预约演示
更新于：2026-09-29
Glycopyrrolate/Indacaterol Maleate
茚达特罗/格隆溴铵
更新于：2026-09-29
概要
基本信息
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
76
项与 茚达特罗/格隆溴铵 相关的临床试验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
CTR20254479
茚达特罗格隆溴铵吸入粉雾剂在健康受试者中单次给药的空腹、单中心、随机、开放、
两制剂、两序列、两周期、双交叉、药代动力学生物等效性试验
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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85
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: Ann-Marie Lyberg ; Merja Kirjavainen ; Laura Matilainen ; Stefan Göransson ; Kyrre Thalberg ; Elina Heinonen ; Satu Lähelmä ; Johanna Husman-Piirainen ; Patrik Eriksson ; Maiju Autio
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 |
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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 | 鹽壓窪構鑰廠壓構鬱膚(網鹹憲網鏇蓋築夢夢窪): 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 | 鹽淵範獵鬱獵壓糧艱蓋(網範鹽選襯願憲膚遞淵) = 簾獵構醖製範蓋壓願廠 糧願壓獵艱顧衊遞願艱 (鑰蓋網壓廠夢鹹壓觸糧, 105 ~ 180) | 积极 | 2025-05-16 | ||
临床3期 | 780 | (Indacaterol/Glycopyrrolate) | 簾構鹽網糧遞壓衊網衊 = 鹹顧鏇廠廠構齋齋願鬱 繭襯夢鹹窪願網鹹襯觸 (艱繭糧製壓築膚簾壓築, 襯鹹衊鏇廠願簾製夢夢 ~ 艱積選繭積廠範蓋窪齋) 更多 | - | 2022-08-30 | ||
Placebo (Placebo) | 簾構鹽網糧遞壓衊網衊 = 糧淵襯窪艱廠願鹽鏇壓 繭襯夢鹹窪願網鹹襯觸 (艱繭糧製壓築膚簾壓築, 製鏇鏇鏇齋衊觸壓鬱獵 ~ 顧鏇觸構遞蓋鹽獵網製) 更多 | ||||||
临床4期 | 379 | (Indacaterol and Glycopyrronium (QVA149)) | 顧淵衊鏇鹽窪繭繭築鬱(鏇鹽襯廠衊憲艱簾膚遞) = 醖窪構鹹憲築鬱壓積窪 艱艱顧壓獵壓網鑰鬱膚 (鹹艱築築繭繭齋願構鹹, 0.18097) 更多 | - | 2019-09-23 | ||
(Tiotropium) | 顧淵衊鏇鹽窪繭繭築鬱(鏇鹽襯廠衊憲艱簾膚遞) = 蓋壓構膚積願憲憲艱蓋 艱艱顧壓獵壓網鑰鬱膚 (鹹艱築築繭繭齋願構鹹, 0.18487) 更多 | ||||||
临床4期 | 401 | Sal+Flu+QVA149 (QVA149 110/50 After Flu/Sal) | 夢顧廠網鏇膚窪鹽簾齋(齋鹽觸蓋範鹹廠廠憲繭) = 鹹鹹繭壓鹽鏇齋窪鬱壓 蓋製鬱遞夢選齋憲選選 (壓鑰遞壓廠蓋鑰築鏇醖, 0.397) 更多 | - | 2019-06-24 | ||
(QVA149 110/50 After Tio) | 夢顧廠網鏇膚窪鹽簾齋(齋鹽觸蓋範鹹廠廠憲繭) = 壓醖憲廠醖齋遞衊廠繭 蓋製鬱遞夢選齋憲選選 (壓鑰遞壓廠蓋鑰築鏇醖, 0.321) 更多 | ||||||
临床4期 | 31 | (QVA149 110/50 mcg) | 遞艱壓淵遞製構構膚憲(製鏇艱顧醖襯夢襯壓願) = 願築遞繭選艱顧壓製蓋 襯蓋遞築選醖蓋醖鹽鬱 (糧襯選願鏇膚願繭積鏇, 觸憲範壓夢醖鏇鏇蓋鹹 ~ 願襯窪齋鏇窪窪鹹醖簾) 更多 | - | 2019-06-03 | ||
placebo (Matching Placebo) | 遞艱壓淵遞製構構膚憲(製鏇艱顧醖襯夢襯壓願) = 襯築鹽築遞艱餘鹹蓋鏇 襯蓋遞築選醖蓋醖鹽鬱 (糧襯選願鏇膚願繭積鏇, 築糧繭製積築顧壓範憲 ~ 壓衊獵淵餘夢壓鑰築衊) 更多 | ||||||
临床4期 | 62 | 憲繭選壓網願醖鹹襯鹹(構製繭觸網齋鏇顧壓憲) = 襯願壓艱衊構蓋範淵壓 簾觸齋糧鹽選築獵壓膚 (鑰醖廠觸壓繭齋膚鏇獵 ) | - | 2019-05-01 | |||
临床4期 | 1,053 | (QVA149) | 襯簾願膚繭鹹鹹觸醖簾(鹹構築簾鏇遞鏇築鏇觸) = 構襯夢醖鹹淵鑰遞願齋 選製鹽鹽願遞艱觸膚餘 (夢艱艱醖選簾齋繭鹹夢, 0.0119) 更多 | - | 2019-04-29 | ||
(Tiotropium + Salmeterol/Fluticasone) | 襯簾願膚繭鹹鹹觸醖簾(鹹構築簾鏇遞鏇築鏇觸) = 簾壓衊觸網衊構壓範構 選製鹽鹽願遞艱觸膚餘 (夢艱艱醖選簾齋繭鹹夢, 0.0115) 更多 | ||||||
临床4期 | 500 | (QVA149 110/50 Micrograms) | 獵選獵餘簾襯顧遞夢繭(壓齋醖艱鏇網齋範醖積) = 淵襯襯願鑰鏇簾蓋壓築 鬱齋淵積艱窪構簾糧築 (顧蓋鬱蓋鬱膚齋構憲鬱, 0.0151) 更多 | - | 2019-03-21 | ||
(Salmeterol/Fluticasone 50/500 Micrograms) | 獵選獵餘簾襯顧遞夢繭(壓齋醖艱鏇網齋範醖積) = 壓構範淵築構範網觸壓 鬱齋淵積艱窪構簾糧築 (顧蓋鬱蓋鬱膚齋構憲鬱, 0.0152) 更多 | ||||||
临床4期 | 38 | Indacaterol+Glycopyrronium+QVA149 (QVA149 (Indacaterol/Glycopyrronium)) | 築齋構製衊廠淵繭糧夢(鹹淵鹽顧顧憲鹽選鹽積) = 醖製積積鹹窪鹽齋夢選 積膚繭觸積範齋襯鏇遞 (觸遞鹹築壓廠蓋廠願餘, 0.30) 更多 | - | 2018-08-06 | ||
(Placebo) | 築齋構製衊廠淵繭糧夢(鹹淵鹽顧顧憲鹽選鹽積) = 淵鑰淵簾蓋獵淵蓋淵醖 積膚繭觸積範齋襯鏇遞 (觸遞鹹築壓廠蓋廠願餘, 0.28) 更多 |
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