sepetaprost (DE-126) / Santen, Ono Pharma - LARVOL DELTA

Angel-J2: A Long Term Study of STN1012600 in Subjects With Open Angle Glaucoma or Ocular Hypertension (clinicaltrials.gov) - P3 | N=131 | Completed | Sponsor: Santen Pharmaceutical Co., Ltd. | Recruiting ➔ Completed

Trial completion • Cardiovascular • Glaucoma • Ophthalmology

Angel-J1: A Comparative Confirmatory Study of STN1012600 in Subjects With Primary Open Angle Glaucoma or Ocular Hypertension (clinicaltrials.gov) - P3 | N=325 | Completed | Sponsor: Santen Pharmaceutical Co., Ltd. | Recruiting ➔ Completed

Trial completion • Cardiovascular • Glaucoma • Ophthalmology

Pharmacokinetic Study of STN1012600 Ophthalmic Solution in Healthy Adult Males Volunteers (clinicaltrials.gov) - P1 | N=8 | Completed | Sponsor: Santen Pharmaceutical Co., Ltd. | Recruiting ➔ Completed

Trial completion • Ophthalmology

Prostaglandin FP receptor agonists in the treatment of glaucoma and ocular hypertension: a literature review. (PubMed, Expert Opin Investig Drugs) - "Three novel drugs targeting FP receptors were identified, including latanoprostene bunod, NCX 470, and sepetaprost. 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."

Journal • Review • Cardiovascular • Glaucoma • Ophthalmology

Pharmacokinetic Study of STN1012600 Ophthalmic Solution in Healthy Adult Males Volunteers (clinicaltrials.gov) - P1 | N=8 | Recruiting | Sponsor: Santen Pharmaceutical Co., Ltd.

New P1 trial • Ophthalmology

FP and EP2 prostanoid receptor agonist drugs and aqueous humor outflow devices for treating ocular hypertension and glaucoma. (PubMed, Exp Eye Res) - "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...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..."

Journal • Review • Cardiovascular • Glaucoma • Ophthalmology • PTGER2

Sepetaprost Noninferiority to Timolol Maleate in POAG or Ocular Hypertension: The ANGEL-2 Study (AAO 2022) - P2b | "The primary objective of the study, non-inferiority of sepetaprost to timolol, was met. There were no significant safety concerns."

Head-to-Head • Glaucoma • Ophthalmology

A Long Term Study of STN1012600 in Subjects With Open Angle Glaucoma or Ocular Hypertension (clinicaltrials.gov) - P3 | N=138 | Recruiting | Sponsor: Santen Pharmaceutical Co., Ltd.

Combination therapy • New P3 trial • Cardiovascular • Glaucoma • Ophthalmology

A Comparative Confirmatory Study of STN1012600 in Subjects With Primary Open Angle Glaucoma or Ocular Hypertension (clinicaltrials.gov) - P3 | N=300 | Recruiting | Sponsor: Santen Pharmaceutical Co., Ltd.

New P3 trial • Cardiovascular • Glaucoma • Ophthalmology

Emerging drugs for the treatment of glaucoma: A review of phase II & III trials. (PubMed, Expert Opin Emerg Drugs) - "However, the availability of generic prostaglandin analogs may limit adoption of these novel compounds as first line agents, except for certain subgroups of glaucoma patients. Use as adjuvant or second line therapy appears more likely for the majority of glaucoma patients."

Journal • P2 data • Review • Glaucoma • Ocular Inflammation • Ophthalmology • Optic Neuritis • Pain

Phase 2b, Randomized, 3-Month, Dose-Finding Study of Sepetaprost in Patients with Primary Open-Angle Glaucoma or Ocular Hypertension: The ANGEL Study. (PubMed, J Ocul Pharmacol Ther) - P2b | " 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%."

Clinical • Journal • P2b data • Glaucoma • Ophthalmology

The Roles Played by FP/EP3 Receptors During Pressure-lowering in Mouse Eyes Mediated by a Dual FP/EP3 Receptor Agonist. (PubMed, Invest Ophthalmol Vis Sci) - "We investigated the intraocular pressure (IOP)-lowering effect of topical sepetaprost (SPT), a dual agonist of the FP and EP3 receptors. The IOP-lowering effect of SPT lasted longer than that of latanoprost. Our data imply that this may be attributable to augmented outflow facility mediated by the FP and EP3 receptors."

Journal • Preclinical

ANGEL-2: Multicenter Study Assessing the Efficacy and Safety of DE-126 Ophthalmic Solution 0.002% Compared With Timolol Maleate Ophthalmic Solution 0.5% in Subjects With Primary Open Angle Glaucoma or Ocular Hypertension (clinicaltrials.gov) - P2b | N=323 | Completed | Sponsor: Santen Inc. | Active, not recruiting ➔ Completed | Trial completion date: Apr 2022 ➔ Dec 2021

Trial completion • Trial completion date • Glaucoma • Ophthalmology

ANGEL-2: Multicenter Study Assessing the Efficacy and Safety of DE-126 Ophthalmic Solution 0.002% Compared With Timolol Maleate Ophthalmic Solution 0.5% in Subjects With Primary Open Angle Glaucoma or Ocular Hypertension (clinicaltrials.gov) - P2b; N=323; Active, not recruiting; Sponsor: Santen Inc.; Recruiting ➔ Active, not recruiting

Clinical • Enrollment closed • Glaucoma • Ophthalmology

Clinical study comparing the efficacy and safety of DE-126 with latanoprost in patients with glaucoma (high pressure inside the eye) (clinicaltrialsregister.eu) - P2; N=40; Ongoing; Sponsor: SANTEN INCORPORATED

Clinical • New P2 trial • Glaucoma • Ophthalmology

ANGEL-2: Multicenter Study Assessing the Efficacy and Safety of DE-126 Ophthalmic Solution 0.002% Compared With Timolol Maleate Ophthalmic Solution 0.5% in Subjects With Primary Open Angle Glaucoma or Ocular Hypertension (clinicaltrials.gov) - P2b; N=294; Recruiting; Sponsor: Santen Inc.

Clinical • New P2b trial • Glaucoma • Hypertension • Ophthalmology

Prostaglandin analogues and nitric oxide contribution in the treatment of ocular hypertension and glaucoma. (PubMed, Br J Pharmacol) - "Latanoprostene bunod (LBN) and NCX 470, NO-donating derivatives of latanoprost and bimatoprost, respectively, are examples of such compounds. LBN ophthalmic solution, 0.024% (Vyzulta™), showed greater IOP-lowering efficacy compared with that of Xalatan (latanoprost ophthalmic solution, 0.005%) or 0.5% timolol maleate in clinical settings...Selective EP receptor agonists (i.e. taprenepag isopropyl, omidenepag isopropyl and aganepag isopropyl) and non-selective prostanoid receptor agonists (i.e. ONO-9054, sepetaprost isopropyl) that concomitantly stimulate FP and EP receptors have also been shown to hold promise as effective IOP-lowering agents. NCX 470 was found more effective than bimatoprost in animal models of ocular hypertension and glaucoma. Selective EP receptor agonists (i.e., taprenepag isopropyl, omidenepag isopropyl; aganepag isopropyl) and non-selective prostanoid receptors agonists (i.e., ONO-9054, sepetaprost isopropyl) that concomitantly stimulate FP and EP..."

Journal • Review • Cardiovascular • Glaucoma • Hypertension • Ophthalmology

A Novel Dual Agonist of EP3 and FP Receptors for OAG and OHT: Safety, Pharmacokinetics, and Pharmacodynamics of ONO-9054 in Healthy Volunteers. (PubMed) - Invest Ophthalmol Vis Sci - "A single dose of the novel EP3 and FP receptor agonist ONO-9054 was safe and well tolerated in healthy volunteers at doses between 0.3 and 30.0 μg/mL and resulted in a significant reduction in intraocular IOP with maximum reduction at 9 hours post dose. This supports further evaluation of ONO-9054 for the treatment of ocular hypertension and open angle glaucoma. (ClinicalTrials.gov number, NCT01508988.)."

Journal • Biosimilar

Ocular Hypotensive Effect of ONO-9054, an EP3/FP Receptor Agonist: Results of a Randomized, Placebo-controlled, Dose Escalation Study. (PubMed, J Glaucoma) - "ONO-9054 was well-tolerated and elicited dose-dependent reductions in IOP, which were sustained for at least 24 hours following 2 weeks of consecutive daily dosing."

Journal • Biosimilar • Cardiovascular • Complement-mediated Rare Disorders • Glaucoma • Immunology • Ocular Inflammation • Ophthalmology • Rare Diseases

DE-126: Completion of P2b trial (NCT03216902) for glaucoma/ocular hypertension in US/Japan in H1 2018 (Santen) - Q1 FY 2017 Results

Trial completion date • Glaucoma • Ophthalmology

Sepetaprost: Completion of P2b study for glaucoma in H1 2018 (Santen) - Q3 FY2017 Results

Trial completion date • Glaucoma • Ophthalmology

A Phase IIb Safety and Efficacy Study of DE-126 Ophthalmic Solution in Primary Open-Angle Glaucoma or Ocular Hypertension- Angel Study (clinicaltrials.gov) - P2b; N=241; Completed; Sponsor: Santen Inc.; Recruiting ➔ Completed

Clinical • Trial completion

Dose-Finding Study of Sepetaprost Ophthalmic Solution in Patients With POAG or OHT: The Phase 2b ANGEL Study (AAO 2019) - P2b; "The most frequently reported adverse event was conjunctival hyperemia (LAT, 27.3%; SEP 0.002%, 20.5%). Conclusion This study found that SEP 0.002% was the optimal dose and showed efficacy and safety comparable with those of LAT."

Clinical • P2b data

Dose-Finding Study of Sepetaprost Ophthalmic Solution in Patients With POAG or OHT: The Phase 2b ANGEL Study (AAO 2019) - No abstract available.

Clinical • P2b data

Santen eyes North American glaucoma, retina markets (Healio) - "Santen Pharmaceutical Co. is eyeing the North American market and planning to launch products for glaucoma and retina disease, Shigeo Taniuchi, president and chief operating officer, said at the 37th annual J.P. Morgan Healthcare Conference...The company has targeted launches planned in the coming years for its glaucoma products DE-117, DE-126..."

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