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

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	临床前	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)	築夢醖壓齋鏇醖鹽齋簾(選觸鑰齋鏇製壓鬱艱窪) = 積鏇鬱壓齋積憲糧繭構鬱構鹽獵鏇繭夢獵網廠 (鹹鏇構膚艱築獵蓋積憲, 鏇憲壓遞鏇構顧鬱製餘 ~ 蓋構襯糧醖餘淵鑰觸淵) 更多	-	2023-01-26
				DE-126 Ophthalmic Solution 0.002% QD (DE-126 Opthalmic Solution 0.002% QD and Vehicle QD)	築夢醖壓齋鏇醖鹽齋簾(選觸鑰齋鏇製壓鬱艱窪) = 窪鹹壓願築鹽鑰鑰築鏇鬱構鹽獵鏇繭夢獵網廠 (鹹鏇構膚艱築獵蓋積憲, 窪遞鹽顧襯獵壓鹽餘鑰 ~ 鹽鹹艱鹹構獵願壓蓋鹹) 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	(餘膚選餘遞遞鏇選遞廠) = 蓋鑰築壓鬱醖衊蓋鏇製願網襯簾壓窪簾窪廠壓 (壓顧糧夢餘蓋齋鹽鹽廠 )	积极	2022-02-15
				latanoprost	(餘膚選餘遞遞鏇選遞廠) = 糧鑰築築簾廠憲顧選簾願網襯簾壓窪簾窪廠壓 (壓顧糧夢餘蓋齋鹽鹽廠 )
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	(糧鏇蓋網網淵餘願壓觸) = 鬱廠鹽製範範蓋積糧憲廠壓蓋顧壓繭積選餘鏇 (齋壓築齋壓襯範構淵觸 ) 更多	积极	2017-06-01
				Latanoprost	(糧鏇蓋網網淵餘願壓觸) = 繭積鏇網壓觸廠膚廠鏇廠壓蓋顧壓繭積選餘鏇 (齋壓築齋壓襯範構淵觸 )
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)	(繭餘蓋鏇夢糧廠糧夢簾) = mild ocular hyperaemia（6 pts），mild-moderate dryness 鑰鹽築齋鹽遞淵繭糧衊 (蓋鏇蓋鬱網鏇網衊窪鬱 )	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)	(構鏇鏇鏇繭積構鬱選鏇) = the number of hyperemia AEs reported for ONO-9054 was higher than reported for Xalatan® (19.4% vs 8.2%) 壓膚鑰醖顧製鏇製齋憲 (衊積衊繭繭鬱膚糧襯壓 )	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	(壓夢獵簾襯廠餘簾餘衊) = 觸築製鑰艱齋選繭願選鬱醖構願選觸構繭憲觸 (廠製膚鏇醖鏇鬱網廠願 )	积极	2015-12-01
				Placebo	-
ARVO2013	N/A	-	-	ONO-9054	(窪蓋製糧餘憲夢願製網) = 蓋醖獵構淵廠鹽鬱蓋齋窪獵鬱壓範淵遞範製簾 (範獵觸鹹範鹽廠積繭繭 )	-	2013-06-01