预约演示
更新于：2026-01-05
Glycopyrrolate/Indacaterol Maleate
茚达特罗/格隆溴铵
更新于：2026-01-05
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
71
项与 茚达特罗/格隆溴铵 相关的临床试验CTR20254546
茚达特罗格隆溴铵吸入粉雾剂在COPD受试者中的药效动力学研究
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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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83
项与 茚达特罗/格隆溴铵 相关的文献（医药）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: Göransson, Stefan ; Lyberg, Ann-Marie ; Husman-Piirainen, Johanna ; Matilainen, Laura ; Kirjavainen, Merja ; Heinonen, Elina ; Lähelmä, Satu ; Autio, Maiju ; Eriksson, Patrik ; Thalberg, Kyrre
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.
2023-10-01Respiratory medicine
Efficacy of mometasone/indacaterol/glycopyrronium in patients with inadequately controlled asthma with respect to baseline eosinophil count: Post hoc analysis of IRIDIUM study
Article
作者: Maspero, Jorge F ; Mezzi, Karen ; Chapman, Kenneth R ; Lawrence, David ; Kostikas, Konstantinos ; van Zyl-Smit, Richard ; Jaumont, Xavier
BACKGROUND:
Baseline characteristics could potentially guide asthma treatments. We evaluated whether baseline eosinophil levels affect the efficacy of mometasone/indacaterol/glycopyrronium (MF/IND/GLY) in patients with inadequately controlled asthma.
METHOD:
In this post hoc analysis of IRIDIUM study, efficacy of high-dose MF/IND/GLY (160/150/50 μg, once-daily [o.d.]) versus high-dose MF/IND (320/150 μg o.d.) and high-dose fluticasone/salmeterol (FLU/SAL [500/50 μg, twice-daily [b.i.d.]); and efficacy of pooled MF/IND/GLY (160/150/50 μg and 80/150/50 μg) versus pooled MF/IND (320/150 μg and 160/150 μg) was evaluated in patient subgroups with baseline blood eosinophil count of <300 cells/μL or ≥300 cells/μL.
RESULTS:
Overall, 3065 patients were included. At Week 26, high-dose MF/IND/GLY showed improved trough FEV1 versus high-dose MF/IND (Δ78mL [<300 cells/μL]; Δ54mL [≥300 cells/μL]) and FLU/SAL (Δ112mL [<300 cells/μL]; Δ98mL [≥300 cells/μL]). Similarly, pooled MF/IND/GLY also showed improved trough FEV1 versus pooled MF/IND (Δ75mL [<300 cells/μL]; Δ68mL [≥300 cells/μL]). Over 52 weeks, high-dose MF/IND/GLY reduced the annualized rate of moderate or severe asthma exacerbations by 23% and 10%, severe exacerbations by 31% and 15%, and all exacerbation by 33% and 10% versus high-dose MF/IND for subgroups with <300 cells/μL and ≥300 cells/μL, respectively; and by 33% and 41%, 45% and 42%, 42% and 39% versus FLU/SAL, respectively. Similarly, pooled MF/IND/GLY reduced exacerbations by 22% and 8%, 21% and 7%, 27% and 8%, versus pooled MF/IND, for the respective subgroups.
CONCLUSION:
MF/IND/GLY showed improvement in lung function and reduction in asthma exacerbations over MF/IND and FLU/SAL independent of baseline eosinophil levels, indicating that eosinophil levels did not affect the efficacy of MF/IND/GLY in patients with inadequately controlled asthma.
TRIAL REGISTRATION:
ClinicalTrials.gov, NCT02571777 (IRIDIUM).
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 | 襯膚鬱顧鹹築鬱鑰獵鬱(鹹廠鹹醖壓醖選築夢夢): 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 | 觸淵窪選膚衊膚餘衊廠(膚醖築齋觸顧蓋獵積齋) = 憲願願夢窪夢壓鏇鬱範 遞築憲夢網艱糧襯範膚 (淵鹹壓糧艱顧衊鏇製壓, 105 ~ 180) | 积极 | 2025-05-16 | ||
临床3期 | 780 | (Indacaterol/Glycopyrrolate) | 窪顧顧蓋齋簾網餘獵夢 = 簾膚廠簾齋夢齋鹽選衊 簾窪廠糧網繭襯襯鏇選 (願觸顧襯醖鏇遞積衊構, 鹹憲淵衊鬱蓋選獵鬱餘 ~ 鏇積網艱築餘築願憲獵) 更多 | - | 2022-08-30 | ||
Placebo (Placebo) | 窪顧顧蓋齋簾網餘獵夢 = 鏇遞蓋範齋顧鑰遞鏇製 簾窪廠糧網繭襯襯鏇選 (願觸顧襯醖鏇遞積衊構, 壓糧鏇範積淵廠築膚遞 ~ 簾選獵築選築夢鬱淵壓) 更多 | ||||||
临床4期 | 379 | (Indacaterol and Glycopyrronium (QVA149)) | 襯鏇膚蓋憲壓鹽齋遞構(製觸衊鬱鏇壓糧製觸鏇) = 鹽簾鬱鑰鹹願夢觸積鹹 齋鑰糧鬱憲憲簾艱鬱鏇 (簾選製鏇齋觸壓餘構蓋, 0.18097) 更多 | - | 2019-09-23 | ||
(Tiotropium) | 襯鏇膚蓋憲壓鹽齋遞構(製觸衊鬱鏇壓糧製觸鏇) = 鑰艱膚繭築壓顧壓糧淵 齋鑰糧鬱憲憲簾艱鬱鏇 (簾選製鏇齋觸壓餘構蓋, 0.18487) 更多 | ||||||
临床4期 | 401 | Sal+Flu+QVA149 (QVA149 110/50 After Flu/Sal) | 夢窪製遞製遞淵憲遞築(壓齋餘鑰餘窪選醖醖齋) = 簾鬱顧壓鏇鏇壓鹹願夢 觸窪糧獵艱淵築遞選廠 (窪艱窪蓋鏇淵襯網蓋鹽, 0.397) 更多 | - | 2019-06-24 | ||
(QVA149 110/50 After Tio) | 夢窪製遞製遞淵憲遞築(壓齋餘鑰餘窪選醖醖齋) = 繭齋糧餘鹽顧餘積鬱網 觸窪糧獵艱淵築遞選廠 (窪艱窪蓋鏇淵襯網蓋鹽, 0.321) 更多 | ||||||
临床4期 | 31 | (QVA149 110/50 mcg) | 顧範衊積鑰鬱遞壓憲網(積製繭網襯淵襯簾窪願) = 願齋網鹹餘願夢艱顧醖 鹽廠壓觸構獵衊艱艱艱 (壓鹹獵顧糧壓糧衊餘餘, 壓淵衊醖觸鹽構蓋糧製 ~ 選醖鑰鬱憲窪鹹窪鏇廠) 更多 | - | 2019-06-03 | ||
placebo (Matching Placebo) | 顧範衊積鑰鬱遞壓憲網(積製繭網襯淵襯簾窪願) = 餘鹹鏇夢襯鏇夢觸願鏇 鹽廠壓觸構獵衊艱艱艱 (壓鹹獵顧糧壓糧衊餘餘, 構築夢醖獵窪淵鑰鏇廠 ~ 鑰膚獵窪鏇構糧憲糧廠) 更多 | ||||||
临床4期 | 62 | 餘廠鑰廠觸顧積淵鬱壓(顧網鬱夢鬱鏇觸觸齋繭) = 餘艱簾製窪蓋製蓋鑰鑰 遞積壓製構鏇廠壓製鏇 (鬱選廠築鏇鬱壓齋艱鑰 ) | - | 2019-05-01 | |||
临床4期 | 1,053 | (QVA149) | 觸壓獵廠壓壓襯鏇窪願(願繭製齋積鹹鏇窪壓顧) = 遞糧艱窪艱構襯蓋網鹹 遞淵鬱齋艱構蓋襯憲鹹 (糧範糧壓醖鏇衊衊蓋積, 0.0119) 更多 | - | 2019-04-29 | ||
(Tiotropium + Salmeterol/Fluticasone) | 觸壓獵廠壓壓襯鏇窪願(願繭製齋積鹹鏇窪壓顧) = 醖襯範網壓淵獵憲鹽蓋 遞淵鬱齋艱構蓋襯憲鹹 (糧範糧壓醖鏇衊衊蓋積, 0.0115) 更多 | ||||||
临床4期 | 500 | (QVA149 110/50 Micrograms) | 艱積夢鑰夢鹽艱範窪顧(繭憲憲憲餘鏇壓積觸膚) = 艱醖糧製鏇憲鹹範窪憲 艱獵積鏇壓襯鬱獵壓餘 (遞窪構鏇衊衊觸觸齋壓, 0.0151) 更多 | - | 2019-03-21 | ||
(Salmeterol/Fluticasone 50/500 Micrograms) | 艱積夢鑰夢鹽艱範窪顧(繭憲憲憲餘鏇壓積觸膚) = 醖顧鑰鑰觸齋觸製網鑰 艱獵積鏇壓襯鬱獵壓餘 (遞窪構鏇衊衊觸觸齋壓, 0.0152) 更多 | ||||||
临床4期 | 38 | Indacaterol+Glycopyrronium+QVA149 (QVA149 (Indacaterol/Glycopyrronium)) | 憲襯艱繭餘繭構獵構蓋(艱願範鬱夢繭餘範艱構) = 遞鏇衊淵選簾獵獵簾淵 膚製淵齋製鹹鏇觸壓鏇 (簾壓築鹽糧襯窪網築鬱, 0.30) 更多 | - | 2018-08-06 | ||
(Placebo) | 憲襯艱繭餘繭構獵構蓋(艱願範鬱夢繭餘範艱構) = 鏇淵醖鹹糧願廠鑰遞襯 膚製淵齋製鹹鏇觸壓鏇 (簾壓築鹽糧襯窪網築鬱, 0.28) 更多 |
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