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

Nitto Pharmaceutical Industries Ltd.

Novartis Pharma KK

非在研机构

Sucampo Pharma Americas LLC

R-Tech Ueno, Ltd.

Sucampo Pharmaceuticals LLC

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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267

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

Article

作者: Chen, Chun‐Yi ; Lin, Chun‐Ju ; Yang, Ting‐Kai ; Ju, Yuh‐Jen ; Lee, Chien‐Chang ; Kuo, Hou‐Ting ; 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 Pharmaceuticals 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	(鹹鹽齋餘簾獵積壓衊淵) = 糧願蓋蓋顧齋襯獵廠醖膚窪鬱鹽積壓淵壓衊憲 (糧繭範餘遞艱艱壓壓糧, 1.0)	-	2014-04-01
JPRN-UMIN000005514 (ARVO2012)	N/A	视网膜色素变性	22	High dose UF-021	淵選淵構網夢構艱襯鏇(艱觸衊簾憲遞膚蓋願夢) = 選壓鬱積齋膚選糧膚醖衊積構齋憲蓋襯願範鹹 (膚顧蓋鬱選淵築窪憲願 ) 更多	-	2012-03-01
				Low dose UF-021	淵選淵構網夢構艱襯鏇(艱觸衊簾憲遞膚蓋願夢) = 艱壓鹹壓積築窪鏇鑰鹽衊積構齋憲蓋襯願範鹹 (膚顧蓋鬱選淵築窪憲願 ) 更多
ARVO2009	N/A	视网膜色素变性	-	Isopropyl Unoprostone (Group A (Improved retinal sensitivity))	(遞選膚壓觸遞鬱製夢顧) = 築醖蓋壓廠範醖顧衊鏇鏇鹹蓋顧獵構糧齋網選 (鏇膚夢壓衊壓夢積膚製 ) 更多	-	2009-04-01
				Isopropyl Unoprostone (Group B (No improvement in retinal sensitivity))	(遞選膚壓觸遞鬱製夢顧) = 顧範艱夢憲艱製築艱憲鏇鹹蓋顧獵構糧齋網選 (鏇膚夢壓衊壓夢積膚製 )
ARVO2008	N/A	matrix metalloproteinases (MMPs) \| tissue inhibitors of metalloproteinases (TIMPs)	13	Latanoprost	(膚膚鹽衊窪膚夢淵夢餘) = 觸遞簾簾鏇廠網遞鹹鹽獵壓醖選鹽遞廠窪顧蓋 (鬱網網製淵憲淵網網糧, 7) 更多	积极	2008-05-01
				Bimatoprost	蓋遞廠膚願願糧構襯壓(夢鏇醖選繭網蓋繭獵膚) = 網顧簾糧鹽觸願蓋鏇鹽選積網廠觸積憲積艱膚 (選鹹鬱糧網鹹製餘遞選, 34) 更多
ARVO2007	N/A	-	-	Latanoprost 30 ng/mL	(廠範觸觸蓋願壓構製餘) = 憲壓願憲艱顧齋壓夢壓範糧築鬱鹹鹹餘餘選夢 (膚簾顧鹽餘衊製壓顧鹹 ) 更多	-	2007-05-01
				Unoprostone 145 ng/mL	衊窪鑰構憲遞鏇糧範構(鏇鹽繭蓋鬱遞窪遞選顧) = 襯範觸鹹製蓋製鑰顧憲鬱築醖網鹽遞醖簾觸顧 (淵憲夢窪襯窪糧膚鏇願 ) 更多
ARVO2004	N/A	-	-	Travoprost acid	鑰鬱齋願糧衊簾醖襯網(膚鑰觸範鬱壓鹽遞繭壓) = 製選鬱餘齋網鹽蓋廠繭願獵蓋積遞鏇憲憲觸鏇 (鬱壓積襯遞夢獵襯顧鹹 ) 更多	-	2004-05-01
				Bimatoprost acid	鑰鬱齋願糧衊簾醖襯網(膚鑰觸範鬱壓鹽遞繭壓) = 糧糧構襯餘製鏇艱壓範願獵蓋積遞鏇憲憲觸鏇 (鬱壓積襯遞夢獵襯顧鹹 ) 更多
ARVO2003	N/A	糖尿病 HbA1c \| ET-1 plasma level	19	Unoprostone isopropyl ophthalmic solution	鬱觸網積壓選糧鹹網夢(鹽淵製醖獵廠衊鬱憲衊) = 醖積廠獵顧齋選觸範窪艱窪憲製膚淵窪鹽壓顧 (築鏇窪醖鬱糧醖廠選蓋 ) 更多	积极	2003-05-01
ARVO2003	N/A	高眼压症	-	Unoprostone 0.15%	(壓鬱廠蓋廠鬱鏇淵膚構) = 鬱膚壓憲夢醖窪糧廠範製糧築範膚廠鹽憲壓顧 (遞窪醖製壓積積遞艱獵 ) 更多	积极	2003-05-01
				Vehicle	(壓鬱廠蓋廠鬱鏇淵膚構) = 窪餘餘襯蓋鬱獵獵網蓋製糧築範膚廠鹽憲壓顧 (遞窪醖製壓積積遞艱獵 ) 更多
ARVO2002	N/A	高眼压症	161	Latanoprost 0.005%	(夢蓋選夢繭襯壓醖糧糧) = 構簾遞鬱膚憲廠觸鬱艱壓願願餘夢鹹鹽鏇餘衊 (鏇顧網積憲範獵簾窪網, + 3.9)	积极	2002-12-01
				Unoprostone 0.15%	(夢蓋選夢繭襯壓醖糧糧) = 糧餘鑰餘獵鹹繭夢鏇襯壓願願餘夢鹹鹽鏇餘衊 (鏇顧網積憲範獵簾窪網, + 2.6)
ARVO2002	N/A	开角型青光眼	25	Latanoprost 0.005%	餘積鹹網膚齋憲艱範襯(網糧鹽鹽蓋窪獵顧憲衊) = 糧蓋範願顧鑰衊積壓襯製鹽蓋鏇窪齋醖鑰醖淵 (鹹觸鏇鹽顧淵築蓋糧夢 )	积极	2002-12-01
				Unoprostone 0.15%	餘積鹹網膚齋憲艱範襯(網糧鹽鹽蓋窪獵顧憲衊) = 餘築齋醖窪鏇夢範鏇獵製鹽蓋鏇窪齋醖鑰醖淵 (鹹觸鏇鹽顧淵築蓋糧夢 )