Sepetaprost(Sepetaprost) - 药物靶点：EP3 x PTGFR_在研适应症：开角型青光眼1A_专利_临床

概要

基本信息

药物类型

小分子化药

别名

+ [1]

靶点

EP3 x PTGFR

作用机制

EP3激动剂(前列腺素EP3受体激动剂)、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

开角型青光眼1A

非在研适应症-

原研机构

Ono Pharmaceutical Co., Ltd.

在研机构

Santen Pharmaceutical Co., Ltd.

非在研机构

Ono Pharma USA, Inc.

Ono Pharmaceutical Co., Ltd.

最高研发阶段临床3期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构/序列

分子式C26H36F2O6

InChIKeyBKVUSNOUTQMSBE-XCMGCKIWSA-N

CAS号1262873-06-2

关联

9

项与 Sepetaprost 相关的临床试验

JPRN-jRCT2051230035

/ Completed临床1期IIT

Pharmacokinetic study of STN1012600 ophthalmic solution in healthy adult males volunteers

开始日期2023-06-11

申办/合作机构-

NCT05905653

/ Completed临床1期

Pharmacokinetic Study of STN1012600 Ophthalmic Solution in Healthy Adult Males Volunteers

To evaluate the safety and plasma pharmacokinetics of STN1012600 ophthalmic solution 0.002% (1 drop once daily for 7 days) in healthy adult male subjects.

开始日期2023-05-25

申办/合作机构

Santen Pharmaceutical Co., Ltd.

NCT05495061

/ Completed临床3期

A Phase III, Randomized, Observer-Masked, Active-Controlled, Parallel-Group, Multicenter Study Assessing the Efficacy and Safety of STN1012600 Ophthalmic Solution 0.002% Compared With Latanoprost 0.005% in Subjects With Primary Open Angle Glaucoma or Ocular Hypertension (Angel-J1 Study)

To investigate whether the IOP lowering efficacy of STN1012600 ophthalmic solution 0.002% is non-inferior to that of latanoprost 0.005% in subjects with POAG or OHT after treatment for 4 weeks.

开始日期2022-08-09

申办/合作机构

Santen Pharmaceutical Co., Ltd.

100 项与 Sepetaprost 相关的临床结果

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100 项与 Sepetaprost 相关的转化医学

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100 项与 Sepetaprost 相关的专利（医药）

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11

项与 Sepetaprost 相关的文献（医药）

2023-11-02·Expert Opinion on Investigational Drugs

Prostaglandin FP receptor agonists in the treatment of glaucoma and ocular hypertension: a literature review

Review

作者: Kerr, Nathan Mitchell ; Moshegov, Sophia

INTRODUCTIONGlaucoma is a leading cause of blindness with intraocular pressure (IOP) as the only known modifiable risk factor. Prostaglandin FP receptor agonists are the first-line medical treatment for glaucoma and ocular hypertension. Despite their efficacy, their IOP lowering effect may be insufficient requiring second agents, and poor patient compliance to medical therapy may preclude their full effect.AREAS COVEREDThis literature review examines the novel FP receptor drugs and drug delivery devices in clinical phase trials for treatment of glaucoma. Three novel drugs targeting FP receptors were identified, including latanoprostene bunod, NCX 470, and sepetaprost. Additionally, sustained drug delivery devices in early clinical phase trials included intracameral implants, punctal plugs, ocular rings, and contact lenses.EXPERT OPINIONNO hybrid FP receptor agonists and dual FP/EP3 receptor agonists may show promise as novel medical therapies with greater efficacy than approved prostaglandin analogs in clinical use, with a similar safety profile. Alternatively, drug delivery systems may provide a similar IOP lowering effect to existing agonists but overcome issues with patient compliance and convenience. A personalized approach to drug delivery devices may be required to ensure the most appropriate fit for the patient according to the invasiveness and duration of therapy desired.

2023-04-01·Experimental Eye Research

FP and EP2 prostanoid receptor agonist drugs and aqueous humor outflow devices for treating ocular hypertension and glaucoma

Review

作者: Sharif, Najam A ; Pinchuk, Leonard ; Lu, Fenghe ; Odani-Kawabata, Noriko

Prostaglandin (PG) receptors represent important druggable targets due to the many diverse actions of PGs in the body. From an ocular perspective, the discovery, development, and health agency approvals of prostaglandin F (FP) receptor agonists (FPAs) have revolutionized the medical treatment of ocular hypertension (OHT) and glaucoma. FPAs, such as latanoprost, travoprost, bimatoprost, and tafluprost, powerfully lower and control intraocular pressure (IOP), and became first-line therapeutics to treat this leading cause of blindness in the late 1990s to early 2000s. More recently, a latanoprost-nitric oxide (NO) donor conjugate, latanoprostene bunod, and a novel FP/EP3 receptor dual agonist, sepetaprost (ONO-9054 or DE-126), have also demonstrated robust IOP-reducing activity. Moreover, a selective non-PG prostanoid EP2 receptor agonist, omidenepag isopropyl (OMDI), was discovered, characterized, and has been approved in the United States, Japan and several other Asian countries for treating OHT/glaucoma. FPAs primarily enhance uveoscleral (UVSC) outflow of aqueous humor (AQH) to reduce IOP, but cause darkening of the iris and periorbital skin, uneven thickening and elongation of eyelashes, and deepening of the upper eyelid sulcus during chronic treatment. In contrast, OMDI lowers and controls IOP by activation of both the UVSC and trabecular meshwork outflow pathways, and it has a lower propensity to induce the aforementioned FPA-induced ocular side effects. Another means to address OHT is to physically promote the drainage of the AQH from the anterior chamber of the eye of patients with OHT/glaucoma. This has successfully been achieved by the recent approval and introduction of miniature devices into the anterior chamber by minimally invasive glaucoma surgeries. This review covers the three major aspects mentioned above to highlight the etiology of OHT/glaucoma, and the pharmacotherapeutics and devices that can be used to combat this blinding ocular disease.

2022-04-01·Journal of Ocular Pharmacology and Therapeutics4区 · 医学

Phase 2b, Randomized, 3-Month, Dose-Finding Study of Sepetaprost in Patients with Primary Open-Angle Glaucoma or Ocular Hypertension: The ANGEL Study

4区 · 医学

Article

作者: Odani-Kawabata, Noriko ; Wirta, David L. ; Lu, Fenghe ; Kuwayama, Yasuaki ; Shao, Hui

Purpose: This phase 2b, randomized, observer-masked, placebo- and active-controlled, parallel-group, multinational (USA and Japan), multicenter study (NCT03216902) assessed the optimal dose of sepetaprost ophthalmic solution in patients with primary open-angle glaucoma or ocular hypertension. Methods: After washout, patients ≥18 years (USA) or ≥20 years of age (Japan) received once-daily sepetaprost for 3 months [0.0005% (n = 43); 0.001% (n = 43); 0.002% (n = 44); and 0.003% (n = 45)], latanoprost 0.005% (n = 44) or placebo until week 6, followed by sepetaprost 0.003% until month 3 (n = 22). Safety assessments included adverse event (AE) occurrence. Results: Baseline mean diurnal intraocular pressure (IOP) was 24.3 mmHg for latanoprost and ranged between 24.1 and 24.5 mmHg for the sepetaprost groups. Sepetaprost 0.002% had the lowest IOP at each month 3 time point (9:00 AM; 1:00 PM; 5:00 PM) of all sepetaprost concentrations (mean ± standard error: 17.6 ± 0.5; 17.4 ± 0.4; 16.7 ± 0.4 mmHg); similar values were observed with latanoprost (18.1 ± 0.6; 17.3 ± 0.5; 17.2 ± 0.5 mmHg). A positive dose-response relationship was observed with the 3 lower sepetaprost doses; sepetaprost 0.002% had numerically greater IOP-lowering effects than sepetaprost 0.003%. All sepetaprost doses had statistically significantly greater IOP reductions from baseline versus placebo at week 6 (P < 0.0001). This IOP-lowering effect was consistent between Japan- and USA-based patients. Most AEs were mild and occurred numerically less frequently with sepetaprost 0.002% (34.1%) versus latanoprost (50.0%). The most frequently reported AE was conjunctival hyperemia. Conclusion: In this study, sepetaprost 0.002% was the optimal concentration, showing comparable IOP-lowering efficacy and safety with latanoprost 0.005%. Most AEs were mild; occurrence was numerically lower with sepetaprost 0.002% than latanoprost 0.005%.

100 项与 Sepetaprost 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	-	-	DB12043

研发状态

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
开角型青光眼1A	临床3期	日本	Santen Pharmaceutical Co., Ltd.	2022-08-09
开角型青光眼	临床1期	美国	Ono Pharmaceutical Co., Ltd.	2014-05-01

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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


NCT04742283 (ANGEL-2, CTgov)	临床2期	开角型青光眼	323	Timolol Maleate Ophthalmic Solution 0.5% BID (Timolol Maleate Opthalmic Solution 0.5% BID)	獵獵艱襯淵製製顧繭鬱(夢鹹廠蓋鏇壓鑰壓夢餘) = 蓋餘襯淵獵壓衊膚願壓艱顧膚觸餘襯觸顧築鬱 (選製齋積繭醖餘積襯襯, 鏇選鏇壓網願選憲網鬱 ~ 範醖構鹽簾衊築窪觸蓋) 更多	-	2023-01-26
				DE-126 Ophthalmic Solution 0.002% QD (DE-126 Opthalmic Solution 0.002% QD and Vehicle QD)	獵獵艱襯淵製製顧繭鬱(夢鹹廠蓋鏇壓鑰壓夢餘) = 夢糧廠繭膚醖範鬱範鏇艱顧膚觸餘襯觸顧築鬱 (選製齋積繭醖餘積襯襯, 憲窪獵構襯窪壓齋壓繭 ~ 獵積襯窪簾積築鹹糧選) 更多
NCT03216902 (Angel Study, Pubmed) 人工标引	临床2期	高眼压症 \| 开角型青光眼	174	Sepetaprost	(壓願製膚繭蓋範觸獵糧) = 壓構遞鬱鬱顧積網簾繭壓選醖鑰簾鹽醖夢憲鹽 (積壓網網鏇鑰鬱衊夢艱 )	积极	2022-02-15
				latanoprost	(壓願製膚繭蓋範觸獵糧) = 餘淵獵築襯觸膚淵顧鹹壓選醖鑰簾鹽醖夢憲鹽 (積壓網網鏇鑰鬱衊夢艱 )
NCT02083289 (Pubmed \| Br J Ophthalmol) 人工标引	临床2期	高眼压症 \| 开角型青光眼	123	ONO-9054	(獵艱顧鏇夢鏇窪積鏇壓) = 襯選觸餘衊觸糧淵選鹹鑰襯選鹹積壓壓餘範願 (網憲廠淵鏇築窪糧願範 ) 更多	积极	2017-06-01
				Latanoprost	(獵艱顧鏇夢鏇窪積鏇壓) = 鹹鏇獵衊範醖鬱製艱廠鑰襯選鹹積壓壓餘範願 (網憲廠淵鏇築窪糧願範 )
NCT01670266 (Pubmed \| Br J Ophthalmol) 人工标引	临床1期	高眼压症 \| 开角型青光眼	12	Placebo+ONO-9054 (AM dosing)	(製選獵壓鹽蓋願鏇艱醖) = mild ocular hyperaemia（6 pts），mild-moderate dryness 憲壓壓壓鑰網選鏇鏇醖 (遞繭齋憲鏇艱鑰鹽鏇繭 )	积极	2016-06-01
				Placebo+ONO-9054 (PM dosing)
ARVO2016	临床2期	开角型青光眼 \| 高眼压症	-	ONO-9054 (0.003%, 30 μg/mL)	(艱積膚願淵鹹範鑰鬱鬱) = the number of hyperemia AEs reported for ONO-9054 was higher than reported for Xalatan® (19.4% vs 8.2%) 遞獵鹽選積鹹積鏇觸襯 (齋艱鹽鹹鹽艱廠鑰鏇壓 )	积极	2016-05-01
				Xalatan® (0.005%, 50 μg/mL)
NCT01508988 (Pubmed \| Invest Ophthalmol Vis Sci) 人工标引	临床1期	开角型青光眼 \| 高眼压症	48	ONO-9054	(鹹鹽積衊齋顧遞網襯夢) = 構襯鏇襯繭窪願廠衊餘願齋鬱獵餘範願製壓選 (蓋顧選膚願網窪繭觸繭 )	积极	2015-12-01
				Placebo	-
ARVO2013	N/A	-	-	ONO-9054	(淵鹽艱鹽鬱餘繭網鹹艱) = 構餘觸鏇鬱壓餘構遞窪鑰築繭積鹽壓製鹹淵壓 (醖製築鑰齋顧壓齋築鬱 )	-	2013-06-01