A comparative study on the pharmacokinetic characteristics of timolol maleate ophthalmic colloidal solution after multiple administration in healthy subjects and the pharmacokinetic characteristics of timolol maleate gel in the patients with hyperplastic infant hemangioma with shallow phenotype

Start Date14 Jun 2024

Sponsor / Collaborator-

ChiCTR2400081513 / SuspendedEarly Phase 1IIT

Study on the effectiveness and safety of topical use of timolol maleate in the prevention of burn scar

Start Date01 Apr 2024

Sponsor / Collaborator-

IRCT20230712058759N1 / CompletedPhase 1/2IIT

Efficacy of topical 0.5% Timolol Maleate in chronic recalcitrant heel fissures

Start Date12 Jun 2023

Sponsor / Collaborator-

100 Clinical Results associated with Timolol Maleate

100 Translational Medicine associated with Timolol Maleate

100 Patents (Medical) associated with Timolol Maleate

1,874

Literatures (Medical) associated with Timolol Maleate

01 Dec 2024·COLLOIDS AND SURFACES B-BIOINTERFACES

Oxidized cellulose microneedle patch combined with vascular embolization and local delivery of timolol maleate for hemangiomas

Article

Author: Jiang, Yizhou ; Li, Haibo ; Niu, Chuanqiang ; Tan, Xiaoyun ; Pang, Ningdong ; Zhou, Zijun ; Jiang, Hua ; Guo, Yiqun ; Liu, Lu ; Liu, Lang

Hemangiomas are superficial tumors characterized by dense vascular structures that often affect the patient's aesthetic appearance due to the obvious red appearance on the skin. Current treatments, especially timolol maleate in the form of eye drops and hydrogels, suffer from low transdermal drug delivery rates, resulting in prolonged treatment time. To address this challenge, our study introduced a soluble microneedle patch with dextran as the main material to form microcatheters for sustained delivery of timolol maleate. In addition, we proposed a vascular embolization strategy to disrupt the blood supply in hemangiomas. Oxidized cellulose (C-cellulose) was selected for its excellent hemostatic properties. We incorporated C-cellulose into dextran microneedles to facilitate thrombosis in the vascular-rich areas of hemangiomas. The innovative microneedle patch we developed can penetrate the skin to a depth of 430 μm and dissolve rapidly within 3 minutes, ensuring direct drug delivery to the subcutaneous layer. Notably, the treated skin area regained its original appearance within two hours after treatment. In addition to excellent skin permeability and rapid dissolution, these patches significantly promoted apoptosis and inhibited cell migration in mouse hemangioendothelioma EOMA cells. Our results demonstrate that this approach not only achieves significant tumor inhibition in a mouse hemangioma model, but also represents a more effective, convenient, and non-invasive treatment option. Therefore, dextran/C-cellulose/timolol maleate microneedle patch (MNs/Timolol) has broad clinical application prospects in the treatment of hemangiomas, minimizing the risk of additional damage and improving treatment efficacy.

01 Nov 2024·Drug delivery and translational research

Chitosan nanoparticles laden contact lenses for enzyme-triggered controlled delivery of timolol maleate: A promising strategy for managing glaucoma

Article

Author: Maulvi, Furqan A ; Patel, Ashmi R ; Shah, Dinesh O ; Shetty, Kiran H ; Desai, Ditixa T ; Willcox, Mark D P

To improve drug bioavailability, eye drops can be replaced by drug-eluting contact lenses. However, issues of drug leaching from lenses during manufacture and storage, and sterilization, currently limit their commercial application. To address the issues, stimuli-(lysozyme)-sensitive chitosan nanoparticles were developed to provide controlled ocular drug delivery. Nanoparticles were prepared by ionic gelation and characterized by TEM, X-ray diffraction, DSC, and FTIR. In the flux study, conventional-soaked contact lenses (SM-TM-CL) showed high-burst release, while with direct drug-only laden contact lenses (DL-TM-CL) the drug was lost during extraction and sterilization, as well as having poor swelling and optical properties. The nanoparticle-laden contact lenses (TM-Cht-NPs) showed controlled release of timolol for 120 h in the presence of lysozyme, with acceptable opto-physical properties. In the shelf-life study, the TM-Cht-NPs contact lenses showed no leaching or alteration in the drug release pattern. In animal studies, the TM-NPs-CL lenses gave a high drug concentration in rabbit tear fluid (mean = 11.01 µg/mL for 56 h) and helped maintain a low intraocular pressure for 120 h. In conclusion, the chitosan nanoparticle-laden contact lenses demonstrated the potential application to treat glaucoma with acceptable opto-physical properties and addressed the issues of drug-leaching during sterilization and storage.

01 Nov 2024·Journal of advanced research

Ginsenoside Rb2 inhibits p300-mediated SF3A2 acetylation at lysine 10 to promote Fscn1 alternative splicing against myocardial ischemic/reperfusion injury

Article

Author: Guo, Chen ; Zhao, Daqing ; Wang, Yisa ; Li, Xiangyan ; Chen, Jinjin ; Zhao, Linhua ; Yao, Yao ; Li, Jing ; Huang, Qingxia ; Lou, Jia ; Yang, Wenzhi ; Tong, Xiaolin ; Wu, Mingxia

INTRODUCTION:

Ginsenosides (GS) derived from Panax ginseng can regulate protein acetylation to promote mitochondrial function for protecting cardiomyocytes. However, the potential mechanisms of GS for regulating acetylation modification are not yet clear.

OBJECTIVES:

This study aimed to explore the potential mechanisms of GS in regulating protein acetylation and identify ginsenoside monomer for fighting myocardial ischemia-related diseases.

METHODS:

The 4D-lable free acetylomic analysis was employed to gain the acetylated proteins regulated by GS pretreatment. The co-immunoprecipitation assay, immunofluorescent staining, and mitochondrial respiration measurement were performed to detect the effect of GS or ginsenoside monomer on acetylated protein level and mitochondrial function. RNA sequencing, site-specific mutation, and shRNA interference were used to explore the downstream targets of acetylation modificationby GS. Cellular thermal shift assay and surface plasmon resonance were used for identifying the binding of ginsenoside with target protein.

RESULTS:

In the cardiomyocytes of normal, oxygen glucose deprivation and/or reperfusion conditions, the acetylomic analysis identified that the acetylated levels of spliceosome proteins were inhibited by GS pretreatment and SF3A2 acetylation at lysine 10 (K10) was significantly decreased as a potential target of GS. Ginsenoside Rb2 was identified as one of the active ginsenoside monomers for reducing the acetylation of SF3A2 (K10), which enhanced mitochondrial respiration against myocardial ischemic injury in in vivo and in vitro experiments. RNA-seq analysis showed that ginsenoside Rb2 promoted alternative splicing of mitochondrial function-related genes and the level of fascin actin-bundling protein 1 (Fscn1) was obviously upregulated, which was dependent on SF3A2 acetylation. Critically, thermodynamic, kinetic and enzymatic experiments demonstrated that ginsenoside Rb2 directly interacted with p300 for inhibiting its activity.

CONCLUSION:

These findings provide a novel mechanism underlying cardiomyocyte protection of ginsenoside Rb2 by inhibiting p300-mediated SF3A2 acteylation for promoting Fscn1 expression, which might be a promising approach for the prevention and treatment of myocardial ischemic diseases.

News (Medical) associated with Timolol Maleate

14 Oct 2024

·endpts.com

Bausch + Lomb's stock rises following report of potential bid from private equity firms TPG and Blackstone

Private equity firms TPG and Blackstone are working on a potential deal to buy Brent Saunders-led eye care company Bausch + Lomb, the Financial Times reports. Citing “people familiar with the matter,” FT wrote Monday that the groups had already expressed interest in buying Bausch + Lomb before it was publicly listed in 2022. Its stock $BLCO rose about 9% on Monday following the reporting, trading around $21. Incoming offers for the company are expected to value it at an enterprise value between $13 billion and $14 billion, FT reports, with formal offers expected by as early as the end of October, though “several” other private equity firms considering making an offer have dropped out of the race. FT added that the sale process for the company is led by advisors at Goldman Sachs and started in order to resolve a feud between shareholders and creditors of its parent company Bausch Health, which is also a majority owner. Representatives for Bausch, Blackstone and TPG all declined to comment to Endpoints News , with Bausch adding that it doesn’t comment on “rumors or speculation.” Bausch + Lomb is known for its vision care products like contact lenses and eye drops, including its glaucoma drugs Vyzulta, Timoptic and Istalol. The company recorded $1.2 billion in revenue for the second quarter of 2024, a 17% increase from the same quarter last year.

Acquisition

21 Mar 2024

·www.prnewswire.com

Landmark Non-inferiority Clinical Trial Demonstrates Nanodropper's Positive Impact on Glaucoma Treatment

A new study published in Ophthalmology demonstrated no clinically significant difference in IOP with microdrops with the Nanodropper® Adaptor versus conventional eyedrops of the glaucoma treatment timolol maleate 0.5%. ROCHESTER, Minn., March 21, 2024 /PRNewswire/ -- Nanodropper, Inc., an ophthalmic device company that created the eyedrop volume-reducing Nanodropper® Adaptor, announced today that its clinical trial "An Evaluation of the Efficacy and Safety of Timolol Maleate 0.5% Microdrops Administered with the Nanodropper" was published in the journal Ophthalmology. Continue Reading This was a prospective, multicenter, randomized, parallel-group, single-masked, active-controlled, non-inferiority trial. The trial enrolled glaucoma patients and demonstrated there was no clinically significant difference in the intraocular pressure (IOP)-lowering effects of microdrops administered with the Nanodropper Adaptor compared to conventional eyedrops of timolol, an eyedrop medication commonly used to treat glaucoma. This was observed at all time points throughout the eight-hour study. Subjects in the microdrops arm also experienced a significantly smaller decrease in heart rate compared to those that received conventional drops, demonstrating there could be an enhanced safety profile of using a microdrop of timolol compared to a conventionally-sized eyedrop. Landmark Non-inferiority Clinical Trial Demonstrates Nanodropper's Positive Impact on Glaucoma Treatment Post this "We are thrilled, albeit not surprised, by these encouraging results demonstrating the Nanodropper Adaptor's capacity to improve patient safety," said Jenny Steger, PhD, Chief Scientific Officer of Nanodropper. "Thousands of eyecare clinics in the U.S., and tens of thousands of patients worldwide, are already utilizing the Nanodropper to great effect. This study reflects the benefits these patients have been experiencing." The Nanodropper Adaptor is the first and only sterile adaptor for eyedrop bottles that reduces eyedrop volume to just what the eye can absorb, significantly reducing medication waste and financial barriers for patients and clinics. This study's results suggest the Nanodropper Adaptor's microdrops provide patients an enhanced safety improvement over conventional eyedrops while maintaining the efficacy of the medication. "Eyedrop size has not seriously been commercially addressed in the past," said Alan L. Robin, MD, corresponding author on the publication and a global leader in glaucoma research and treatment for decades. He is a charter member of the American Glaucoma Society, its first executive vice president, and sits on Nanodropper's Medical Advisory Board. His previous research on microvolume delivery of eyedrops directly inspired the creation of the Nanodropper Adaptor. "I believe microvolume delivery technologies may offer solutions in the form of less waste, increased patient savings, and hopefully better safety profiles for many topical ophthalmic medications," said Dr. Robin. "Nanodropper is the first commercially available potential solution to this long-standing problem." To review the study in Ophthalmology, the full-text version can be viewed at this link. Where are Nanodropper Adaptors available? Nanodroppers are available at , and in over 2,500 eyecare clinics across all 50 states, Puerto Rico, and the U.S. Virgin Islands. Nanodropper Adaptors have also been made available via the company's Give the Gift of Vision charitable program to U.S.-based patients who cannot afford to purchase one, and internationally through more than a dozen nonprofit partners providing access to eyecare on a global scale. Contact: Mackenzie Andrews [email protected] SOURCE Nanodropper

Clinical Result

21 Mar 2024

·www.prnewswire.com

OcuMension (01477.HK) Invests Over RMB 123.8 Million in Research, Technology and Self-development Progress in Tandem, Main Product Sales Show Comprehensive Growth

SHANGHAI, March 21, 2024 /PRNewswire/ -- On the evening of March 21st, OcuMension Therapeutics (Shanghai) Co., Ltd. (01477.HK, hereinafter referred to as "OcuMension" or the "Company") disclosed its 2023 annual performance report. The company achieved a total operating income of RMB 246.4 million for the full year, a year-on-year increase of 55.0%; with a comprehensive gross profit of RMB 144.4 million, representing a year-on-year increase of 40.3%. During the reporting period, the company's major operating indicators performed well, benefiting from rapid growth in sales revenue and further improvement in operational efficiency and cost control. Enhanced Product Matrix, Rapid Expansion Leveraging First-mover Advantage Adhering to the development philosophy of "providing world-class holistic solutions for pharmaceuticals," OcuMension has consistently devoted itself to identifying, developing, and commercializing innovative or best-in-class ophthalmic therapies. The company continuously enriches and expands its product matrix to meet the significant demand gap in Chinese ophthalmic medical care while maintaining its leading position in the ophthalmic track. A diversified product matrix has laid the foundation for the company's steady growth. Leveraging its strong corporate strength, the company possesses a leading ophthalmic pharmaceutical platform with various drugs for both anterior and posterior segments, providing strong support for the company's development. Among them, the company's main products such as Ouqin (sodium hyaluronate eye drops), Emidin (timolol maleate eye drops), and Shilida (latanoprost eye drops) have all maintained steady growth. Additionally, as one of OcuMension's outstanding products, OT-401(YUTIQ)® for the treatment of chronic non-infectious uveitis was successfully included in the medical insurance catalog in December of last year. It is reported that OT-401(YUTIQ)® completed the first domestic injection in December 2022, breaking the deadlock in the treatment of uveitis in China at that time, filling the treatment gap domestically, alleviating the burden on patients to the greatest extent, and marking the formal entry of the product into ophthalmic clinical applications. It is worth noting that since OT-401(YUTIQ)® officially entered the medical insurance catalog on January 1st of this year, the company has rapidly promoted its medical insurance landing work nationwide with its comprehensive commercialization capabilities, bringing better and more affordable treatment options for uveitis patients. As of the disclosure date of the report, the terminal injection volume of OT-401(YUTIQ)® has exceeded the total for the previous year and is expected to continue to rapidly expand. Overcoming Technological Peaks, Strengthening Self-defense with R&D Strength To break the previous dominance of foreign capital in the Chinese ophthalmic drug market, the company continues to increase its investment in research and development, focusing on dual-source innovation, optimizing registration and development, promoting commercialization, and adhering to high-quality technical standards throughout the entire production cycle to ensure product safety, efficacy, and quality control. With years of technological accumulation and industrial experience, in 2023, the company achieved several milestone breakthroughs with the assistance of clinical PI, including the submission of NDA for OT-1001 (timolol hydrochloride eye drops) accepted by CDE and included in the priority review program; completion of global patient enrollment for Phase III MRCT of OT-101 (atropine sulfate eye drops); completion of real-world studies for OT-502 (dexamethasone implant), currently in the Pre-NDA stage; the completion of patient enrollment for Phase II clinical trials of OT-202 (tyrosine kinase inhibitor), a self-developed drug for dry eye syndrome, in 25 experimental centers, with a total of over 700 patients enrolled during the year. This not only enriches the company's product pipeline but also provides more high-quality treatment options for patients. The edge of technology stems from the strength of research and development behind it. Throughout 2023, the company invested a total of RMB 123.8 million in research and development, injecting strong momentum into the company's continued development. Meanwhile, the company also focuses on building a clinical research platform and constructing a research and development team to enrich the company's product pipeline and produce multi-level products that better meet patient needs. So far, the company has a total of 25 drug assets for both anterior and posterior segments, with 12 products already commercialized, covering both anterior and posterior segments and forming a strong product matrix in the fields of anti-allergy and glaucoma. Among them, five products in the company's pipeline are still in Phase III clinical trials, making it one of the companies with the highest number of Phase III clinical trials for innovative drugs in the Chinese ophthalmic drug market. It is noteworthy that the company has made breakthrough progress in the research and development of the myopia drug Atropine recently. Faced with the challenge of stability, the company cleverly solved the long-term storage stability problem of low-concentration atropine sulfate solution by using a dual-chamber device of reconstitution solution and freeze-dried powder. Currently, the company's self-developed product OT-101-S (0.01% and 0.05% atropine sulfate eye drops) has had its Phase III clinical trial application accepted by CDE in China. Accelerated Commercialization Process Provides Strong Support for Sales Revenue on the Sales Side As one of the powerful driving forces for terminal sales, commercialization has also shown remarkable performance for OcuMension in terms of product hospitalization. In 2023, with a complete product pipeline, the company continued to expand hospital coverage and accelerate product hospitalization. Currently, the company has formed a nationwide sales network, covering 1558 tertiary hospitals, with a commercial team of over 230 people. On this basis, the company deeply explores the commercial penetration of strong products such as Shilida and Emidin, achieving rapid growth in sales revenue. In addition, under the full play of national fiscal funds' guiding role in the development of innovative drugs, more approval resources will tilt towards high-value innovative drugs. With the company's increasingly mature commercialization process and the policy-driven tailwind, the company's image in the secondary market, previously underestimated, is expected to change. Within the month, the Hong Kong stock innovative drug sector has seen a full-scale increase, and the company gradually returned to a benign growth track in this round of valuation restoration of Hong Kong stock pharmaceuticals. In the future, driven by multiple factors such as aging, electronic lifestyle, increasing medical awareness among patients, and rising resident payment levels, China's ophthalmic market has tremendous development potential. The company will rely on its first-mover advantage to rapidly enhance its competitiveness and penetration in the domestic market, while actively expanding overseas markets to enhance the company's international influence. By continuously deepening hospital cooperation, optimizing sales network layout, the company will further improve product coverage, providing more patients with high-quality and efficient medical services. Chasing light and encountering, forging ahead. The development of innovative drugs in the field of Chinese ophthalmology is arduous but promising. With the continuous improvement in market recognition of the company's products, OcuMension will continue to uphold the development philosophy of innovation-driven and quality-oriented, continuously strengthen research and development investment, introduce more innovative and competitive products, strive to lead the market, and provide greater returns for investors. SOURCE OcuMension

Phase 3Financial StatementNDA

100 Deals associated with Timolol Maleate

External Link

KEGG	Wiki	ATC	Drug Bank
D00603	Timolol Maleate	S01ED01 C07AA06	DBSALT000989

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Cataract	JP	Wakamoto Pharmaceutical Co., Ltd.	17 Sep 1999
Ocular Hypertension	JP	Wakamoto Pharmaceutical Co., Ltd.	17 Sep 1999
Glaucoma	JP	Santen Pharmaceutical Co., Ltd.	04 Jun 1981
Glaucoma, Open-Angle	US	Bausch & Lomb, Inc.	17 Aug 1978

Developing

10 top R&D records.

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Hemangioma	NDA/BLA	CN	Shanghai Auson Pharmaceuticals Co., Ltd.	01 Nov 2024
Hemangioma	NDA/BLA	CN	Shanghai New Asiatic Pharmaceutical Minhang Co. Ltd.	01 Nov 2024
Capillary Hemangioma	Phase 2	CN	Shanghai Aucta Pharmaceuticals Co. Ltd.	28 Oct 2020

Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


ARVO2021	Not Applicable	Optic Disk Drusen	-	Timolol TM 0.01%	ynrgyasyhv(npoqlrklrm) = djtalgzpmh mlxyzrjqrn (ohmwdjzpzo ) View more	-	01 Jun 2021
NCT03323164 (CTgov)	Phase 4	Glaucoma, Open-Angle \| Low Tension Glaucoma	35	Brimonidine Tartrate (Brimonidine)	hmmeusedlj(dejxqognox) = rqeznmkpxq cuyzopdrci (lscryyqsda, fqvieinmpa - hhegowesru) View more	-	31 Dec 2020
				Timolol Maleate (Timolol)	hmmeusedlj(dejxqognox) = gwzhziexqi cuyzopdrci (lscryyqsda, szbjlltseb - cpioammmmh) View more
LUNAR Study (ARVO2016)	Phase 3	Ocular Hypertension \| Glaucoma, Open-Angle	387	Latanoprostene Bunod 0.024%	nodmjrxoqo(dzwucrxsok) = iexxmkmgjc fkpvwffprd (nqrrwrdltb ) View more	Positive	01 May 2016
				Timolol Maleate 0.5%	nodmjrxoqo(dzwucrxsok) = sygocyzqjp fkpvwffprd (nqrrwrdltb ) View more
ARVO2012	Not Applicable	Glaucoma	-	Xalacom (Latanoprost+Timolol Maleate)	blwarhcdqj(wiutaselge) = wrdxfytdgm azjpxumdev (uyebdztqyc ) View more	-	01 Mar 2012
				Duotrav(Travoprost+Timolol Maleate)	blwarhcdqj(wiutaselge) = zbhixstuzz azjpxumdev (uyebdztqyc ) View more
NCT00735449 (CTgov)	Phase 4	Glaucoma	204	timolol maleate 0.5%+latanoprost 0.005%	ddswqzrtgy(ixunqtsvns) = hubpgfvujq ulqabvrdev (oghzwhyocn, njpaukespi - rwdltmsemn) View more	-	24 Nov 2011
ARVO2008	Not Applicable	-	-	Istalol	dnfibqzasa(hkflqwxage) = beoybvwyxm tuvbpbuupa (dkoofiqxmh ) View more	-	01 May 2008
				Betimol	dnfibqzasa(tkfdfuyecy) = bcqgkbvcep iphhqypjjx (ovaztgyuty ) View more
ARVO2007	Not Applicable	Myopia	32	Topical Timolol Maleate	rsnvlgtwyp(rrmcpbqtku) = yuvjvkunbo qrhoenddqw (mtuatnifts )	-	01 May 2007
Pubmed \| Eur J Ophthalmol	Not Applicable	Ocular Hypertension \| Glaucoma, Open-Angle	-	Timolol Maleate 0.5%	uyiiwlihak(gtwkclqrci) = nldozzgzvq rvibngbfjw (ckloweixyz, +/ - 3.0) View more	Positive	01 Nov 2006
				Brinzolamide 1%	uyiiwlihak(gtwkclqrci) = knlnubbjoj rvibngbfjw (ckloweixyz, +/ - 2.7) View more
ARVO2006	Not Applicable	Ocular Hypertension	-	Timolol Maleate 0.5%	cofvsfoprv(gzqunsfmgq) = aouzuidjry xqbztcxxav (zqzzmrniku, 3.6)	Positive	01 May 2006
				Brinzolamide 1%	cofvsfoprv(gzqunsfmgq) = jijmhjpwpa xqbztcxxav (zqzzmrniku, 3.3)
ARVO2002	Not Applicable	-	11	0.5% Timolol Maleate with Preservative (0.005% Benzalkonium Chloride)	wmkjokkved(mdgdrdfykr) = lhreqsgpcn jjefuiqgug (fnfwhqdlxk ) View more	-	01 Dec 2002
				0.5% Timolol Maleate without Preservative	wmkjokkved(mdgdrdfykr) = vbiyxcytyb jjefuiqgug (fnfwhqdlxk ) View more

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