预约演示
更新于：2025-04-17
Tafluprost/Timolol Maleate
他氟前列腺素/马来酸噻吗洛尔
更新于：2025-04-17
概要
基本信息
药物类型 小分子化药 |
别名 Tafluprost/timolol、Tapcom-S、Taptiqom + [12] |
作用方式 激动剂、拮抗剂 |
作用机制 PTGFR激动剂(前列腺素FP受体激动剂)、β-adrenoceptors拮抗剂(β-肾上腺素能受体家族拮抗剂) |
治疗领域 |
非在研适应症- |
在研机构 |
最高研发阶段批准上市 |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构/序列
分子式C17H28N4O7S |
InChIKeyWLRMANUAADYWEA-NWASOUNVSA-N |
CAS号26921-17-5 |
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关联
16
项与 他氟前列腺素/马来酸噻吗洛尔 相关的临床试验NCT04828057
Preservative-free Fixed-dose Combination of Tafluprost 0.0015% / Timolol 0.5% in Patients With Open-angle Glaucoma or Ocular Hypertension: Clinical Effectiveness, Tolerability and Safety in a Real World Setting
NCT04489810
GlutDigest - Enzymes-assisted Gluten Digestion
NCT04489836
GlutDigest - Enzymes-assisted Gluten Digestion (Pilot Study)
100 项与 他氟前列腺素/马来酸噻吗洛尔 相关的临床结果
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100 项与 他氟前列腺素/马来酸噻吗洛尔 相关的转化医学
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100 项与 他氟前列腺素/马来酸噻吗洛尔 相关的专利（医药）
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12
项与 他氟前列腺素/马来酸噻吗洛尔 相关的文献（医药）2024-12-03Beneficial Microbes
Bacillus subtilis DE111 partially reverses endothelial dysfunction in western-diet fed mice
Article
作者: Brown, G.D. ; Wei, Y. ; Stark, G.C. ; Graham, E.L. ; Risk, B.D. ; Gentile, C.L. ; Weir, T.L. ; Zhang, M.
Abstract:
Imbalances in the gut microbiome have emerged as an important factor in endothelial dysfunction, a significant risk factor for cardiovascular disease. Thus, interventions targeting the microbiome may prove helpful in preventing or reversing this impairment. We previously reported that spore-forming Bacillus subtilis DE111 improved endothelial function in a cohort of healthy, non-obese humans after a four-week intervention. Building on these promising results, the present study sought to investigate whether administering B. subtilis DE111 could reverse endothelial dysfunction in mice with diet-induced obesity. Male C57BL/6J mice were fed a Western diet (WD; n = 24) or standard diet (SD; n = 24) for ten weeks to induce endothelial dysfunction, after which half of the animals in each group (n = 12) were allocated to receive B. subtilis DE111 (hereafter, PB) formulated into the diet for an additional eight weeks. Outcomes included endothelial-dependent arterial dilation, glucose tolerance, body weight changes, microbiota profiles, and assessments of intestinal permeability and mucosal immunity markers. Furthermore, a cell culture model of gut barrier function was used to assess the effects of PB on gut barrier integrity. PB treatment significantly attenuated WD-induced mesenteric endothelial-dependent arterial dilation, independent of changes in other cardiometabolic parameters or changes in gut barrier function. In vitro trans-epithelial electrical resistance of the Caco-2 cell culture confirmed that neither PB-conditioned media nor faecal waters from B. subtilis-treated human stool resulted in gut barrier improvements, nor did they protect against inflammation-associated barrier disruptions. Unsurprisingly, microbiota analysis revealed significant differences in Shannon’s alpha diversity of WD-fed animals compared to SD. These data suggest that PB consumption significantly attenuated WD diet-induced endothelial dysfunction; however, the underlying mechanisms of this protection were not determined. Improvement in endothelial function was independent of PB-mediated changes to body weight or gut barrier function. Further studies should explore B. subtilis-mediated immune responses or metabolite production as mechanisms underlying these endothelial protective effects.
2023-02-23Beneficial microbes
Acute physiological effects following Bacillus subtilis DE111 oral ingestion – a randomised, double blinded, placebo-controlled study
Article
作者: Khokhlova, E. ; Buckley, M. ; Phipps, C. ; Mazhar, S. ; Colom, J. ; Brodkorb, A. ; Simon, A. ; Rea, K. ; Freitas, D. ; Deaton, J.
Previous studies using ileostomy samples from study participants demonstrated that the spore-forming probiotic Bacillus subtilis DE111® can germinate in the small intestine as early as 4 hours after ingestion. Metabolomics, proteomics and sequencing technologies, enabled further analysis of these samples for the presence of hypoglycaemic, hypolipidemic, antioxidant, anti-inflammatory and antihypertensive molecules. In the DE111 treatment group, the polyphenols trigonelline and 2,5-dihydroxybenzoic acid, orotic acid, the non-essential amino acid cystine and the lipokine 12,13-diHome were increased. DE111 also reduced acetylcholine levels in the ileostomy samples, and increased the expression of leucocyte recruiting proteins, antimicrobial peptides and intestinal alkaline phosphatases of the brush border in the small intestine. The combination of B. subtilis DE111 and the diet administered during the study increased the expression of the proteins phosphodiesterase ENPP7, ceramidase ASAH2 and the adipokine Zn-alpha-2-glycoprotein that are involved in fatty acid and lipid metabolism. Acute B. subtilis DE111 ingestion had limited detectable effect on the microbiome, with the main change being its increased presence. These findings support previous data suggesting a beneficial role of DE111 in digestion, metabolism, and immune health that appears to begin within hours of consumption.
2022-05-01FASEB JOURNAL
RETRACTED: Bacillus Subtilis DE111 Improves Endothelial Dependent Vascular Dilation in Mice Fed a Western Diet
Article
作者: Risk, Briana D.
Vascular dysfunction often precedes the development of cardiovascular disease in which data from our lab and others suggest a role of the gut microbiome in the development of this defect. In a pilot study of healthy humans, we observed that the spore‐based probiotic, Bacillus Subtilis DE111(DE111), improved reactive hyperemia index (RHI) scores, indicating improved vascular dilation. To further explore whether DE111 impacts cardiovascular function, the current study examined its efficacy in a diet‐induced obesity model in mice. Male C57/BJ mice were fed a standard diet (SD; n=24) or Western diet (WD; n=24) for 8 weeks to induce vascular dysfunction and were then further divided such that (n=12) half of the animals on each diet received 1billion colony forming units per day (CFU/d) of DE111. Weekly body weight was measured until termination at 6 months of age. WD and WD+DE111 mice exhibited similar increases in body weight (SD: 31.2±2.3 vs WD: 47.4±3.3 and WD+DE111: 45.7±4.0) and impairments in glucose tolerance compared to SD mice (SD: 237.1±68.0 vs WD: 410±26.9 and WD+DE111: 460±116.8, p<0.05). A 28% decrease in vessel dilation was observed with mice on a WD as compared to mice on a SD after addition of the endothelial‐dependent dilator acetylcholine (AUC, 918.3±49.25, p<0.05). However, the addition of DE111 improved endothelial mediated vessel dilation in mice fed a WD+DE111 (AUC, 991.7±47.9, p<0.05). This increase was observed independent of body weight changes and improvement in glucose tolerance. In conclusion, the addition of DE111 increased endothelial‐dependent dilation in mice fed a WD. Further analyses are underway to establish the mechanisms of this gut‐vasculature crosstalk, but our animal and human studies both suggest that the novel probiotic, DE111 may support cardiovascular health.
100 项与 他氟前列腺素/马来酸噻吗洛尔 相关的药物交易
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外链
| KEGG | Wiki | ATC | Drug Bank |
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研发状态
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 |
|---|---|---|---|
| 开角型青光眼 | 中国 | 2025-03-25 | |
| 青光眼 | 日本 | 2013-09-20 | |
| 高眼压症 | 日本 | 2013-09-20 |
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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4期 | 42 | Preserved latanoprost | 鹽觸製壓鑰簾壓製鬱憲(淵艱壓膚餘鑰衊衊鑰鬱) = Hyperemia was more common with preserved latanoprost (21.4 vs. 7.1%; P = 0.031) 艱簾憲觸齋蓋壓遞憲糧 (獵範範淵鏇製襯鏇襯鹽 ) | - | 2018-12-01 | ||
N/A | 1,157 | 築繭鬱醖構構鏇製醖繭(醖窪夢鏇鏇鏇齋製鑰鹹) = few adverse events 築積積鹹願遞繭範壓襯 (鑰襯觸衊顧遞構觸襯膚 ) | 积极 | 2016-10-16 | |||
N/A | - | - | Taf/T FDC | 範餘壓襯糧齋繭鹹醖艱(願獵遞膚艱製願餘簾衊) = 願膚顧鏇糧製艱襯簾鹽 艱獵廠糧顧夢蓋窪糧構 (蓋範壓齋壓衊製淵繭廠 ) 更多 | - | 2015-06-01 | |
Lat/T FDC | 範餘壓襯糧齋繭鹹醖艱(願獵遞膚艱製願餘簾衊) = 餘淵選鬱範壓顧憲鹽衊 艱獵廠糧顧夢蓋窪糧構 (蓋範壓齋壓衊製淵繭廠 ) 更多 | ||||||
临床3期 | 166 | Placebo+DE-111 (DE-111) | 齋壓夢廠壓齋壓築鹹蓋(遞鬱鹹範蓋鏇顧繭糧鏇) = 遞選繭淵範繭築網鹹獵 顧積醖艱齋窪簾獵膚蓋 (選醖壓壓餘範襯窪製顧, 2.1) 更多 | - | 2015-05-15 | ||
(Timolol) | 齋壓夢廠壓齋壓築鹹蓋(遞鬱鹹範蓋鏇顧繭糧鏇) = 齋膚糧網鬱選簾構憲選 顧積醖艱齋窪簾獵膚蓋 (選醖壓壓餘範襯窪製顧, 2.1) 更多 | ||||||
临床3期 | 489 | Placebo+DE-111 (DE-111) | 壓鑰繭齋襯範糧簾積繭(蓋壓襯淵壓構淵鬱鏇艱) = 遞範獵觸範窪鹽鏇選餘 範網壓衊鏇憲襯觸糧廠 (遞夢構構構選齋鏇鹽構, 1.8) 更多 | - | 2015-05-14 | ||
(Tafluprost) | 壓鑰繭齋襯範糧簾積繭(蓋壓襯淵壓構淵鬱鏇艱) = 壓糧淵餘鹽膚窪範壓簾 範網壓衊鏇憲襯觸糧廠 (遞夢構構構選齋鏇鹽構, 1.7) 更多 | ||||||
临床3期 | 148 | Timolol+Tafluprost+DE-111 | 鏇窪淵醖壓窪齋遞願蓋(選淵積鹽獵築膚願構觸) = 遞範觸壓窪製蓋繭齋鏇 憲夢觸夢醖壓鬱襯齋遞 (遞簾壓鹽簾蓋齋鬱鬱膚, 2.2) 更多 | - | 2015-05-14 |
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