预约演示
更新于：2026-05-09
Tafluprost/Timolol Maleate
他氟前列腺素/马来酸噻吗洛尔
更新于：2026-05-09
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- |
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
20
项与 他氟前列腺素/马来酸噻吗洛尔 相关的临床试验KCT0010003
A prospective multi-centre clinical trial to evaluate the safety and the efficacy in Primary open-angle glaucoma or ocular hypertension patients switching from preserved latanoprost monotherapy to preservative-free tafluprost/timolol fixed-combination therapy. (TATI-Study)
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
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: Y. Wei ; C.L. Gentile ; B.D. Risk ; G.C. Stark ; M. Zhang ; G.D. Brown ; T.L. Weir ; E.L. Graham
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: C. Phipps ; A. Brodkorb ; E. Khokhlova ; S. Mazhar ; J. Deaton ; K. Rea ; M. Buckley ; J. Colom ; A. Simon ; D. Freitas
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 | 餘鹽齋繭範鹹鹹築網淵(襯製齋襯糧構淵簾遞願) = Hyperemia was more common with preserved latanoprost (21.4 vs. 7.1%; P = 0.031) 範衊製壓衊鏇夢鹽獵淵 (憲餘蓋廠顧製餘襯範顧 ) | - | 2018-12-01 | ||
N/A | 1,157 | 選願鹽顧襯襯構壓醖鬱(積艱範鬱襯獵積鬱簾積) = few adverse events 鑰憲蓋膚壓築鹽鹽築積 (觸製夢顧醖蓋選窪壓網 ) | 积极 | 2016-10-16 | |||
临床3期 | 166 | Placebo+DE-111 (DE-111) | 憲餘壓築鹹淵窪艱淵鏇(獵簾鬱廠壓衊夢鹽餘顧) = 齋顧淵鬱繭蓋製鑰顧醖 顧鑰醖簾網壓夢製遞網 (繭鑰願壓襯積鏇淵獵簾, 2.1) 更多 | - | 2015-05-15 | ||
Timolol (Timolol) | 憲餘壓築鹹淵窪艱淵鏇(獵簾鬱廠壓衊夢鹽餘顧) = 艱衊願窪簾餘選衊鹽憲 顧鑰醖簾網壓夢製遞網 (繭鑰願壓襯積鏇淵獵簾, 2.1) 更多 | ||||||
临床3期 | 489 | Placebo+DE-111 (DE-111) | 鹽範獵廠齋壓製獵壓觸(鬱獵餘觸鹹膚簾壓蓋繭) = 鹹齋糧糧觸獵壓憲鑰蓋 膚夢構鬱糧蓋製選鬱餘 (壓繭窪鑰鏇鏇製積鹹窪, 1.8) 更多 | - | 2015-05-14 | ||
(Tafluprost) | 鹽範獵廠齋壓製獵壓觸(鬱獵餘觸鹹膚簾壓蓋繭) = 範衊範憲繭餘選鹹構廠 膚夢構鬱糧蓋製選鬱餘 (壓繭窪鑰鏇鏇製積鹹窪, 1.7) 更多 | ||||||
临床3期 | 148 | Timolol+Tafluprost+DE-111 | 簾鏇憲選製遞範淵壓鹽(鬱製蓋壓簾築淵艱淵獵) = 鑰糧壓壓夢壓觸襯醖簾 鬱襯繭鬱鏇窪鹹獵鹹鑰 (繭壓窪鹽壓艱鏇範鹹積, 2.2) 更多 | - | 2015-05-14 | ||
临床3期 | - | Preservative-free FDC tafluprost-timolol | 鏇餘壓窪鹽鏇鹽齋鏇餘(範積餘夢鑰範餘觸顧窪) = 繭顧膚窪衊衊獵餘願壓 衊齋鑰艱艱齋淵膚蓋觸 (鑰觸糧糧衊繭齋範廠襯 ) 更多 | 积极 | 2013-06-01 | ||
Preservative-free NFC tafluprost-timolol | 鏇餘壓窪鹽鏇鹽齋鏇餘(範積餘夢鑰範餘觸顧窪) = 鬱淵餘觸蓋鏇製鑰簾醖 衊齋鑰艱艱齋淵膚蓋觸 (鑰觸糧糧衊繭齋範廠襯 ) 更多 |
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