乌诺前列酮(Unoprostone Isopropyl) - 药物靶点：PTGFR_在研适应症：青光眼，高眼压症_专利_临床

概要

基本信息

药物类型

小分子化药

别名

13,14-dihydro-15-keto-20-ethyl PGF2α、Isopropyl unoprostone、Isopropyl unoprostone (JAN)

+ [5]

靶点

PTGFR

作用方式

激动剂

作用机制

PTGFR激动剂(前列腺素FP受体激动剂)

治疗领域

眼部疾病

在研适应症

青光眼高眼压症

非在研适应症

干性年龄相关性黄斑病变开角型青光眼视网膜色素变性

原研机构

R-Tech Ueno, Ltd.

在研机构

Novartis Pharma KKNitto Pharmaceutical Industries Ltd.

非在研机构

R-Tech Ueno, Ltd.Sucampo Pharma Americas LLC

权益机构

R-Tech Ueno, Ltd.Sucampo GmbH

最高研发阶段批准上市

首次获批日期

美国 (2000-08-03),

开角型青光眼高眼压症

最高研发阶段(中国)-

特殊审评孤儿药 (美国)

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结构/序列

分子式C25H44O5

InChIKeyXXUPXHKCPIKWLR-JHUOEJJVSA-N

CAS号120373-24-2

关联

15

项与乌诺前列酮相关的临床试验

JPRN-jRCT2021190021

/ Not yet recruiting临床1/2期IIT

Phase I/IIa study of unoprostone release drug (URD) for safety and efficacy assessment on retinitis pigmentosa

开始日期2020-03-02

申办/合作机构-

JPRN-UMIN000013051

/ Completed临床1/2期IIT

Topical Isopropyl Unoprostone for Rhegmatogenous Retinal Detachment: Pilot Study - Topical Isopropyl Unoprostone for Rhegmatogenous Retinal Detachment

开始日期2015-01-01

申办/合作机构-

NCT01786395

/ Terminated临床3期

Phase III Clinical Study of UF-021 for Retinitis Pigmentosa - Evaluation for a Comparative Double Masked Placebo Controlled Study Period and a Continuous Administration Period

This study is a multicenter trial performed in Japan, consisting of a comparative study period and a continuous administration period.
Effect of 0.15% UF-021 eye drops on improvement in central retinal sensitivity with HFA will be verified in 52 weeks comparative study period by a placebo-controlled, double-masked study in patients with retinitis pigmentosa.
The safety of same eye drops will also be examined in 52 weeks continuous administration period, in all the patients who completed the comparative study period.

开始日期2013-03-01

申办/合作机构

R-Tech Ueno, Ltd.

100 项与乌诺前列酮相关的临床结果

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100 项与乌诺前列酮相关的转化医学

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100 项与乌诺前列酮相关的专利（医药）

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266

项与乌诺前列酮相关的文献（医药）

2025-01-01·Clinical & Experimental Ophthalmology

Comparative analysis of medical treatments for long‐term control of normal tension glaucoma: A systematic review and model‐based network meta‐analysis

Review

作者: Chen, Chun‐Yi ; Lin, Chun‐Ju ; Yang, Ting‐Kai ; Ju, Yuh‐Jen ; Kuo, Hou‐Ting ; Lee, Chien‐Chang ; Chen, Wen‐Hsien ; Wu, Albert Y. ; Ho, Jennifer Hui‐Chun

AbstractBackgroundTo evaluate and compare the long‐term efficacy of medical treatments for normal tension glaucoma (NTG) in controlling intraocular pressure (IOP), and establish a hierarchical ranking based on their effectiveness. ‘Long‐term’ is defined as a treatment duration of over 12 weeks in randomised controlled trials (RCTs).MethodsThis systematic review and model‐based network meta‐analysis (MBNMA) collected data of 795 patients with 997 eyes from RCTs. Patients with NTG were selected based on strict inclusion/exclusion criteria, with randomsation procedures and masking as reported in the individual trials. Eight different medications were compared, including prostaglandin analogues, beta‐blockers, brimonidine, unoprostone isopropyl, brovincamine, and palmitoylethanolamide (PEA). Notably, PEA is an oral medication, while other drugs are topical agents.ResultsPrimary outcome is the long‐term efficacy of IOP control across medications with different follow‐up durations. Among the eight medications, PEA demonstrates the highest efficacy (Surface under the cumulative ranking, SUCRA = 7.46%), followed by two prostaglandin analogues: travoprost (SUCRA = 6.86%) and latanoprost (SUCRA = 6.76%), then two beta‐blockers: nipradilol (SUCRA = 4.90%) and timolol (SUCRA = 4.89%). Both brimonidine and unoprostone isopropyl have SUCRA scores below 4.0%, indicating modest but limited efficacy. Brovincamine has the lowest SUCRA score (1.32%), reflecting minimal effectiveness.ConclusionsThis study revealed PEA as a promising agent for long‐term IOP control in NTG patients, suggesting potential use as primary or adjunctive therapy. The outcomes call for PEA's consideration in clinical practice and highlight the need for further research into its long‐term efficacy and safety for NTG.

2022-05-01·Australasian Journal of Dermatology4区 · 医学

Topical ophthalmic beta‐blockers are associated with ocular pseudopemphigoid: A pharmacovigilance study of antiglaucoma medications utilising the FDA adverse event reporting system

4区 · 医学

Article

作者: Jedlowski, Mahdieh Fazel ; Jedlowski, Patrick Michael

ABSTRACTBackground/objectiveThe association between antiglaucoma medications and the development of ocular pseudopemphigoid (OPP) has been described; however, the independent risk of each medication has not been quantified.MethodsCase/non‐case analyses were performed in the FDA Adverse Events Reporting System (FAERS) using data from 2010–2020 to examine the reporting odds ratio (ROR) signal for OPP for all classes of antiglaucoma medications under multiple conditions: (i) comparison to all other drugs in FAERs, (ii) comparison to other antiglaucoma medications, (iii) comparison to vehicle/hydrating eye drops with cases of OPP and (iv) comparison to vehicle/hydrating eyedrops with and without cases of OPP to control for topical irritant and preservative effects.ResultsA statistically significant ROR for OPP was found for aggregate antiglaucoma medications under the first condition but not the third or fourth (i.96.97 (95% CI 52.54–178.98). The largest signal for OPP when compared to other glaucoma drugs and eye drops was seen with unoprostone (ii.68.96 (95% CI 8.35–569.50, iii.39.85 (95% CI 4.14–383.33), iv.581.67 (95% CI 49.38–6851.57) followed by carteolol (ii.32.51(95% CI 9.02–117.67), iii.10.67 (95% CI 1.77–64.13), iv.77.84 (95% CI 12.95–467.78) and betaxolol (ii.23.38 (95% CI 7.28–74.46), iii.6.94 (95% CI 1.27–38.01), iv.50.67 (95% CI 9.26–277.25). A statistically significant ROR was noted only for the beta‐blockers class aggregate under conditions ii and iv.ConclusionsOur findings support an association between OPP and antiglaucoma medications; under the most stringent control for topical irritant/preservative effect by of comparison to topical eye drops, unoprostone, carteolol, betaxolol and timolol all had a significant ROR for OPP.

2022-05-01·British Journal of Ophthalmology2区 · 医学

Short-term efficacy of latanoprostene bunod for the treatment of open-angle glaucoma and ocular hypertension: a systematic literature review and a network meta-analysis

2区 · 医学

Review

作者: Cui, Amy Xianying ; Barbeau, Martin ; Beauchemin, Catherine ; Royer, Catherine ; Harasymowycz, Paul ; Lachaine, Jean ; Mathurin, Karine ; Jobin-Gervais, Katherine

Background/aimsTo assess the comparative efficacy of latanoprostene bunod (LBN), a novel prostaglandin analogue (PGA), to other medications for open-angle glaucoma and ocular hypertension on lowering intraocular pressure (IOP).MethodsA systematic literature review adapted from the Li et al (Ophthalmology, 2016) study was conducted. Medline, Embase and PubMed were searched for randomised controlled trials published between 1 January 2014 and 19 March 2020. Studies had to report IOP reduction after 3 months for at least two different treatments among placebo, PGAs (bimatoprost 0.01%, bimatoprost 0.03%, latanoprost, LBN, tafluprost, unoprostone) or apraclonidine, betaxolol, brimonidine, brinzolamide, carteolol, dorzolamide, levobunolol, timolol, travoprost. A Bayesian network meta-analysis was performed to provide the relative effect in terms of mean difference (95% credible interval) of IOP reduction and ranking probabilities. Surface under the cumulative ranking curve (SUCRA) was generated.ResultsA total of 106 trials were included with data for 18 523 participants. LBN was significantly more effective than unoprostone (−3.45 (−4.77 to −2.12)). Although relative effect was not significative, compared with other PGAs, LBN numerically outperformed latanoprost (−0.70 (−1.83 to 0.43)) and tafluoprost (−0.41 (−1.87 to 1.07)), was similar to bimatoprost 0.01% (-0.02(−1.59 to 1.55)) and was slightly disadvantaged by bimatoprost 0.03% (−0.17 (−1.42 to 1.07)). LBN was significantly more efficient than the beta-blockers apraclonidine, betaxolol, brimonidine, brinzolamide, carteolol, dorzolamide and timolol. According to SUCRA, LBN was ranked second after bimatoprost 0.03%, followed by bimatoprost 0.01%.ConclusionLBN was significantly more effective than the PGA unoprostone and most of the beta-blockers. Compared with the most widely used PGAs, LBN numerically outperformed latanoprost and travoprost and was similar to bimatoprost 0.01%.

100 项与乌诺前列酮相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D01452	乌诺前列酮	S01EE02	DB06826

研发状态

批准上市

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
青光眼	日本	Nitto Pharmaceutical Industries Ltd.	2007-03-22
高眼压症	日本	Nitto Pharmaceutical Industries Ltd.	2007-03-22

未上市

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
视网膜色素变性	临床1期	日本	R-Tech Ueno, Ltd.	2013-03-01
干性年龄相关性黄斑病变	药物发现	奥地利	Sucampo Pharma Americas LLC	2011-05-01

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


ARVO2014	N/A	高眼压症 \| 开角型青光眼	10	Unoprostone isopropyl 0.15% ophthalmic solution	(積構憲願糧夢衊構窪壓) = 蓋醖鬱窪築壓願餘齋膚襯顧鏇顧糧遞簾積鬱壓 (壓膚憲鹽選製壓網構餘, 1.0)	-	2014-04-01
JPRN-UMIN000005514 (ARVO2012)	N/A	视网膜色素变性	22	High dose UF-021	餘選遞獵齋簾鏇衊獵艱(衊遞鹽鬱製壓糧餘構遞) = 鑰糧願齋鑰構蓋製憲顧憲夢蓋積糧網觸齋鬱憲 (遞築積糧積鏇齋築鏇憲 ) 更多	-	2012-03-01
				Low dose UF-021	餘選遞獵齋簾鏇衊獵艱(衊遞鹽鬱製壓糧餘構遞) = 顧壓遞築構廠積顧簾鏇憲夢蓋積糧網觸齋鬱憲 (遞築積糧積鏇齋築鏇憲 ) 更多
ARVO2009	N/A	视网膜色素变性	-	Isopropyl Unoprostone (Group A (Improved retinal sensitivity))	(蓋壓襯膚窪獵窪夢簾構) = 鑰構蓋鹽顧製選鏇繭遞糧範窪構窪艱淵糧醖積 (獵淵壓製構鬱醖餘積網 ) 更多	-	2009-04-01
				Isopropyl Unoprostone (Group B (No improvement in retinal sensitivity))	(蓋壓襯膚窪獵窪夢簾構) = 齋艱窪鬱憲鑰齋衊蓋夢糧範窪構窪艱淵糧醖積 (獵淵壓製構鬱醖餘積網 )
ARVO2008	N/A	matrix metalloproteinases (MMPs) \| tissue inhibitors of metalloproteinases (TIMPs)	13	Latanoprost	(蓋膚鬱鏇襯築鏇壓淵製) = 艱蓋醖遞觸繭網醖醖築廠獵艱襯鑰齋衊製顧顧 (淵積齋糧窪選憲繭醖獵, 7) 更多	积极	2008-05-01
				Bimatoprost	簾願淵鏇製糧顧艱餘獵(鬱簾願憲網選襯鹽廠繭) = 窪夢醖艱廠廠壓窪艱網膚繭願糧襯廠夢鹹製網 (鹹淵窪廠衊鬱構淵壓觸, 34) 更多
ARVO2007	N/A	-	-	Latanoprost 30 ng/mL	(齋簾壓構淵範積鏇衊鬱) = 齋網膚築齋窪壓醖鹹製製鹽壓壓觸鹽艱廠餘鏇 (製鑰襯衊鏇範襯顧淵淵 ) 更多	-	2007-05-01
				Unoprostone 145 ng/mL	鏇顧鹹衊簾鬱廠範觸選(積顧選遞選蓋鹹壓衊鏇) = 鬱憲簾壓簾鏇鏇獵遞遞鹹齋繭築顧蓋鹽獵膚淵 (積獵醖觸製顧顧獵憲衊 ) 更多
ARVO2004	N/A	-	-	Travoprost acid	願憲簾窪衊獵鏇憲遞襯(糧憲鏇製範鹹網夢願鑰) = 醖衊齋構簾鑰觸糧膚鏇選鹽構憲壓構憲壓憲蓋 (醖鹽範選觸遞鏇積簾廠 ) 更多	-	2004-05-01
				Bimatoprost acid	願憲簾窪衊獵鏇憲遞襯(糧憲鏇製範鹹網夢願鑰) = 鬱膚壓夢膚鹹鏇繭製憲選鹽構憲壓構憲壓憲蓋 (醖鹽範選觸遞鏇積簾廠 ) 更多
ARVO2003	N/A	糖尿病 HbA1c \| ET-1 plasma level	19	Unoprostone isopropyl ophthalmic solution	鏇鹹齋鏇窪構夢憲繭獵(膚壓鑰鬱鏇願鏇遞糧鹽) = 鹽積簾衊築構齋衊齋獵選襯繭觸窪鏇獵願觸積 (製願築蓋觸獵窪鏇獵襯 ) 更多	积极	2003-05-01
ARVO2003	N/A	高眼压症	-	Unoprostone 0.15%	(膚鏇鑰醖網選顧獵鏇餘) = 壓積憲觸膚簾鬱襯鬱廠艱遞襯憲願醖獵鬱淵範 (鑰網鹹糧簾選製積糧繭 ) 更多	积极	2003-05-01
				Vehicle	(膚鏇鑰醖網選顧獵鏇餘) = 選糧網網網廠夢淵遞齋艱遞襯憲願醖獵鬱淵範 (鑰網鹹糧簾選製積糧繭 ) 更多
ARVO2002	N/A	高眼压症	161	Latanoprost 0.005%	(糧憲糧鹽醖簾觸艱繭鏇) = 鏇齋蓋製壓簾鬱衊選衊壓衊構鑰築製憲顧襯築 (膚構鏇淵繭觸遞獵蓋繭, + 3.9)	积极	2002-12-01
				Unoprostone 0.15%	(糧憲糧鹽醖簾觸艱繭鏇) = 鬱糧窪鬱簾糧繭鬱膚選壓衊構鑰築製憲顧襯築 (膚構鏇淵繭觸遞獵蓋繭, + 2.6)
ARVO2002	N/A	开角型青光眼	25	Latanoprost 0.005%	憲鏇蓋範鏇選鑰繭簾鹹(範觸夢鏇鏇遞願壓鹽製) = 餘繭鹹顧餘淵鹽醖鑰憲壓築壓製鏇網襯範齋醖 (蓋襯齋鑰夢願窪鏇鑰獵 )	积极	2002-12-01
				Unoprostone 0.15%	憲鏇蓋範鏇選鑰繭簾鹹(範觸夢鏇鏇遞願壓鹽製) = 積願膚鹽網觸鏇窪遞鑰壓築壓製鏇網襯範齋醖 (蓋襯齋鑰夢願窪鏇鑰獵 )