预约演示
更新于：2025-08-28
Sepetaprost
更新于：2025-08-28
概要
基本信息
药物类型 小分子化药 |
别名 DE 126、DE-126、ONO 9054 + [7] |
作用方式 激动剂 |
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 |
非在研适应症- |
最高研发阶段批准上市 |
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
10
项与 Sepetaprost 相关的临床试验JPRN-jRCT2051230035
Pharmacokinetic study of STN1012600 ophthalmic solution in healthy adult males volunteers
NCT05905653
Pharmacokinetic Study of STN1012600 Ophthalmic Solution in Healthy Adult Males Volunteers
NCT05495061
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)
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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14
项与 Sepetaprost 相关的文献（医药）2025-08-01ADVANCES IN THERAPY
A Study of 24-h Efficacy and Safety of Sepetaprost vs. Latanoprost in Patients with Primary Open-Angle Glaucoma or Ocular Hypertension
Article
作者: Ropo, Auli ; Voykov, Bogomil ; Konstas, Anastasios-Georgios ; Garhöfer, Gerhard ; Lübke, Jan
INTRODUCTION:
Understanding the 24-h efficacy and safety of a novel therapy option, sepetaprost ophthalmic solution 0.002% vs. latanoprost ophthalmic solution 0.005%, may delineate its future position in glaucoma treatment.
METHODS:
In this exploratory study (EudraCT 2020-004836-93), adults with primary open-angle glaucoma (POAG) or ocular hypertension (OHT) were randomized to sepetaprost or latanoprost for 3 months following a ≤ 35-day screening period. The primary endpoint was mean 24-h intraocular pressure (IOP) at month 3 with sepetaprost vs. latanoprost. Safety outcomes included rate of adverse events (AEs).
RESULTS:
Overall, 33 participants received treatment (sepetaprost, n = 17; latanoprost, n = 16). Mean 24-h IOP was numerically lower with sepetaprost vs. latanoprost at month 3 (- 0.88 mmHg; 95% confidence interval [CI] - 2.89, 1.14; not statistically significant at the 0.05 level [NS]). Mean change from baseline in IOP at month 3 ranged from - 5.63 to - 7.00 mmHg for sepetaprost and - 3.84 to - 6.66 mmHg for latanoprost. Lower nocturnal IOP was observed with sepetaprost vs. latanoprost at month 3 (- 1.61 mmHg difference; 95% CI - 4.05, 0.83; not statistically significant; however, the 90% CI was - 5.27, - 0.17 and therefore, nominal statistical significance was achieved at the 0.10 level). Mean difference between groups indicated similar, or numerically lower, IOP with sepetaprost at individual time points at week 6 and month 3. At 36 and 48 h following sepetaprost cessation, mean IOP was lower vs. baseline IOP at the same time points. AEs occurred in 13 (76.5%) vs. 11 (68.8%) participants treated with sepetaprost vs. latanoprost.
CONCLUSION:
In participants with POAG or OHT, mean 24-h IOP and nocturnal IOP at month 3 were consistently numerically lower with sepetaprost vs. latanoprost. Safety profiles were similar between groups.
TRIAL REGISTRATION:
EudraCT 2020-004836-93.
2025-03-01Ophthalmology Glaucoma
Sepetaprost 0.002% Noninferiority vs. Timolol 0.5% in Patients with Primary Open-Angle Glaucoma or Ocular Hypertension
Article
作者: Bacharach, Jason ; Wirta, David L ; Tepedino, Michael E ; El-Harazi, Sherif M
PURPOSE:
Sepetaprost is a novel investigative prodrug, the active form of which is a dual agonist targeting both prostaglandin F receptors and prostaglandin E receptor 3. This study (NCT04742283) aimed to demonstrate the noninferiority of sepetaprost ophthalmic solution 0.002% to timolol maleate ophthalmic solution 0.5% in participants with primary open-angle glaucoma (POAG) or ocular hypertension (OHT).
DESIGN:
A phase IIb, randomized, double-masked, active-controlled, multicenter study conducted in the United States.
PARTICIPANTS:
In total, 323 adult (≥18 years) participants (POAG, 68.4%; OHT, 31.6%) were randomized 1:1 to receive either once-daily sepetaprost (n = 162) or twice-daily timolol (n = 161) in 1 eye for 3 months.
METHODS:
Intraocular pressure (IOP) was measured at 3 timepoints (8:00 am, 10:00 am, and 4:00 pm) at 3 visits (weeks 2 and 6 and month 3).
MAIN OUTCOME MEASURES:
The primary efficacy endpoint was noninferiority of sepetaprost to timolol. Noninferiority was established if the upper limit of the 2-sided 95% confidence interval (CI) for the difference in mean IOP (sepetaprost minus timolol) was ≤1.5 mmHg at all 9 specified timepoints and ≤1.0 mmHg at 5 or more of the 9 timepoints. Superiority was tested if noninferiority was achieved. Safety, including adverse events (AEs) and suspected adverse reactions, was evaluated throughout.
RESULTS:
The primary endpoint, the noninferiority of sepetaprost to timolol in mean IOP reductions, was met. The upper limit of the 2-sided 95% CI for the between-group difference in mean IOP score was <1.0 mmHg at all 9 timepoints. Superiority of sepetaprost to timolol was observed at 4:00 pm in week 2, week 6, and month 3; IOP mean difference (standard error): -0.76 (0.302), -0.73 (0.328), and -0.95 (0.319), respectively (all P < 0.05). Overall, 23.6% of participants receiving sepetaprost and 21.3% receiving timolol experienced AEs. The most commonly reported ocular AE in both groups was conjunctival hyperemia (sepetaprost, 9.9%; timolol, 2.5%).
CONCLUSIONS:
Once-daily sepetaprost 0.002% was statistically noninferior to twice-daily timolol 0.5% for lowering IOP in participants with POAG or OHT. There were no unexpected safety concerns observed, and all AEs were mild or moderate in severity.
FINANCIAL DISCLOSURE(S):
Proprietary or commercial disclosure may be found in the Footnotes and Disclosures at the end of this article.
2023-11-02Expert opinion on investigational drugs
Prostaglandin FP receptor agonists in the treatment of glaucoma and ocular hypertension: a literature review
Review
作者: Moshegov, Sophia ; Kerr, Nathan Mitchell
INTRODUCTION:
Glaucoma 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 COVERED:
This 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 OPINION:
NO 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.
100 项与 Sepetaprost 相关的药物交易
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外链
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研发状态
批准上市
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 青光眼 | 日本 | 2025-08-25 | |
| 高眼压症 | 日本 | 2025-08-25 |
未上市
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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 | 临床3期 | 日本 | 2022-08-08 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
临床2期 | 323 | (Timolol Maleate Opthalmic Solution 0.5% BID) | 襯鏇築顧壓醖糧鑰遞鑰(積網鏇壓窪繭獵鑰選淵) = 積遞鹹獵遞鑰膚繭蓋選 積獵壓艱獵築積壓繭衊 (糧築餘積夢衊壓遞窪醖, 0.242) 更多 | - | 2023-01-26 | ||
(DE-126 Opthalmic Solution 0.002% QD and Vehicle QD) | 襯鏇築顧壓醖糧鑰遞鑰(積網鏇壓窪繭獵鑰選淵) = 膚襯鹽積願夢願淵鬱獵 積獵壓艱獵築積壓繭衊 (糧築餘積夢衊壓遞窪醖, 0.239) 更多 | ||||||
临床2期 | 174 | 顧鑰蓋膚齋繭鬱衊網鹹(範艱襯鬱製窪鹹鑰遞顧) = 鑰製鹹顧糧範餘顧選鹽 鏇襯壓築製範鬱憲醖簾 (壓餘醖餘遞繭衊鬱蓋壓 ) | 积极 | 2022-02-15 | |||
顧鑰蓋膚齋繭鬱衊網鹹(範艱襯鬱製窪鹹鑰遞顧) = 蓋獵觸鏇顧鏇衊醖膚製 鏇襯壓築製範鬱憲醖簾 (壓餘醖餘遞繭衊鬱蓋壓 ) | |||||||
临床2期 | 123 | 築糧衊餘襯醖構獵繭襯(鬱齋窪憲衊網觸選觸齋) = 積獵鏇繭簾夢膚獵鬱廠 齋鬱鏇壓選遞壓製艱憲 (築鬱鹹夢鬱窪糧顧壓製 ) 更多 | 积极 | 2017-06-01 | |||
築糧衊餘襯醖構獵繭襯(鬱齋窪憲衊網觸選觸齋) = 選齋鏇築憲鑰憲膚遞觸 齋鬱鏇壓選遞壓製艱憲 (築鬱鹹夢鬱窪糧顧壓製 ) | |||||||
临床1期 | 12 | Placebo+ONO-9054 (AM dosing) | 廠夢鹽糧壓艱製鏇壓網(鏇淵艱蓋淵糧選鑰鏇製) = mild ocular hyperaemia（6 pts），mild-moderate dryness 蓋餘製夢夢壓繭鬱觸鑰 (鑰艱鑰選蓋壓憲窪構積 ) | 积极 | 2016-06-01 | ||
Placebo+ONO-9054 (PM dosing) | |||||||
临床2期 | - | 醖襯顧觸鏇遞夢觸鹹積(範簾艱網簾獵壓窪淵餘) = the number of hyperemia AEs reported for ONO-9054 was higher than reported for Xalatan® (19.4% vs 8.2%) 壓繭遞艱膚壓襯獵簾選 (鬱繭淵膚願醖積鬱鏇願 ) | 积极 | 2016-05-01 | |||
临床1期 | 48 | 繭範積鑰簾網簾廠衊壓(選網範艱鹹鬱鬱簾鬱膚) = 憲鬱網餘願遞網襯顧繭 顧糧願淵膚遞齋築顧蓋 (選夢願製憲窪獵憲艱醖 ) | 积极 | 2015-12-01 | |||
Placebo | - |
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