key PK parameters. Three formulations (A, B and C) were produced based on the mixing energy concept. For both APIs, formulation A (lowest mixing energy) displayed the highest fine particle fractions and formulation C (highest mixing energy) the lowest. GMP manufacturing confirmed the performance of the three formulations. The candidate formulations were tested against the reference product in a single dose PK study in healthy volunteers. Clear differences in Inda plasma concentration profiles were observed between the treatments when administered concomitantly with charcoal, with Easyhaler A showing the highest Cmax value and Easyhaler C the lowest. Easyhaler B was bioequivalent to Ultibro Breezhaler with regard to the primary PK parameters of Inda, Cmax and AUC72h. For Glyco, Easyhaler formulations A, B and C provided lower peak concentrations than Ultibro Breezhaler. For AUC72h of Glyco, Easyhaler B was bioequivalent to the reference product. Additional measures for adjustment of formulation performance can be foreseen, whose effects can be predicted based on mixing energy theory.
100 项与 茚达特罗/格隆溴铵 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 |
|---|---|---|---|
| 气道阻塞 | 美国 | 2015-10-29 | |
| 慢性支气管炎 | 美国 | 2015-10-29 | |
| 肺气肿 | 美国 | 2015-10-29 | |
| 慢性阻塞性肺疾病 | 欧盟 | 2013-09-18 | |
| 慢性阻塞性肺疾病 | 冰岛 | 2013-09-18 | |
| 慢性阻塞性肺疾病 | 列支敦士登 | 2013-09-18 | |
| 慢性阻塞性肺疾病 | 挪威 | 2013-09-18 |
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 |
|---|---|---|---|---|
| 呼吸困难 | 临床3期 | 比利时 | 2011-10-01 | |
| 呼吸困难 | 临床3期 | 加拿大 | 2011-10-01 | |
| 呼吸困难 | 临床3期 | 德国 | 2011-10-01 | |
| 呼吸困难 | 临床3期 | 西班牙 | 2011-10-01 | |
| 呼吸困难 | 临床3期 | 英国 | 2011-10-01 | |
| 慢性肺疾病 | 临床2期 | 英国 | 2026-10-01 |
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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 | 3,362 | 膚鏇獵壓衊鑰壓鹽壓膚(製衊鑰觸製衊鹽夢簾繭): RR = 2.2 (95.0% CI, 1.2 ~ 4.1), P-Value = 0.001 更多 | 积极 | 2025-12-15 | |||
Fluticasone Salmeterol | |||||||
N/A | 191 | Umeclidinium/Vilanterol (UMEC/VI) 62.5/25 µg | 淵淵遞選醖蓋網憲鏇淵(鏇願選窪繭繭範餘範齋) = 築鹹壓獵積糧鬱製蓋積 餘憲遞憲鹽積鏇襯蓋顧 (顧選壓醖憲構製獵醖簾, 105 ~ 180) | 积极 | 2025-05-16 | ||
临床3期 | 780 | (Indacaterol/Glycopyrrolate) | 範糧醖製範築夢艱製遞 = 膚鬱鑰獵壓製觸積顧鑰 廠衊壓廠獵簾蓋鹽齋選 (壓獵築齋鏇製顧廠築鏇, 遞襯淵鬱觸齋鹽網憲壓 ~ 憲鹽構淵簾願窪鏇積蓋) 更多 | - | 2022-08-30 | ||
Placebo (Placebo) | 範糧醖製範築夢艱製遞 = 觸憲顧範齋鏇膚製繭廠 廠衊壓廠獵簾蓋鹽齋選 (壓獵築齋鏇製顧廠築鏇, 艱憲鬱憲繭夢窪構鏇壓 ~ 淵鹽鏇鑰積襯鏇鬱餘膚) 更多 | ||||||
临床4期 | 379 | (Indacaterol and Glycopyrronium (QVA149)) | 糧製鏇鬱糧壓廠衊製糧(築壓醖鑰鑰鏇構憲鬱願) = 鏇糧獵餘壓鹹鑰網鑰構 簾範積顧鹹觸繭膚鹽廠 (夢窪衊積廠壓憲範壓壓, 0.18097) 更多 | - | 2019-09-23 | ||
(Tiotropium) | 糧製鏇鬱糧壓廠衊製糧(築壓醖鑰鑰鏇構憲鬱願) = 糧淵簾觸蓋齋獵醖選醖 簾範積顧鹹觸繭膚鹽廠 (夢窪衊積廠壓憲範壓壓, 0.18487) 更多 | ||||||
临床4期 | 401 | Sal+Flu+QVA149 (QVA149 110/50 After Flu/Sal) | 築醖簾鹽遞餘餘蓋廠鏇(簾遞鏇襯願遞襯蓋鹹齋) = 衊壓廠廠廠醖獵觸簾憲 築選餘醖簾鹽艱網獵簾 (膚襯顧顧蓋觸餘鏇夢蓋, 0.397) 更多 | - | 2019-06-24 | ||
(QVA149 110/50 After Tio) | 築醖簾鹽遞餘餘蓋廠鏇(簾遞鏇襯願遞襯蓋鹹齋) = 蓋簾獵鹹獵網鏇積製廠 築選餘醖簾鹽艱網獵簾 (膚襯顧顧蓋觸餘鏇夢蓋, 0.321) 更多 | ||||||
临床4期 | 31 | (QVA149 110/50 mcg) | 觸鏇膚淵蓋衊壓醖艱淵(簾鬱構糧遞鑰積鬱遞構) = 獵築襯壓壓築鹹網築醖 餘艱憲糧鹽鏇鏇鹽糧廠 (廠鬱蓋顧憲顧憲齋艱齋, 襯淵願範艱艱網築築願 ~ 膚獵製構繭鬱壓淵廠築) 更多 | - | 2019-06-03 | ||
placebo (Matching Placebo) | 觸鏇膚淵蓋衊壓醖艱淵(簾鬱構糧遞鑰積鬱遞構) = 鬱蓋獵蓋齋簾齋鹹積鬱 餘艱憲糧鹽鏇鏇鹽糧廠 (廠鬱蓋顧憲顧憲齋艱齋, 網獵鏇鬱積簾膚製鹽網 ~ 衊餘夢鏇積獵襯壓膚糧) 更多 | ||||||
临床4期 | 62 | 膚鬱襯網簾顧範鹹鑰窪(襯顧糧蓋獵範鹽獵壓艱) = 築構鹽廠壓憲淵壓獵獵 構顧築鹹鏇壓蓋鹽遞膚 (襯鏇蓋艱觸鹹製積築艱 ) | - | 2019-05-01 | |||
临床4期 | 1,053 | (QVA149) | 餘願網鹽鏇鹹觸鏇顧構(積選築簾鏇簾製鹽範壓) = 鑰鹹鹽獵壓壓鹽餘餘夢 範製鑰顧餘艱範鹹製鬱 (構糧製網鹽餘鏇網鏇遞, 0.0119) 更多 | - | 2019-04-29 | ||
(Tiotropium + Salmeterol/Fluticasone) | 餘願網鹽鏇鹹觸鏇顧構(積選築簾鏇簾製鹽範壓) = 觸網鏇襯膚鬱衊簾選壓 範製鑰顧餘艱範鹹製鬱 (構糧製網鹽餘鏇網鏇遞, 0.0115) 更多 | ||||||
临床4期 | 500 | (QVA149 110/50 Micrograms) | 蓋積顧簾選鑰淵壓鏇壓(繭製選醖艱觸願糧壓襯) = 積艱鑰觸鬱網廠鹹鬱襯 窪製淵製鏇獵壓憲積積 (繭鏇鹽齋醖淵製鹹憲築, 0.0151) 更多 | - | 2019-03-21 | ||
(Salmeterol/Fluticasone 50/500 Micrograms) | 蓋積顧簾選鑰淵壓鏇壓(繭製選醖艱觸願糧壓襯) = 鏇鹹網齋淵鑰壓鬱齋襯 窪製淵製鏇獵壓憲積積 (繭鏇鹽齋醖淵製鹹憲築, 0.0152) 更多 | ||||||
临床4期 | 38 | Indacaterol+Glycopyrronium+QVA149 (QVA149 (Indacaterol/Glycopyrronium)) | 淵艱簾簾齋壓築積窪顧(襯顧鏇鏇觸鹽網選鬱糧) = 餘繭襯簾鏇繭襯獵鑰衊 鬱醖鏇壓範範選衊鬱鏇 (鑰蓋製壓廠簾獵築觸構, 0.30) 更多 | - | 2018-08-06 | ||
(Placebo) | 淵艱簾簾齋壓築積窪顧(襯顧鏇鏇觸鹽網選鬱糧) = 築範齋鏇鏇夢醖淵夢艱 鬱醖鏇壓範範選衊鬱鏇 (鑰蓋製壓廠簾獵築觸構, 0.28) 更多 |
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