预约演示
更新于：2025-10-11
Lesogaberan
更新于：2025-10-11
概要
基本信息
原研机构 |
在研机构- |
权益机构- |
最高研发阶段无进展临床2期 |
首次获批日期- |
最高研发阶段(中国)- |
特殊审评- |
登录后查看时间轴
结构/序列
分子式C3H9FNO2P |
InChIKeyLJNUIEQATDYXJH-GSVOUGTGSA-N |
CAS号344413-67-8 |
关联
12
项与 Lesogaberan 相关的临床试验EUCTR2014-005074-11-GB
The Role of GABAb receptor mechanisms in cough: Double-blind randomised controlled trial of Lesogaberan in Chronic cough patients with positive and negative symptom association probabilities - GARMIN-II: double-blind randomised controlled trial of lesogaberan in cough
NCT02818309
Efficacy and Safety of Lesogaberan (AZD3355) in Chinese Patients With Reflux Symptoms Refractory to Proton Pump Inhibitor Therapy: a Randomized Placebo-controlled Trial
ISRCTN82391675
The Role of GABAB Receptor Mechanisms in Cough: Effect of Lesogaberan, Baclofen and Placebo on Experimentally Induced Cough Responses in Healthy Controls
100 项与 Lesogaberan 相关的临床结果
登录后查看更多信息
100 项与 Lesogaberan 相关的转化医学
登录后查看更多信息
100 项与 Lesogaberan 相关的专利（医药）
登录后查看更多信息
40
项与 Lesogaberan 相关的文献（医药）2023-08-01EClinicalMedicine
Efficacy and safety of pharmacotherapy for refractory or unexplained chronic cough: a systematic review and network meta-analysis
Article
作者: Chen, Ruchong ; Wu, Tong ; Morice, Alyn ; Xie, Shuojia ; Tang, Kailun ; Lan, Xiaoqing ; Huang, Junfeng ; Li, Shiyue ; Song, Woo-Jung ; Xiang, Ziyuan ; Lin, Zikai ; Zheng, Ziwen
Background:
Refractory chronic cough (RCC) has a significant impact on patient's health-related quality of life and represents a challenge in clinical management. However, the optimal treatment for RCC remains controversial. This study aimed to investigate and compare the efficacy and safety of the current pharmacological therapeutic options for RCC.
Methods:
A systematic review was performed by searching PubMed, Web of Science, Embase, and Ovid databases from January 1, 2008 to March 1, 2023. All randomised control trials (RCTs) reporting outcomes of efficacy or/and safety were included in the Bayesian network meta-analysis. Here, we compared the effects on Leicester Cough Questionnaire (LCQ), Visual Analogue Scale (VAS), and objective cough frequency of patients with RCC. Besides, we also compared the incidence of adverse events (AEs) for analysis of safety. PROSPERO registration: CRD42022345940.
Findings:
19 eligible RCTs included 3326 patients and 7 medication categories: P2X3 antagonist, GABA modulator, Transient Receptor Potential (TRP) modulator, NK-1 agonist, opioid analgesic, macrolide, and sodium cromoglicate. Compared with placebo, mean difference (MD) of LCQ and 24 h cough frequency for P2X3 antagonist relief were 1.637 (95% CI: 0.887-2.387) and -11.042 (P = 0.035). Compared with placebo, effect sizes (MD for LCQ and cough severity VAS) for GABA modulator were 1.347 (P = 0.003) and -7.843 (P = 0.003). In the network meta-analysis, gefapixant is the most effective treatment for patients with RCC (The Surface Under the Cumulative Ranking Curves (SUCRA) is 0.711 in LCQ, 0.983 in 24 h cough frequency, and 0.786 in cough severity VAS). Lesogaberan had better efficacy than placebo (SUCRA: 0.632 vs. 0.472) in 24 h cough frequency. Eliapixant and lesogaberan had better efficacy than placebo in cough severity VAS. However, TRP modulator had worse efficacy than placebo. In the meta-analysis of AEs, the present study found P2X3 antagonist had a significant correlation to AEs (RR: 1.129, 95% CI: 1.012-1.259), especially taste-related AEs (RR: 6.216, P < 0.05).
Interpretation:
In this network meta-analysis, P2X3 antagonist showing advantages in terms of efficacy is currently the most promising medication for treatment of RCC. GABA modulator also showed potential efficacy for RCC but with AEs of the central system. Nevertheless, the role of TRP modulator needed to be revisited. Further research is needed to determine the potential beneficiary population for optimizing the pharmacological management of chronic cough.
Funding:
National Natural Science Foundation of China (81870079), Guangdong Science and Technology Project (2021A050520012), Incubation Program of National Science Foundation for Distinguished Young Scholars (GMU2020-207).
2022-01-01ERJ open research
A double-blind randomised placebo-controlled trial investigating the effects of lesogaberan on the objective cough frequency and capsaicin-evoked coughs in patients with refractory chronic cough
Article
作者: Smith, Jacky A ; Badri, Huda ; Escott, K Jane ; Wilkinson, Greame ; Whorwell, Peter ; Gibbard, Carmen ; Al-Sheklly, Bashar ; Holt, Alison ; Satia, Imran ; Treadway, Sam ; Dockry, Rachel J ; Canning, Brendan J ; Lee, Augustine ; Holt, Kimberley ; McGuiness, Kevin ; Denton, Dimitra ; Lee, Theresa ; Houghton, Lesley
Objective:
Baclofen is a centrally acting γ-aminobutyric acid type B (GABAB) receptor agonist which reduces gastro-oesophageal reflux and suppresses the cough reflex; however, central nervous system side-effects limit its use. Lesogaberan is a novel peripherally acting GABABagonist, but its effects on refractory chronic cough are unknown.
Design:
We performed a single-centre, placebo-controlled, double-blind randomised crossover study in patients with chronic cough, refractory to the treatment of underlying conditions. Patients were randomised to treatment with lesogaberan 120 mg modified release twice daily or matched placebo for 2 weeks and then crossed over to the alternative therapy after a 2-week washout. The primary end-point was 24-h cough frequency measured with an acoustic monitoring system. In addition, cough responses to capsaicin were measured, and gastro-oesophageal reflux assessed by 24-h pH/impedance at screening.
Results:
22 patients were randomised to receive lesogaberan/placebo or placebo/lesogaberan (female (73%); mean±sdage 63.7±7.2 years; median (interquartile range) cough duration 10.5 (5.8–17.0) years; mean (95% CI) 45 (29–67) reflux events in 24 h; two patients had abnormal oesophageal acid exposure times). Although lesogaberan reduced cough counts by 26% over placebo, this did not reach statistical significance (p=0.12). However, lesogaberan did significantly improve cough responses to capsaicin (p=0.04) and the number of cough bouts (p=0.04) compared with placebo. Lesogaberan was well tolerated in this study.
Conclusions:
Lesogaberan improved cough hypersensitivity and the number of bouts of coughing, but not coughs per hour. This implies a possible role for peripheral GABABreceptors in refractory chronic cough.
2021-12-01Pulmonary pharmacology & therapeutics3区 · 医学
Effect of centrally and peripherally acting GABAB agonism on the healthy human cough reflex
3区 · 医学
Article
作者: Satia, Imran ; Badri, Huda ; Escott, Jane ; Dockry, Rachel J ; LGibbard, Carmen ; Wilkinson, Greame ; Holt, Kimberley ; Holt, Alison ; Denton, Dimitra ; Smith, Jacky A ; Canning, Brendan J
BACKGROUND:
Currently there are no effective licensed anti-tussive therapies. Understanding how the neuronal mechanisms mediating the cough reflex in animal models translate to humans is important for the development of effective therapies. Pre-clinical studies suggest that the activation of GABAB receptors in both the peripheral and central nervous systems inhibit cough.
OBJECTIVE:
To compare the effect of central and peripherally acting GABAB agonists (lesogaberan and baclofen) on the cough reflex in healthy volunteers.
METHODS:
We performed a single center, double-blind, double-dummy, three-way crossover trial in healthy controls comparing single doses of lesogaberan (120 mg MR), with baclofen (40 mg) and placebos. Cough responses to inhaled capsaicin were assessed at screening and 2h post-dose on each study day. The primary endpoint was the maximum number of coughs evoked at any concentration of capsaicin (Emax) and the secondary endpoint was the concentration evoking 50% of the maximal response (ED50).
RESULTS:
Fifteen participants enrolled onto the study (median age 29 (IQR 25-44) years; 7 females, mean BMI 24.6(±3.0). Lesogaberan treatment produced a small, statistically significant increase in Emax compared with placebo [mean 13.4coughs (95%CI 10.1-17.9) vs. 11.8coughs (8.8-15.9), p = 0.04], but had no effect on ED50 [geometric mean 47.4 μM (95%CI 24.4-91.7) vs 37.6 μM (95%CI 19.2-73.5), p = 0.37]. In contrast, baclofen had no significant effect on Emax (11.1, 95%CI 8.1-15.4) (p = 0.23), but significantly increased ED50 compared with placebo (geometric mean 75.2 μM (95%CI 37.2-151.8), p = 0.002).
CONCLUSION:
This data suggests the anti-tussive actions of GABAB agonists, in healthy volunteers, occur in the central rather than the peripheral nervous system.
100 项与 Lesogaberan 相关的药物交易
登录后查看更多信息
外链
| KEGG | Wiki | ATC | Drug Bank |
|---|---|---|---|
| - | Lesogaberan | - |
研发状态
10 条进展最快的记录, 后查看更多信息
登录
| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 难治性慢性咳嗽 | 临床2期 | 英国 | 2015-04-16 | |
| 胃灼热 | 临床2期 | 美国 | 2009-10-01 | |
| 胃食管反流 | 临床2期 | 澳大利亚 | 2006-11-01 | |
| 胃食管反流 | 临床2期 | 比利时 | 2006-11-01 | |
| 胃食管反流 | 临床2期 | 法国 | 2006-11-01 | |
| 胃食管反流 | 临床2期 | 德国 | 2006-11-01 | |
| 胃食管反流 | 临床2期 | 匈牙利 | 2006-11-01 | |
| 胃食管反流 | 临床2期 | 荷兰 | 2006-11-01 | |
| 胃食管反流 | 临床2期 | 挪威 | 2006-11-01 | |
| 胃食管反流 | 临床2期 | 罗马尼亚 | 2006-11-01 |
登录后查看更多信息
临床结果
临床结果
适应症
分期
评价
查看全部结果
临床2期 | 661 | 醖觸醖壓鹽鑰遞壓廠鏇(餘鏇網窪醖餘積遞鏇醖) = 網構醖鬱觸餘鏇觸糧鬱 願夢願遞襯積壓鬱積繭 (壓網網淵構選餘醖夢餘 ) | 不佳 | 2013-09-01 | |||
醖觸醖壓鹽鑰遞壓廠鏇(餘鏇網窪醖餘積遞鏇醖) = 襯壓齋獵憲製憲齋積觸 願夢願遞襯積壓鬱積繭 (壓網網淵構選餘醖夢餘 ) | |||||||
临床2期 | 478 | 網鬱築獵夢夢築選鹽衊(壓網艱鑰壓廠簾積艱選) = 簾壓積蓋齋鹹衊構鬱網 蓋廠簾窪鏇網憲蓋衊膚 (醖餘蓋範選壓壓觸網淵, 襯憲觸淵餘觸獵夢糧範 ~ 蓋遞網鹽鏇糧壓壓夢膚) 更多 | - | 2011-06-20 | |||
Placebo+Gelusil® (Placebo) | 網鬱築獵夢夢築選鹽衊(壓網艱鑰壓廠簾積艱選) = 餘廠鹹壓憲選鏇遞餘鬱 蓋廠簾窪鏇網憲蓋衊膚 (醖餘蓋範選壓壓觸網淵, 繭選選選淵襯襯簾憲鹽 ~ 醖蓋願獵願蓋顧顧網獵) 更多 | ||||||
临床2期 | 27 | (AZD3355 30 mg) | 顧艱鹽觸衊憲膚鑰遞艱(構鹽築艱鹽範選膚糧鬱) = 衊積選簾顧範衊製膚蓋 壓糧憲窪願窪醖齋廠鬱 (願衊艱衊壓積製顧選鹹, 網憲積遞衊衊廠積醖膚 ~ 鬱餘淵餘鹹蓋鑰鬱築餘) 更多 | - | 2011-06-14 | ||
(AZD3355 90 mg) | 顧艱鹽觸衊憲膚鑰遞艱(構鹽築艱鹽範選膚糧鬱) = 齋窪鹽構糧製繭夢夢艱 壓糧憲窪願窪醖齋廠鬱 (願衊艱衊壓積製顧選鹹, 襯壓製鹹簾築鏇蓋鏇鑰 ~ 簾鹽簾夢獵鹽衊鑰憲膚) 更多 | ||||||
临床2期 | 27 | (AZD3355) | 齋網憲齋壓鬱遞憲齋網(鹹壓廠壓窪遞艱網顧齋) = 鏇夢餘願窪糧鏇選艱膚 壓淵網艱艱願廠衊醖鹹 (鹹艱糧鑰積觸鬱壓製鏇, 製築餘積窪醖襯衊醖願 ~ 壓鏇鏇淵衊廠衊選憲襯) 更多 | - | 2011-06-10 | ||
placebo (Placebo) | 齋網憲齋壓鬱遞憲齋網(鹹壓廠壓窪遞艱網顧齋) = 鹽遞網壓膚顧鏇顧鏇築 壓淵網艱艱願廠衊醖鹹 (鹹艱糧鑰積觸鬱壓製鏇, 醖淵淵鹹網範淵齋憲夢 ~ 鏇觸蓋鬱獵願鹹簾襯鏇) 更多 | ||||||
临床2期 | 661 | Placebo | 範鏇鑰鬱鏇鹽夢鏇願廠 = 鹽積鏇衊鏇醖積憲齋鬱 憲蓋顧鏇膚構廠襯壓鹹 (獵簾範製積糧窪衊糧鬱, 遞鏇鑰齋範窪衊壓鹽觸 ~ 獵夢獵衊夢襯製鹹觸範) 更多 | - | 2011-04-25 |
登录后查看更多信息
转化医学
使用我们的转化医学数据加速您的研究。
登录
或
药物交易
使用我们的药物交易数据加速您的研究。
登录
或
核心专利
使用我们的核心专利数据促进您的研究。
登录
或
临床分析
紧跟全球注册中心的最新临床试验。
登录
或
批准
利用最新的监管批准信息加速您的研究。
登录
或
特殊审评
只需点击几下即可了解关键药物信息。
登录
或
Eureka LS:
全新生物医药AI Agent 覆盖科研全链路，让突破性发现快人一步
立即开始免费试用!
智慧芽新药情报库是智慧芽专为生命科学人士构建的基于AI的创新药情报平台，助您全方位提升您的研发与决策效率。
立即开始数据试用!
智慧芽新药库数据也通过智慧芽数据服务平台，以API或者数据包形式对外开放，助您更加充分利用智慧芽新药情报信息。
生物序列数据库
生物药研发创新
免费使用
化学结构数据库
小分子化药研发创新
免费使用