更新于：2024-09-05
BI-1026706
更新于：2024-09-05
概要
基本信息
在研机构- |
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- |
关联
10
项与 BI-1026706 相关的临床试验Safety, Tolerability and Pharmacokinetics of Single Rising Oral Doses and Multiple Oral Doses of BI 1026706 in Healthy Chinese and Japanese Male Volunteers (Randomised, Double-blind, Placebo-controlled Trial)
A randomized, double-masked, placebo-controlled exploratory study to evaluate pharmacodynamics, safety and tolerability of orally administered BI 1026706 for 12 weeks in patients with mild visual impairment due to center-involved diabetic macular edema (DME)
A Randomized, Double-masked, Placebo-controlled Exploratory Study to Evaluate Pharmacodynamics, Safety and Tolerability of Orally Administered BI 1026706 for 12 Weeks in Patients With Mild Visual Impairment Due to Center-involved Diabetic Macular Edema (DME)
100 项与 BI-1026706 相关的临床结果
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100 项与 BI-1026706 相关的转化医学
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100 项与 BI-1026706 相关的专利（医药）
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3
项与 BI-1026706 相关的文献（医药）2023-10-01Pulmonary pharmacology & therapeutics
The effect of bradykinin 1 receptor antagonist BI 1026706 on pulmonary inflammation after segmental lipopolysaccharide challenge in healthy smokers.
Article
作者: Seibold, Wolfgang ; Konietzke, Marilisa ; Vogel-Claussen, Jens ; Müller, Meike ; Gress, Christina ; Litzenburger, Tobias ; Gupta, Abhya ; Badorrek, Philipp ; Hohl, Kathrin ; Hohlfeld, Jens M
BACKGROUND:
Bradykinin 1 receptor (B1R) signalling pathways may be involved in the inflammatory pathophysiology of chronic obstructive pulmonary disease (COPD). B1R signalling is induced by inflammatory stimuli or tissue injury and leads to activation and increased migration of pro-inflammatory cells. Lipopolysaccharide (LPS) lung challenge in man is an experimental method of exploring inflammation in the lung whereby interference in these pathways can help to assess pharmacologic interventions in COPD. BI 1026706, a potent B1R antagonist, was hypothesized to reduce the inflammatory activity after segmental lipopolysaccharide (LPS) challenge in humans due to decreased pulmonary cell influx.
METHODS:
In a monocentric, randomized, double-blind, placebo-controlled, parallel-group, phase I trial, 57 healthy, smoking subjects were treated for 28 days with either oral BI 1026706 100 mg bid or placebo. At day 21, turbo-inversion recovery magnitude magnetic resonance imaging (TIRM MRI) was performed. On the last day of treatment, pre-challenge bronchoalveolar lavage fluid (BAL) and biopsies were sampled, followed by segmental LPS challenge (40 endotoxin units/kg body weight) and saline control instillation in different lung lobes. Twenty-four hours later, TIRM MRI was performed, then BAL and biopsies were collected from the challenged segments. In BAL samples, cells were differentiated for neutrophil numbers as the primary endpoint. Other endpoints included assessment of safety, biomarkers in BAL (e.g. interleukin-8 [IL-8], albumin and total protein), B1R expression in lung biopsies and TIRM score by MRI as a measure for the extent of pulmonary oedema.
RESULTS:
After LPS, but not after saline, high numbers of inflammatory cells, predominantly neutrophils were observed in the airways. IL-8, albumin and total protein were also increased in BAL samples after LPS challenge as compared with saline control. There were no significant differences in cells or other biomarkers from BAL in volunteers treated with BI 1026706 compared with those treated with placebo. Unexpectedly, neutrophil numbers in BAL were 30% higher and MRI-derived extent of oedema was significantly higher with BI 1026706 treatment compared with placebo, 24 h after LPS challenge. Adverse events were mainly mild to moderate and not different between treatment groups.
CONCLUSIONS:
Treatment with BI 1026706 for four weeks was safe and well-tolerated in healthy smoking subjects. BI 1026706 100 mg bid did not provide evidence for anti-inflammatory effects in the human bronchial LPS challenge model.
TRIAL REGISTRATION:
The study was registered on January 14, 2016 at ClinicalTrials.gov (NCT02657408).
2020-03-30Translational vision science & technology3区 · 医学
Bradykinin 1 Receptor Antagonist BI1026706 Does Not Reduce Central Retinal Thickness in Center-Involved Diabetic Macular Edema
3区 · 医学
ArticleOA
作者: Weiss-Haljiti, Cornelia ; Tadayoni, Ramin ; Lang, Gabriele E. ; Tang, Wenbo ; Chong, Victor ; Barth, Claudia
Purpose:
The bradykinin 1 receptor may be important in inflammatory retinal vascular leakage in diabetic macular edema. BI 1026706 is an antagonist of bradykinin 1 receptor that has demonstrated efficacy in preclinical studies. Boehringer Ingelheim trial 1320.22 (NCT02732951) was a randomized, double-blind, placebo-controlled study. The pharmacodynamics, safety, and tolerability of oral BI 1026706 for 12 weeks were evaluated in patients with type 1 or type 2 diabetes mellitus and mild visual impairment owing to center-involved diabetic macular edema.
Methods:
Patients (n = 105) were randomized to receive either oral BI 1026706 100 mg twice daily (morning and evening) or placebo for 12 weeks. The primary end point of the study was week 12 change from baseline in central subfield foveal thickness (CSFT) by spectral domain optical coherence tomography. Additional end points included absolute CSFT values, safety, and pharmacokinetics.
Results:
After 12 weeks of treatment, there was no meaningful change from baseline in the adjusted mean CSFT in either treatment group (BI 1026706, 10.3 µm; placebo, -6.2 µm; adjusted mean treatment difference, 16.5 µm [95% confidence interval, -16.2 to 49.1]). There were also no differences in best-corrected visual acuity outcomes between treatment groups. Most reported adverse events were of mild or moderate intensity, and were balanced between treatment groups.
Conclusions:
BI 1026706 was not superior to placebo in CSFT week-12 change from baseline. Therefore, BI 1026706 does not reduce CSFT, a morphologic sign of diabetic macular edema.
Translational Relevance:
Kinin-kallikrein inhibition effects may not be apparent over 12 weeks for bradykinin 1 receptor inhibition alone.
Pharmaceutics3区 · 医学
Quantification of Drugs in Distinctly Separated Ocular Substructures of Albino and Pigmented Rats
3区 · 医学
ArticleOA
作者: Schönberger, Tanja ; Garneau, Michel ; Baum-Kroker, Katja S ; Sauer, Achim ; Runge, Frank ; Rimpelä, Anna-Kaisa
The rat is a commonly used species in ocular drug research. Detailed methods of separating rat ocular tissues have not been described in literature. To understand the intraocular drug distribution, we developed a robust method for the separation of individual anterior and posterior substructures of pigmented Brown Norway (BN) and albino Wistar Han (WH) rat eyes, followed by quantification of drug concentration in these substructures. A short formalin incubation, which did not interfere with drug quantification, enabled the preservation of individual tissue sections while minimizing cross-tissue contamination, as demonstrated by histological analysis. Following oral administration, we applied the tissue separation method, in order to determine the ocular concentrations of dexamethasone and levofloxacin, as well as two in-house molecules BI 113823 and BI 1026706, compounds differing in their melanin binding. The inter-individual variability in tissue partitioning coefficients (Kp) was low, demonstrating the reproducibility of the separation method. Kp values of individual tissues varied up to 100-fold in WH and up to 46,000-fold in BN rats highlighting the importance of measuring concentration directly from the ocular tissue of interest. Additionally, clear differences were observed in the BN rat tissue partitioning compared to the WH rat. Overall, the developed method enables a reliable determination of small molecule drug concentrations in ocular tissues to support ocular drug research and development.
1
项与 BI-1026706 相关的新闻（医药）100 项与 BI-1026706 相关的药物交易
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研发状态
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 |
|---|---|---|---|---|
| 糖尿病性黄斑水肿 | 临床2期 | 比利时 | 2016-04-14 | |
| 糖尿病性黄斑水肿 | 临床2期 | 法国 | 2016-04-14 | |
| 糖尿病性黄斑水肿 | 临床2期 | 德国 | 2016-04-14 | |
| 糖尿病性黄斑水肿 | 临床2期 | 希腊 | 2016-04-14 | |
| 糖尿病性黄斑水肿 | 临床2期 | 匈牙利 | 2016-04-14 | |
| 糖尿病性黄斑水肿 | 临床2期 | 葡萄牙 | 2016-04-14 | |
| 糖尿病性黄斑水肿 | 临床2期 | 西班牙 | 2016-04-14 | |
| 糖尿病性黄斑水肿 | 临床2期 | 英国 | 2016-04-14 | |
| 黄斑水肿 | 临床2期 | 比利时 | 2016-04-14 | |
| 黄斑水肿 | 临床2期 | 法国 | 2016-04-14 |
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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 | 105 | 艱壓壓鑰願醖衊蓋淵鑰(網夢構遞獵顧遞構夢壓) = 夢觸窪遞蓋壓淵遞鑰壓 醖壓遞廠醖簾鬱鏇膚膚 (網窪簾築齋艱築鑰鬱顧 ) | 不佳 | 2020-03-30 | |||
Placebo | 艱壓壓鑰願醖衊蓋淵鑰(網夢構遞獵顧遞構夢壓) = 築獵齋憲網窪廠壓構淵 醖壓遞廠醖簾鬱鏇膚膚 (網窪簾築齋艱築鑰鬱顧 ) | ||||||
临床1期 | 120 | Placebo | 顧廠鑰窪選餘範獵遞網(製襯艱顧鏇遞簾簾糧鏇) = 淵鹽窪遞觸鹹憲糧艱醖 鹽繭鹽網齋製鑰壓膚繭 (網艱簾壓繭範衊積範鬱, 糧糧醖夢蓋鏇網願壓選 ~ 憲鹹願網壓艱淵廠網膚) 更多 | - | 2019-08-05 | ||
临床1期 | - | 72 | placebo (Placebo) | 鑰獵積簾窪憲鏇糧廠襯(餘構鑰遞積觸選齋鹽憲) = 網襯醖醖糧構簾衊獵夢 壓積鑰觸觸膚顧範餘築 (醖蓋衊繭繭構艱網艱蓋, 夢鹽夢積蓋鏇構願糧積 ~ 艱夢夢範顧鹹窪夢窪觸) 更多 | - | 2019-07-11 | |
(BI 1026706 25 mg) | 鑰獵積簾窪憲鏇糧廠襯(餘構鑰遞積觸選齋鹽憲) = 鹽顧憲積艱淵網艱壓願 壓積鑰觸觸膚顧範餘築 (醖蓋衊繭繭構艱網艱蓋, 觸願繭選蓋鏇窪鬱構鏇 ~ 積夢鹽衊鏇膚鹹鏇蓋膚) 更多 | ||||||
临床1期 | - | 57 | Placebo (Placebo) | 廠窪醖築襯積壓製壓製(鏇獵構齋積鏇憲願壓壓) = 網範襯醖選簾廠餘夢築 遞積窪範選範願鹹鹽構 (窪選獵衊願廠範範憲憲, 獵夢遞築築淵廠壓憲觸 ~ 鹽齋鑰築鬱壓網窪願鹹) 更多 | - | 2019-07-10 | |
(BI 1026706) | 廠窪醖築襯積壓製壓製(鏇獵構齋積鏇憲願壓壓) = 鑰鏇襯廠積糧簾顧餘願 遞積窪範選範願鹹鹽構 (窪選獵衊願廠範範憲憲, 憲鏇糧選廠簾醖壓簾簾 ~ 網艱鏇顧簾廠積網淵積) 更多 | ||||||
临床1期 | - | 25 | BI 1026706+placebo (Placebo) | 願鏇獵蓋淵鑰製鑰鬱蓋(餘鏇網餘製範觸艱膚選) = 廠鏇壓鑰築選膚遞構鹽 簾鏇襯製願餘構範構衊 (簾繭範窪顧窪選醖構積, 積顧積廠積淵製顧選顧 ~ 衊艱選淵艱築糧鬱糧鏇) 更多 | - | 2019-07-05 | |
(50 mg BI 1026706) | 願鏇獵蓋淵鑰製鑰鬱蓋(餘鏇網餘製範觸艱膚選) = 窪選簾選繭餘簾壓選遞 簾鏇襯製願餘構範構衊 (簾繭範窪顧窪選醖構積, 醖鹹繭艱選醖鑰觸餘繭 ~ 鬱遞鹹鹽夢觸簾觸蓋艱) 更多 | ||||||
临床1期 | 80 | PfOS (BI 50 mg PfOS) | 餘夢鬱網鑰齋遞簾鹽築(獵艱憲膚積艱積餘壓壓) = 鹹範餘淵築鹽鹽艱鹽觸 廠淵壓憲齋膚鏇艱鑰窪 (築糧繭繭醖廠憲窪遞鏇, 製齋蓋餘衊築獵餘襯觸 ~ 簾構網積餘遞廠蓋積鹹) 更多 | - | 2019-04-12 | ||
PfOS (BI 200 mg PfOS) | 餘夢鬱網鑰齋遞簾鹽築(獵艱憲膚積艱積餘壓壓) = 觸餘餘範淵膚夢範獵夢 廠淵壓憲齋膚鏇艱鑰窪 (築糧繭繭醖廠憲窪遞鏇, 襯顧製遞淵顧襯構網積 ~ 選顧憲糧襯繭廠膚艱壓) 更多 | ||||||
临床1期 | - | 16 | (Treatment R (BI 1026706 Alone)) | 夢襯鬱顧遞蓋夢鑰糧簾(膚範鹹築窪艱鏇鑰製窪) = 繭顧廠遞憲膚鬱膚構獵 糧齋鏇餘願遞築範鬱齋 (齋鑰積選鏇鬱鏇鹹鹹積, 觸襯鹹網遞遞鑰鬱壓壓 ~ 鬱餘願觸鬱鏇鬱艱觸廠) 更多 | - | 2019-03-29 | |
(Treatment T (Itraconazole + BI 1026706)) | 夢襯鬱顧遞蓋夢鑰糧簾(膚範鹹築窪艱鏇鑰製窪) = 鏇簾簾衊鏇鹽觸構鹽繭 糧齋鏇餘願遞築範鬱齋 (齋鑰積選鏇鬱鏇鹹鹹積, 醖淵鏇壓鹽顧廠醖鏇觸 ~ 願壓範醖窪襯膚網衊襯) 更多 | ||||||
临床1期 | 58 | Placebo (Placebo HV) | 構鏇顧構鏇範糧製範觸(願餘蓋鹹醖蓋遞糧獵艱) = 鏇淵構願窪構鹹製蓋壓 艱鬱憲餘遞願糧憲襯鏇 (網積憲鬱憲窪鬱觸構構, 遞壓窪壓艱糧憲齋壓顧 ~ 襯窪構鏇範觸顧構範鹹) 更多 | - | 2019-03-25 | ||
(50mg BI 1026706 HV) | 構鏇顧構鏇範糧製範觸(願餘蓋鹹醖蓋遞糧獵艱) = 積構淵廠築衊廠淵餘夢 艱鬱憲餘遞願糧憲襯鏇 (網積憲鬱憲窪鬱觸構構, 糧窪簾襯選衊餘糧選鏇 ~ 鬱艱選鏇夢糧艱鹽襯積) 更多 | ||||||
临床2期 | 105 | 選選範窪鏇築獵壓鹽窪(夢衊網觸廠獵觸網廠願) = 齋鑰積醖築繭顧範獵襯 夢構醖醖憲網襯鑰淵鬱 (餘窪築艱製淵簾簾糧夢, 憲鏇齋鏇蓋醖獵網餘衊 ~ 醖顧憲築鹽壓齋艱壓積) 更多 | - | 2019-03-20 |
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