A Phase III Study Including a Single-Arm, Open-Label, Multi-Dose PK Study Cohort and a Randomized, Evaluator-Masked, Active Drug Controlled, Parallel Group, Multicenter, Bridging Study Cohort With a Long-term Follow-up Phase Assessing the Efficacy and Safety of DE-117B Eye Drops in Subjects With Primary Open Angle Glaucoma or Ocular Hypertension in China

This is a Phase III Study that includes a single arm, open-label, multi-dose PK study cohort and a randomized, evaluator-masked, active drug-control multicenter study.
Subjects diagnosed with POAG (Primary Open Angle Glaucoma) or OHT (Ocular Hypertension) who meet eligibility criteria will washout of their current IOP lowering medication(s), if any.
The study will investigate plasma pharmacokinetics of multi-dose 0.002% DE-117B eye drops (1 drop at a time administered once daily for 7 days) in Chinese subjects with primary open angle glaucoma or ocular hypertension.
It will investigate the safety of multi-dose 0.002% DE-117B eye drops (1 drop at a time administered once daily for 7 days) in Chinese subjects with primary open angle glaucoma or ocular hypertension.
There will be a bridging cohort and extension follow-up phase

Start Date28 Nov 2024

Sponsor / Collaborator

Santen Pharmaceutical Co., Ltd.

NCT05279716

/ Unknown statusPhase 4

Safety and Efficacy Study in NTG, POAG, Glaucoma Suspect, Ocular Hypertension Patients With Diagnosed Prostaglandin Associated Peri-orbitopathy Switching From Preserved Prostaglandin Analogues Monotherapy to Omidenepag Isopropyl

This study is for patients have been using prostaglandin analogue eye drops with a preservative for 3 months or more and have been diagnosed with prostaglandin-associated peri-orbital disease.
the investigators would like to confirm the real world evidence(RWE) of safety and efficacy after changing to Eybelis ophthalmic solution 0.002%.

Start Date15 Feb 2022

Sponsor / Collaborator

Santen Pharmaceutical Asia Pte Ltd.

JPRN-jRCTs031200106

/ CompletedNot ApplicableIIT

24 hour intraocular pressure lowering effect of Omidenepag isopropyl(24 hour IOP-lowering effect of Omidenepag isopropyl)

Start Date27 Sep 2020

Sponsor / Collaborator

Santen Pharmaceutical Co., Ltd.

100 Clinical Results associated with Omidenepag Isopropyl

100 Translational Medicine associated with Omidenepag Isopropyl

100 Patents (Medical) associated with Omidenepag Isopropyl

Literatures (Medical) associated with Omidenepag Isopropyl

01 Apr 2025·JOURNAL OF GLAUCOMA

Bioequivalence of Preservative-Free and Preserved Omidenepag Isopropyl 0.002% Ophthalmic Solutions in Patients With Primary Open Angle Glaucoma or Ocular Hypertension: Phase 3 DAISY Study

Article

Author: Aihara, Makoto ; Lu, Fenghe ; Ikeda, Toshihiro ; Odani-Kawabata, Noriko

Précis::

Preservative-free omidenepag isopropyl (OMDI) 0.002% ophthalmic solution and OMDI 0.002% ophthalmic solution preserved with benzalkonium chloride (BAK) were bioequivalent in lowering intraocular pressure (IOP) after 4 weeks’ treatment in patients with primary open angle glaucoma (POAG) or ocular hypertension (OHT).

Objective::

Preservatives in ophthalmic solutions for lowering IOP are associated with ocular surface disease. The DAISY study evaluated the bioequivalence of preservative-free OMDI 0.002% ophthalmic solution (DE-117B), with OMDI 0.002% preserved with BAK.

Methods::

DAISY was a phase 3, randomized, evaluator-masked, crossover study conducted in Japan. Patients with POAG or OHT were randomized 1:1 to DE-117B or OMDI 0.002% for 4 weeks (period 1) and then crossed over for 4 weeks (period 2). A 4-week washout preceded both periods. The primary efficacy endpoint was mean diurnal (MD) IOP at week 4 (combined periods 1 and 2). Bioequivalence between DE-117B and OMDI was defined as a 95% CI between −1.5 and 1.5 for least squares mean between-group difference in MD IOP. Adverse events were monitored.

Results::

Of 74 patients enrolled, 38 were randomized to DE-117B, then OMDI, and 36 were randomized to OMDI then DE-117B. DE-117B and OMDI demonstrated bioequivalence at week 4 [MD IOP ± SD in summary statistics: 17.76 ± 2.05 mm Hg (DE-117B) vs 17.71 ± 2.01 mm Hg (OMDI); least squares mean ± SE between-group difference in linear mixed effect model: −0.02 ± 0.18 mm Hg (95% CI: −0.38 to 0.35)]. DE-117B versus OMDI was associated with numerically lower overall ocular discomfort.

Conclusions::

Preservative-free DE-117B and BAK-containing OMDI were bioequivalent in lowering IOP after 4 weeks’ treatment in Japanese patients with POAG or OHT. DE-117B was well tolerated with a similar safety profile to OMDI.

01 Dec 2024·REPRODUCTIVE TOXICOLOGY

Male premating treatment in FEED studies: Length is not everything

Review

Author: Barrow, Paul

The ICH S5(R3) guideline recommends that male rodents in a FEED study are treated for ≥2 weeks before mating, which has frequently been criticized as being too short for the detection of all effects on sperm maturation, mating behavior and male fertility. In a FEED study, males generally continue for ≥5 weeks after the start of cohabitation. This review determines how often a 2-week premating treatment period for males was used in FEED studies of novel drugs approved by the FDA in 2022 and 2023. The male premating treatment duration was specified for 44 drugs. Only 16 % of these had a 2-week male premating treatment period. 52 % of drugs had a 4-week period. No examples were found in the literature of drugs for which male-mediated reproductive toxicity could have been detected using a 4-week, but not a 2-week, premating treatment period. Repeat dose studies in 2 species, with a duration of treatment at least equivalent to that in patients, are generally completed before the FEED study is planned. Providing no effects on male reproductive organs are detected in the repeat dose studies, a 2-week premating treatment period appears sufficient for the detection of effects on male mating performance. If toxic effects on spermatogenesis are detected in the repeat dose studies, a male FEED study serves little regulatory purpose. Even in the absence of effects on mating performance and fertility in the FEED study, a drug-related disruption of spermatogenesis would likely be considered pertinent to the human.

08 Nov 2024·Translational Vision Science & Technology

Ocular Tissue Distribution of Omidenepag Isopropyl in Rabbits and Cynomolgus Monkeys

Article

Author: Mano, Hidetoshi ; Fuwa, Masahiro ; Iwamura, Ryo ; Odani-Kawabata, Noriko ; Yamamura, Kenzo

Purpose:

To evaluate the ocular distribution of omidenepag isopropyl (OMDI) and its active form omidenepag (OMD), an EP2 receptor agonist, after topical administration of OMDI into rabbit and monkey eyes, and to determine whether OMDI and OMD interact with target receptors or enzymes of other antiglaucoma agents.

Methods:

Both eyes of six rabbits and of 14 monkeys were topically instilled with 0.03% [14C]-OMDI. Rabbits were sacrificed after one to four hours, and ocular tissues were collected. Monkeys were sacrificed after 0.25 to 24 hours, and blood and ocular tissues were collected. Radioactivity was measured in each sample. The interactions of OMDI and OMD with the receptors and enzymes associated with the mechanisms of action of other antiglaucoma agents were evaluated.

Results:

Most radioactivity applied to rabbit eyes was recovered as OMD from the cornea, aqueous humor, and iris-ciliary body. Similarly, high concentrations of radioactivity were observed in monkey cornea, bulbar/palpebral conjunctiva, and trabecular meshwork. OMD bound to EP2 receptors, but neither OMD nor OMDI bound to α2A, β1, and β2 adrenergic receptors or inhibited enzymatic activities of CA1 and CA2. OMD and OMDI had little or no effect on ROCK1 and ROCK2.

Conclusions:

OMDI rapidly permeates rabbit and monkey corneas and is converted to OMD, which distributes into anterior ocular tissues. Neither OMD nor OMDI interacted with the target receptors or enzymes of other antiglaucoma agents, suggesting that OMD interacts highly selectively with EP2 receptors.

Translational Relevance:

OMDI is a specific antiglaucoma agent that interacts selectively with ocular EP2 receptors.

News (Medical) associated with Omidenepag Isopropyl

08 Apr 2025

·www.globenewswire.com

Onconetix Signs Letter of Intent for Potential Business Combination with Ocuvex Therapeutics, Inc.

CINCINNATI, April 08, 2025 (GLOBE NEWSWIRE) -- Onconetix, Inc. (Nasdaq: ONCO) (“Onconetix” or the “Company”) (formerly Blue Water Biotech Inc.) and Ocuvex Therapeutics, Inc. (“Ocuvex”), a privately held biopharmaceutical company focused on the development and commercialization of ophthalmic therapeutic candidates to address highly prevalent diseases in need of new treatment options, today announced that they have signed a Non-Binding Letter of Intent contemplating a potential business combination transaction with Ocuvex. Andrew J. Oakley, Chairman of the Board of Onconetix, stated, “We are excited about the opportunity to combine forces with Ocuvex, whose pipeline of commercial and late clinical stage ophthalmic assets will immediately expand our reach beyond oncology , enhancing shareholder value.” Anthony W. Amato, President, CEO of Ocuvex, commented, “With an already FDA approved product, and late stage clinical assets, we believe that combining with Onconetix will allow us to broaden access to capital while continuing to focus on innovation and customer satisfaction. This is an exciting new chapter for our employees, customers, and stakeholders.” Onconetix and Ocuvex will continue negotiations to enter into a definitive agreement. Upon closing of the proposed transaction, Onconetix will acquire all the issued and outstanding equity interests of Ocuvex in exchange for newly issued shares of common stock of Onconetix. Immediately following the closing of the proposed transaction, the pre-closing Ocuvex equity holders will own approximately 90% of the equity interests in Onconetix. The Letter of Intent only represents a mutual indication of interest regarding the proposed transaction, and the terms of any such transaction are subject to a number of contingencies, including the completion of due diligence and the negotiation and execution of a definitive agreement. Completion of the proposed transaction will be subject to customary conditions, including (i) the completion of adequate financing, and (ii) the obtainment of applicable regulatory, stockholder and third-party approvals. There can be no assurance that a definitive agreement will be executed or that the proposed transaction will completed as proposed, or at all. About Onconetix, Inc. Onconetix (Nasdaq: ONCO) is a commercial stage biotechnology company focused on the research, development and commercialization of innovative solutions for men’s health and oncology. Through our recent acquisition of Proteomedix, we own Proclarix®, an in vitro diagnostic test for prostate cancer originally developed by Proteomedix and approved for sale in the European Union (“EU”) under the IVDR, which we anticipate will be marketed in the U.S. as a lab developed test (“LDT”) through our license agreement with Labcorp. We also own ENTADFI, an FDA-approved, once daily pill that combines finasteride and tadalafil for the treatment of benign prostatic hyperplasia (“BPH”), a disorder of the prostate. For more information, visit www.onconetix.com. About Ocuvex Therapeutics, Inc. Ocuvex is a privately funded biopharmaceutical company focused on the development and commercialization of ophthalmic therapeutic candidates to address highly prevalent diseases in need of new treatment options and was formed through the merger of Ocuvex Inc. and Visiox Pharmaceuticals, Inc. in August 2024. Ocuvex’s lead asset, Omlonti® (omidenepag isopropyl ophthalmic solution) 0.002%, is an EP2 receptor agonist for ocular hypertension and open-angle glaucoma. It received FDA approval in September 2022. Forward-Looking Statements Certain statements in this press release are “forward-looking” within the meaning of the Private Securities Litigation Reform Act of 1995. These statements may be identified by the use of forward-looking words such as “anticipate,” “believe,” “forecast,” “estimate,” “expect,” and “intend,” among others. These forward-looking statements (including, without limitation, the anticipated benefits and opportunities that may be generated by the proposed transaction described herein) are based on Onconetix’s current expectations, and actual results could differ materially. There are a number of factors that could cause actual events to differ materially from those indicated by such forward-looking statements. These factors include, but are not limited to, whether a definitive agreement for the proposed transaction with Ocuvex and any related financing will be entered into; whether such transactions, or any other contemplated transaction, may be completed with different terms, in an untimely manner, or not at all; whether the Company will be able to realize the benefits of the proposed transaction described herein; Onconetix’s ability to integrate the assets and commercial operations contemplated to be acquired from Ocuvex into the Company’s business; market and other conditions; risks related to Onconetix’s ability to commercialize or monetize Proclarix; risks related to the Company’s present need for capital to commercially launch Proclarix and have adequate working capital; risks related to Onconetix’s ability to attract, hire and retain skilled personnel necessary to commercialize and operate the Company’s commercial products; the failure to obtain and maintain the necessary regulatory approvals to market and commercialize Onconetix’s products; risks related to the Company’s ability to obtain and maintain intellectual property protection for its current products; whether the Company will be able to maintain compliance with Nasdaq’s applicable listing criteria and the effect of a delisting from Nasdaq on the market for the Company’s securities; and the Company’s reliance on third parties, including manufacturers and logistics companies. As with any commercial-stage pharmaceutical product or any product candidate under clinical development, there are significant risks in the development, regulatory approval and commercialization of biotechnology products. Onconetix does not undertake an obligation to update or revise any forward-looking statement. Investors should read the risk factors set forth in Onconetix’s Annual Report on Form 10-K, filed with the SEC on April 11, 2024 and periodic reports filed with the SEC on or after the date thereof. All of Onconetix’s forward-looking statements are expressly qualified by all such risk factors and other cautionary statements. The information set forth herein speaks only as of the date thereof, and Onconetix assumes no obligation to update or revise these statements unless otherwise required by law. No Offer or Solicitation This press release does not and shall not constitute an offer to sell or a solicitation of an offer to buy any securities of Onconetix or Ocuvex, nor shall there be any offer, solicitation or sale of such securities, if any, in any state or jurisdiction in which such offer, solicitation or sale would be unlawful prior to registration or qualification under the securities laws of any such state or jurisdiction. Investor and Media Contact Information: Onconetix, Inc.201 E. Fifth Street, Suite 1900Cincinnati, OH 45202Phone: (513) 620-4101Investor Contact Information: Onconetix Investor RelationsEmail: investors@onconetix.com

AcquisitionLicense out/in

07 Apr 2025

·www.stocktitan.net

Onconetix Signs Letter of Intent for Potential Business Combination with Ocuvex Therapeutics, Inc.

Onconetix (NASDAQ: ONCO) has signed a non-binding Letter of Intent for a potential business combination with Ocuvex Therapeutics, a private biopharmaceutical company specializing in ophthalmic therapeutics. The proposed transaction would result in Ocuvex shareholders owning approximately 90% of Onconetix's equity interests. Ocuvex brings an FDA-approved product, Omlonti®, for ocular hypertension and open-angle glaucoma, along with late-stage clinical assets. Onconetix currently owns Proclarix®, an in vitro diagnostic test for prostate cancer approved in the EU, and ENTADFI, an FDA-approved treatment for benign prostatic hyperplasia. The transaction completion is subject to due diligence, definitive agreement execution, adequate financing, and regulatory and stockholder approvals. There is no guarantee the transaction will be completed as proposed. CINCINNATI, April 08, 2025 (GLOBE NEWSWIRE) -- Onconetix, Inc. (Nasdaq: ONCO) (“Onconetix” or the “Company”) (formerly Blue Water Biotech Inc.) and Ocuvex Therapeutics, Inc. (“Ocuvex”), a privately held biopharmaceutical company focused on the development and commercialization of ophthalmic therapeutic candidates to address highly prevalent diseases in need of new treatment options, today announced that they have signed a Non-Binding Letter of Intent contemplating a potential business combination transaction with Ocuvex. Andrew J. Oakley, Chairman of the Board of Onconetix, stated, “We are excited about the opportunity to combine forces with Ocuvex, whose pipeline of commercial and late clinical stage ophthalmic assets will immediately expand our reach beyond oncology, enhancing shareholder value.” Anthony W. Amato, President, CEO of Ocuvex, commented, “With an already FDA approved product, and late stage clinical assets, we believe that combining with Onconetix will allow us to broaden access to capital while continuing to focus on innovation and customer satisfaction. This is an exciting new chapter for our employees, customers, and stakeholders.” Onconetix and Ocuvex will continue negotiations to enter into a definitive agreement. Upon closing of the proposed transaction, Onconetix will acquire all the issued and outstanding equity interests of Ocuvex in exchange for newly issued shares of common stock of Onconetix. Immediately following the closing of the proposed transaction, the pre-closing Ocuvex equity holders will own approximately 90% of the equity interests in Onconetix. The Letter of Intent only represents a mutual indication of interest regarding the proposed transaction, and the terms of any such transaction are subject to a number of contingencies, including the completion of due diligence and the negotiation and execution of a definitive agreement. Completion of the proposed transaction will be subject to customary conditions, including (i) the completion of adequate financing, and (ii) the obtainment of applicable regulatory, stockholder and third-party approvals. There can be no assurance that a definitive agreement will be executed or that the proposed transaction will completed as proposed, or at all.

18 Aug 2024

·www.ophthalmologytimes.com

Visiox Pharmaceuticals announces merger with Ocuvex Therpeutics

Going forward, the company will operate under the Ocuvex name, building on Visiox's commitment to disrupting the ophthalmic market through high-level collaboration with eye care professionals. Visiox Pharmaceuticals Inc announced it has entered into a definitive merger agreement with Ocuvex Therapeutics Inc. According to a news release, Ocuvex, a privately held ophthalmic pharmaceutical company focused on developing and commercializing novel therapies for glaucoma and other disorders, has a pipeline of near-term ophthalmic medicines. The companies noted the strategic combination will position the newly combined entity as a potential leader in the eye care sector with a portfolio of ophthalmic medicines. Visiox's products include omidenepag isopropyl ophthalmic solution (Omlonti), licensed by Visiox from Santen Pharmaceuticals a year ago. Another, PDP-716 (brimonidine) 0.35%, is the next closest to the market. It is a once-daily solution that the company has been hoping to launch in early 2025. It also has SDN-037 (difluprednate) 0.04%, which will grow Ocuvex's market presence and accelerate the commercialization of these therapeutics. Going forward, the company will operate under the Ocuvex name, building on Visiox's commitment to disrupting the ophthalmic market through high-level collaboration with eye care professionals. "The combination of Visiox and Ocuvex makes for a perfect match," Ryan S. Bleeks, CEO of Visiox, said in the news release. "We have reached significant milestones with our products and Ocuvex is in a great position to take these advancements forward and bring them to market faster and emerge as a future leader in eye care."

AcquisitionDrug Approval

100 Deals associated with Omidenepag Isopropyl

External Link

KEGG	Wiki	ATC	Drug Bank
D10966	-	S01EX06	DB15071

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Glaucoma	Japan	Santen SAS	21 Sep 2018
Glaucoma, Open-Angle	Japan	Santen Pharmaceutical Co., Ltd.	21 Sep 2018
Ocular Hypertension	Japan	Santen SAS	21 Sep 2018

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


DAISY (Pubmed) Manual	Phase 3	Ocular Hypertension \| Glaucoma, Open-Angle	74	Preservative-free Omidenepag Isopropyl (DE-117B) 0.002%	lroynfxwxv(hqwbntvkli) = lhzhkrdiqr xsfktbbvxp (cfvenhewxc, 2.05)	Similar	06 Jan 2025
				Omidenepag Isopropyl (OMDI) 0.002% preserved with benzalkonium chloride	lroynfxwxv(hqwbntvkli) = douizktuip xsfktbbvxp (cfvenhewxc, 2.01)
NCT02981446 (PEONY, CTgov)	Phase 3	Glaucoma, Open-Angle	370	DE-117 (DE-117 Ophthalmic Solution)	ncpjglozps(gulicdpxam) = vcoueoiifi vtikkzzkzw (ihrevppmkq, 0.25) View more	-	15 Mar 2024
				Latanoprost ophthalmic solution (Latanoprost Ophthalmic Solution 0.005%)	ncpjglozps(gulicdpxam) = nbplqzhjzn vtikkzzkzw (ihrevppmkq, 0.25) View more
APAO2024	Not Applicable	Ocular Hypotension	-	Omidenepag Isopropyl (OMDI) 0.002%	khcxzkxfon(dmzxvvbiye) = qhhzlluswq vrajrqnhmc (wcjhpyiyhz, 3.31)	-	22 Feb 2024
				Latanoprost	khcxzkxfon(dmzxvvbiye) = wjnylhdujm vrajrqnhmc (wcjhpyiyhz, 2.12)
APAO2024	Not Applicable	Glaucoma, Open-Angle	-	Omidenepag Isopropyl 0.002%	roitexyvow(skjiiumnlk) = Anterior chamber depth (ACD) was significantly decreased by 0.05 mm to 0.06 mm bhokowajxy (pnzpcnuebv ) View more	-	22 Feb 2024
DAISY (APAO2024)	Not Applicable	Glaucoma, Open-Angle \| Ocular Hypertension	74	DE-117B (omidenepag isopropyl [OMDI] 0.002% preservative-free formulation)	dmtuhbrvpa(srvzegqbwr) = AE rates were similar between DE-117B and OMDI (43.8% vs. 45.9%, respectively) zdbgwvindr (kwtlduwamq ) View more	Positive	22 Feb 2024
				OMDI 0.002% ophthalmic solution
NCT03697811 (Phase 3, Pubmed \| J Glaucoma)	Phase 3	Glaucoma, Open-Angle \| Ocular Hypertension	107	Omidenepag isopropyl 0.002%	onrtupduio(xenwduuzna) = bwbaafnfes ymshgyxsir (imsvfhfhaw, 2.12)	Positive	01 Dec 2023
NCT03697811 (Phase 3, CTgov)	Phase 3	Glaucoma, Open-Angle	107	DE-117 Ophthalmic Solution	mdjpitzaqf(brfnugjpgt) = vpylujuxhq fhokgrabjz (fwfvxhvfle, 2.831) View more	-	30 Aug 2023
NCT03691649 (CTgov)	Phase 3	Glaucoma	426	DE-117 Ophthalmic Solution (DE-117 Ophthalmic Solution)	kxgaqbxrdg(nwbrsvcgds) = sqxnhedjsd quvnsmsxva (rtlfjdxxfl, 0.22) View more	-	30 Aug 2023
				Timolol Maleate Ophthalmic Solution 0.5% (Timolol Maleate Ophthalmic Solution 0.5%)	kxgaqbxrdg(nwbrsvcgds) = ondxibgufq quvnsmsxva (rtlfjdxxfl, 0.21) View more
NCT03691662 (CTgov)	Phase 3	Glaucoma	417	DE-117 Ophthalmic Solution (DE-117 Ophthalmic Solution)	qtxaemelob(vroakowfom) = mhwacsucaz jwsjvwemmz (uwusvffmng, gzozpgtndd - fgqqjlgjvm) View more	-	09 Aug 2023
				Timolol Maleate Ophthalmic Solution 0.5% (Timolol Maleate Ophthalmic Solution 0.5%)	qtxaemelob(vroakowfom) = lyepwrajda jwsjvwemmz (uwusvffmng, uhbymatvyp - buhkbhopep) View more
NCT02981446 (PEONY, AAO2021)	Phase 3	Ocular Hypertension	185	Omidenepag Isopropyl 0.002%	vafabkcylk(aqbqngwsar) = ezbnffjyqh kuhrgpnpxd (gvxtjwseof, 2.3)	Positive	14 Nov 2021
				Latanoprost 0.005%	vafabkcylk(aqbqngwsar) = oiwetdjqwr kuhrgpnpxd (gvxtjwseof, 2.1)

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