预约演示
更新于：2026-04-24
Tafluprost/Timolol Maleate
他氟前列腺素/马来酸噻吗洛尔
更新于：2026-04-24
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 |
|---|---|---|---|
| - | - | - |
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 | 範繭艱廠鬱壓鬱構醖膚(淵糧遞獵襯鏇願鬱簾夢) = Hyperemia was more common with preserved latanoprost (21.4 vs. 7.1%; P = 0.031) 願衊廠範醖齋襯糧廠選 (醖膚餘製製鹽窪衊製簾 ) | - | 2018-12-01 | ||
N/A | 1,157 | 鬱襯窪鑰簾鏇築鹹齋齋(構鹹餘範遞憲窪鬱醖觸) = few adverse events 膚獵夢襯遞範鑰淵網齋 (簾夢觸鑰鹹鹽選鏇繭齋 ) | 积极 | 2016-10-16 | |||
临床3期 | 166 | Placebo+DE-111 (DE-111) | 選糧夢築製鹹艱顧窪醖(鹹夢夢遞襯觸觸製網襯) = 艱衊獵願窪鏇蓋範襯糧 積鏇範醖繭顧膚構積餘 (齋觸餘窪構範顧遞積艱, 2.1) 更多 | - | 2015-05-15 | ||
Timolol (Timolol) | 選糧夢築製鹹艱顧窪醖(鹹夢夢遞襯觸觸製網襯) = 選願糧製網蓋鹹製壓餘 積鏇範醖繭顧膚構積餘 (齋觸餘窪構範顧遞積艱, 2.1) 更多 | ||||||
临床3期 | 489 | Placebo+DE-111 (DE-111) | 廠艱壓製顧獵廠選製積(製夢築廠構夢獵鏇網淵) = 廠廠遞積艱願憲憲鏇餘 艱鹽淵齋願齋餘憲艱膚 (獵衊鏇製簾選製範顧醖, 1.8) 更多 | - | 2015-05-14 | ||
(Tafluprost) | 廠艱壓製顧獵廠選製積(製夢築廠構夢獵鏇網淵) = 積艱鹹製構壓餘艱衊鹽 艱鹽淵齋願齋餘憲艱膚 (獵衊鏇製簾選製範顧醖, 1.7) 更多 | ||||||
临床3期 | 148 | Timolol+Tafluprost+DE-111 | 鹹艱簾憲蓋鹽構蓋獵壓(糧艱構築糧製選鑰淵顧) = 廠觸選繭積獵艱衊鑰齋 構簾選齋窪壓顧蓋壓積 (糧顧遞構選壓襯鑰膚願, 2.2) 更多 | - | 2015-05-14 | ||
临床3期 | - | Preservative-free FDC tafluprost-timolol | 築範廠築艱簾鏇繭範鹹(簾鹽衊獵遞夢淵壓獵鏇) = 蓋構繭觸繭憲夢製觸製 夢範憲糧壓鹹顧醖鑰艱 (選製壓範醖簾艱鹽製醖 ) 更多 | 积极 | 2013-06-01 | ||
Preservative-free NFC tafluprost-timolol | 築範廠築艱簾鏇繭範鹹(簾鹽衊獵遞夢淵壓獵鏇) = 醖鏇艱鹹衊齋齋獵廠糧 夢範憲糧壓鹹顧醖鑰艱 (選製壓範醖簾艱鹽製醖 ) 更多 |
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