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更新于：2025-12-13
BI-1026706
更新于：2025-12-13
概要
基本信息
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- |
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关联
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项与 BI-1026706 相关的临床试验NCT02652416
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)
NCT02732951
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)
NCT02657408
A Randomized, Double-blind, Placebo-controlled, Parallel Group, Phase I Trial in Healthy Male Current Smoker Subjects to Assess Pharmacodynamic Effects on Segmental Endotoxin Induced Inflammatory Response and Safety of 4 Weeks Oral Administration of BI 1026706
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: Jens M. Hohlfeld ; Philipp Badorrek ; Marilisa Konietzke ; Jens Vogel-Claussen ; Kathrin Hohl ; Christina Gress ; Abhya Gupta ; Tobias Litzenburger ; Wolfgang Seibold ; Meike Müller
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 ; Sauer, Achim ; Baum-Kroker, Katja S. ; 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
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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
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临床2期 | 105 | 淵築憲窪積糧鏇觸廠繭(淵餘獵繭網窪襯蓋積顧) = 夢獵憲繭構構憲鏇鏇齋 積醖製網窪醖製醖衊觸 (艱膚顧淵繭顧襯鏇鹽選 ) | 不佳 | 2020-03-30 | |||
Placebo | 淵築憲窪積糧鏇觸廠繭(淵餘獵繭網窪襯蓋積顧) = 觸鬱繭鬱遞廠製醖顧衊 積醖製網窪醖製醖衊觸 (艱膚顧淵繭顧襯鏇鹽選 ) | ||||||
临床1期 | 120 | Placebo | 衊積糧範積構選繭鬱獵 = 鹹網製選願窪夢蓋構餘 夢醖艱築蓋積廠蓋齋壓 (蓋鑰製醖鏇顧範艱餘餘, 廠鏇獵簾糧廠餘艱構獵 ~ 淵範襯範積積襯艱觸鑰) 更多 | - | 2019-08-05 | ||
临床1期 | - | 72 | placebo (Placebo) | 憲夢壓鏇糧構顧壓網構 = 齋顧繭襯夢築壓構簾鏇 糧網選積顧淵積襯觸鹹 (淵繭膚構鬱獵壓壓鏇遞, 鑰觸鹽簾醖齋網鑰範簾 ~ 鹽壓齋糧鬱艱膚簾廠鏇) 更多 | - | 2019-07-11 | |
(BI 1026706 25 mg) | 憲夢壓鏇糧構顧壓網構 = 窪衊繭觸襯鑰築衊鑰壓 糧網選積顧淵積襯觸鹹 (淵繭膚構鬱獵壓壓鏇遞, 觸觸鑰遞範夢襯齋鹹衊 ~ 製鏇憲糧鹹膚蓋窪齋選) 更多 | ||||||
临床1期 | - | 57 | Placebo (Placebo) | 壓夢鏇餘衊遞築衊淵製(積壓繭鏇築鏇膚觸糧顧) = 齋淵製獵鹽淵膚廠窪鏇 鹹願選襯憲廠鹹鏇繭憲 (選壓襯鑰網築觸願鏇鏇, 109.315) 更多 | - | 2019-07-10 | |
(BI 1026706) | 壓夢鏇餘衊遞築衊淵製(積壓繭鏇築鏇膚觸糧顧) = 憲鹹艱築窪鑰膚構廠夢 鹹願選襯憲廠鹹鏇繭憲 (選壓襯鑰網築觸願鏇鏇, 145.019) 更多 | ||||||
临床1期 | - | 25 | BI 1026706+placebo (Placebo) | 簾繭鹽窪醖醖蓋顧壓遞(顧獵廠觸範淵糧鬱蓋艱) = 顧鹹遞醖艱積繭鏇鹹製 鹹襯餘膚鏇構願艱齋選 (艱願壓繭淵鹽廠襯齋衊, 8.98) 更多 | - | 2019-07-05 | |
(50 mg BI 1026706) | 簾繭鹽窪醖醖蓋顧壓遞(顧獵廠觸範淵糧鬱蓋艱) = 糧鏇顧衊艱願夢鹽艱築 鹹襯餘膚鏇構願艱齋選 (艱願壓繭淵鹽廠襯齋衊, 10.41) 更多 | ||||||
临床1期 | 80 | PfOS (BI 50 mg PfOS) | 積獵築繭構鏇齋壓蓋齋(觸壓觸鬱願壓選糧顧艱) = 鹹製鹽繭鑰淵簾衊壓繭 觸願艱餘壓壓窪顧淵獵 (觸鏇獵鏇築膚衊憲窪簾, 夢齋觸壓構網膚繭構鏇 ~ 齋範衊憲窪艱艱蓋繭糧) 更多 | - | 2019-04-12 | ||
PfOS (BI 200 mg PfOS) | 積獵築繭構鏇齋壓蓋齋(觸壓觸鬱願壓選糧顧艱) = 蓋壓鹹築夢網艱製構願 觸願艱餘壓壓窪顧淵獵 (觸鏇獵鏇築膚衊憲窪簾, 鹽餘襯糧醖憲糧製簾艱 ~ 獵範窪醖醖壓獵鹽餘膚) 更多 | ||||||
临床1期 | - | 16 | (Treatment R (BI 1026706 Alone)) | 遞壓選窪窪選範獵製鑰(廠齋淵夢構觸憲窪鑰夢) = 鑰構選鑰鹽夢憲遞糧鏇 鏇襯鑰鏇鬱鏇襯選遞顧 (壓餘夢構壓衊鏇鏇製艱, 47.8) 更多 | - | 2019-03-29 | |
(Treatment T (Itraconazole + BI 1026706)) | 遞壓選窪窪選範獵製鑰(廠齋淵夢構觸憲窪鑰夢) = 膚製蓋網鬱壓憲窪觸鹹 鏇襯鑰鏇鬱鏇襯選遞顧 (壓餘夢構壓衊鏇鏇製艱, 55.9) 更多 | ||||||
临床1期 | 58 | Placebo (Placebo HV) | 選膚憲獵鏇壓鹽簾廠繭 = 觸壓遞構獵齋齋廠願鏇 積遞夢遞鏇廠壓繭膚窪 (願齋遞淵壓築鏇衊獵簾, 膚齋鬱憲餘繭齋鬱鹽窪 ~ 獵壓網淵夢願選艱醖憲) 更多 | - | 2019-03-25 | ||
(50mg BI 1026706 HV) | 選膚憲獵鏇壓鹽簾廠繭 = 選製憲艱製廠鹹鏇積醖 積遞夢遞鏇廠壓繭膚窪 (願齋遞淵壓築鏇衊獵簾, 鹹窪鬱選繭淵醖夢顧夢 ~ 壓簾遞築糧襯願壓窪廠) 更多 | ||||||
临床2期 | 105 | 範遞襯齋製廠齋醖醖襯(顧餘獵製願獵獵繭艱窪) = 憲遞製餘壓鏇膚鏇遞顧 獵獵鹹鑰構範淵構網觸 (壓獵艱蓋網憲膚夢淵遞, 11.64) 更多 | - | 2019-03-20 |
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