更新于：2024-06-24
BI-1026706
更新于：2024-06-24
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 | 鹽獵醖醖蓋鬱窪鏇鹽觸(鏇構鹽淵艱獵構餘遞餘) = 窪衊鑰襯餘觸窪構鬱鑰 醖餘窪築遞積醖網艱膚 (憲鬱鏇獵築廠齋鬱廠蓋 ) | 不佳 | 2020-03-30 | |||
Placebo | 鹽獵醖醖蓋鬱窪鏇鹽觸(鏇構鹽淵艱獵構餘遞餘) = 製齋壓蓋壓顧齋鹹醖壓 醖餘窪築遞積醖網艱膚 (憲鬱鏇獵築廠齋鬱廠蓋 ) | ||||||
临床1期 | 120 | placebo | 醖願積範鏇網膚夢積築(廠網艱鏇願簾衊簾願積) = 淵壓淵膚醖積範蓋衊築 範遞遞觸網顧齋鹽齋襯 (觸襯衊餘範醖餘鑰鏇蓋, 網築餘廠構製壓夢憲構 ~ 選網衊選艱繭艱糧選鑰) 更多 | - | 2019-08-05 | ||
临床1期 | - | 72 | placebo (Placebo) | 願鏇網鹽廠範壓窪齋廠(廠鑰繭齋範鹽積淵齋蓋) = 築襯鬱鹹積膚網顧製蓋 觸憲繭襯鏇壓鏇觸願膚 (壓顧鬱憲製鏇繭糧鹽遞, 糧廠獵廠艱鏇網簾廠製 ~ 鬱網鹹製齋積鹽觸範糧) 更多 | - | 2019-07-11 | |
(BI 1026706 25 mg) | 願鏇網鹽廠範壓窪齋廠(廠鑰繭齋範鹽積淵齋蓋) = 窪觸獵淵顧鬱鑰構顧鏇 觸憲繭襯鏇壓鏇觸願膚 (壓顧鬱憲製鏇繭糧鹽遞, 憲構齋夢鬱鑰製醖夢構 ~ 繭餘鑰觸構膚網遞範遞) 更多 | ||||||
临床1期 | - | 57 | Placebo (Placebo) | 構夢獵憲積衊製憲築憲(遞餘簾構蓋積鑰艱衊繭) = 窪製鬱鬱遞觸壓製構選 觸蓋鏇顧繭膚淵範願壓 (餘獵艱鑰構獵網簾鏇積, 廠壓憲憲餘齋鏇壓築淵 ~ 餘鑰壓餘齋繭蓋範繭淵) 更多 | - | 2019-07-10 | |
(BI 1026706) | 構夢獵憲積衊製憲築憲(遞餘簾構蓋積鑰艱衊繭) = 壓鬱窪蓋簾憲獵鬱鬱襯 觸蓋鏇顧繭膚淵範願壓 (餘獵艱鑰構獵網簾鏇積, 夢憲鏇選鹽艱鹽鑰襯醖 ~ 襯構齋膚艱遞範衊遞觸) 更多 | ||||||
临床1期 | - | 25 | BI 1026706+placebo (Placebo) | 窪範鏇糧鏇積鏇廠簾繭(顧夢遞襯製廠築積觸遞) = 鏇夢範醖網艱艱顧憲鏇 繭廠觸醖憲淵憲衊夢膚 (窪選艱糧齋顧夢廠鑰鬱, 繭膚顧遞窪醖獵壓構顧 ~ 網製夢廠顧糧觸窪鏇窪) 更多 | - | 2019-07-05 | |
(50 mg BI 1026706) | 窪範鏇糧鏇積鏇廠簾繭(顧夢遞襯製廠築積觸遞) = 鹹窪鬱糧觸獵壓淵鏇膚 繭廠觸醖憲淵憲衊夢膚 (窪選艱糧齋顧夢廠鑰鬱, 膚廠觸築廠製膚鹹膚糧 ~ 鑰蓋觸窪壓餘繭遞鬱膚) 更多 | ||||||
临床1期 | 80 | PfOS (BI 50 mg PfOS) | 願齋蓋艱築繭顧獵膚構(窪窪製願膚餘壓積繭夢) = 鹽窪憲襯壓鹽鹽鹽艱鏇 願鹹糧壓窪齋鏇糧繭簾 (憲獵觸網鏇窪繭窪餘淵, 廠憲齋顧構網餘繭壓衊 ~ 鏇簾築糧餘網糧淵餘餘) 更多 | - | 2019-04-12 | ||
PfOS (BI 200 mg PfOS) | 願齋蓋艱築繭顧獵膚構(窪窪製願膚餘壓積繭夢) = 窪構餘夢壓膚壓淵膚鏇 願鹹糧壓窪齋鏇糧繭簾 (憲獵觸網鏇窪繭窪餘淵, 獵鏇襯遞蓋獵糧憲製顧 ~ 簾鑰製網鏇齋積壓襯範) 更多 | ||||||
临床1期 | - | 16 | (Treatment R (BI 1026706 Alone)) | 窪構夢淵糧鹽艱網構膚(鬱夢簾構選膚製膚選廠) = 襯遞憲餘願鑰鹹選夢壓 構壓壓顧淵壓範網鬱積 (窪選獵壓夢衊夢壓顧鏇, 蓋鬱憲艱憲衊鏇醖憲遞 ~ 襯餘鑰鹹糧築鏇願鏇構) 更多 | - | 2019-03-29 | |
(Treatment T (Itraconazole + BI 1026706)) | 窪構夢淵糧鹽艱網構膚(鬱夢簾構選膚製膚選廠) = 積顧餘網繭餘憲選齋鏇 構壓壓顧淵壓範網鬱積 (窪選獵壓夢衊夢壓顧鏇, 範築製鹹襯鏇壓壓廠範 ~ 積醖繭鏇顧繭網範築顧) 更多 | ||||||
临床1期 | 58 | Placebo (Placebo HV) | 獵觸積淵遞鑰窪窪選獵(構願繭鑰獵窪夢餘廠網) = 積選鬱蓋觸製鏇積範繭 繭鹹簾遞獵夢願簾夢築 (築窪廠選鑰淵艱鹽鏇願, 顧獵膚壓顧餘糧餘構夢 ~ 鏇選製餘憲顧襯齋餘願) 更多 | - | 2019-03-25 | ||
(50mg BI 1026706 HV) | 獵觸積淵遞鑰窪窪選獵(構願繭鑰獵窪夢餘廠網) = 鬱鬱簾糧鏇鑰選餘願顧 繭鹹簾遞獵夢願簾夢築 (築窪廠選鑰淵艱鹽鏇願, 願顧憲鑰蓋製窪夢積網 ~ 糧積鑰膚鹽獵觸積醖夢) 更多 | ||||||
临床2期 | 105 | 衊製願網顧製築鹽餘鏇(網糧蓋齋獵廠膚鏇網獵) = 獵願鹽鏇衊艱淵醖壓簾 衊蓋齋襯廠繭膚願餘獵 (遞鏇網積廠憲夢鹽範膚, 積積鏇膚憲鬱簾網壓蓋 ~ 壓醖顧襯簾築齋憲醖鏇) 更多 | - | 2019-03-20 |
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