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timolol (Ophtim / timolol, Thea)

✓ Approved

Takeda · ADRB1 · Small Molecule

What is timolol?

timolol is a small molecule developed by Takeda. It is approved for therapeutic indications via others.

Drug Profile

Brand NamesOphtim, timolol, Thea
CompanyTakeda
Drug ClassSmall Molecule
Molecular TargetADRB1, ADRB2
RouteOthers
StatusApproved
Sources: ClinicalTrials.gov, Takeda

Mechanism of Action

Molecular Targets

timolol acts on 2 molecular targets:

ADRB1adrenoceptor beta 1 (B1AR, RHR)
ADRB2adrenoceptor beta 2 (B2AR, ADRBR)
Want deeper analysis?Noah AI can explain complex mechanisms and compare to similar drugs.

Therapeutic Indications

timolol is developed for 1 unique indication across 1 therapeutic area.

Therapeutic AreaConditionPhase
Eye disordersGlaucoma✓ Approved

Related Research Articles

PubMedPediatric dermatology2026-07-24

A Comprehensive Review of the Current Systemic Medical Treatment Landscape for Vascular Malformations.

Fason Claire C, Jafari Alexander J AJ, Hebert Adelaide A AA

Dermatologists play a central role in the diagnosis and medical management of vascular anomalies. Currently, vascular anomalies are categorized into vascular tumors and vascular malformations. The latest designations for the numerous types of vascular lesions are delineated in the International Society for the Study of Vascular Anomalies website (www.issva.org). The arenas for the therapy for hemangiomas, the most common vascular tumor, have been studied extensively and have been recognized as standard of care by the Society for Pediatric Dermatology, the American Academy of Dermatology and the American Academy of Pediatrics. Options for hemangioma treatment include systemic beta-blockers such as propranolol, atenolol, and nadolol, and the topical beta-blocker timolol. Vascular malformations and overgrowth syndromes encompass a separate set of treatment regimens. Recent pharmacological and technological advances in the medical management of vascular anomalies have decreased the need for surgery in many patients while also leading to improved outcomes and quality of life. This review will guide the dermatologist through the current medical treatment landscape for vascular malformations.

PMID 42492908
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PubMedSeminars in dialysis2026-07-20

Topical Timolol for Peritoneal Dialysis Catheter Exit-Site Granulomas: First Report of Successful Use in CAPD Patients.

S Veenaa Manjari VM, Parthasarathy Rajeevalochana R, N Prashanth P, Saravanan Bhavadharani B et al.

Exit-site granuloma is a frequent and challenging complication in patients undergoing peritoneal dialysis, predisposing to exit-site infections. Recent evidence suggests a potential role for topical timolol in promoting regression of granulomatous tissue. We report two patients on continuous ambulatory peritoneal dialysis who developed exit-site granulomas. Both patients were treated with topical 0.5% timolol maleate ophthalmic solution applied locally to the exit site three times weekly as part of routine exit-site care. Clinical response was monitored using serial photographs. Complete resolution of the granuloma was achieved within 3 weeks in one patient and within 2 months in the other. Neither patient developed local or systemic adverse effects, and no exit-site infections occurred during treatment. Topical 0.5% timolol maleate may represent a safe, non-invasive, and effective treatment option for peritoneal dialysis exit-site granulomas. Larger studies are warranted to establish its efficacy in larger cohorts.

PMID 42472895
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PubMedCurrent drug delivery2026-07-20

Preparation and Characterization of a Low-Molecular-Weight Chitosan Nanoparticle-Based Ocular Formulation for Enhanced Permeation of Timolol Maleate.

Alshweiat Areen A, Emran Sereen Omar SO, Altaani Bashar B, Haddad Razan R

Timolol Maleate (TM) is primarily used to treat glaucoma by reducing intraocular pressure. However, its efficacy is limited by poor ocular bioavailability (<5%) and systemic side effects. This study aimed to develop and evaluate Low-Molecular-Weight Chitosan (LMWC)-based complexes in an eye formulation to sustain TM release and enhance its corneal permeability. TM-LMWC Polyelectrolyte Complexes (PECs) were prepared by ionic interactions between TM and LMWC and characterized for particle size, polydispersity, surface charge, and physicochemical properties. TM Liquid Medicated Nanoparticle Formulations (LMFs) were prepared by the solvent diffusion method, and their dissolution behaviors, release kinetics in simulated tear fluid, and ex vivo permeation through sheep corneas were evaluated. The prepared TM nanoparticles showed a uniform particle size (185-258 nm) and a positive zeta potential exceeding +26 mV, with encapsulation efficiency ranging from 28 to 35%. The formation of a polycationic complex was confirmed by the thermal and structural analyses. The LMFs showed a reduced particle size (65-130 nm). Moreover, the TEM image of LMF 4 revealed a spherical nanoparticle with a smooth surface. Sustained drug release was observed over 24 hours and best fitted to the Korsmeyer-Peppas model, indicating a Fickian diffusion (n < 0.45). Ex vivo studies showed LMF1 increased flux (2.54 ± 0.04 μg cm-2 h-1) and permeation coefficient (0.00987 cm·h⁻¹), representing a 2.62-fold increase in TM permeation. Chitosan molecular weight influenced PEC particle size due to differences in polymer chain length and viscosity. A sustained release of TM from LMFs was observed as TM was entrapped within the chitosan matrix and had to diffuse through the polymer or be released by matrix erosion. The enhanced corneal permeability was attributed to the mucoadhesive properties of the nanoparticles and their interaction with the corneal epithelium. The TM-based nanoparticle formulation enhanced corneal permeation and sustained TM release, offering a promising approach to improve ocular bioavailability and therapeutic efficacy.

PMID 42473223
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PubMedMini reviews in medicinal chemistry2026-07-20

From Chemistry to Clinic: A Review of Latanoprostene Bunod and Its Therapeutic Potential.

Bharati Biswa Deepak BD, Mansuri Rani R, Diwan Anupama A, Kumar Neeraj N et al.

Open-Angle Glaucoma (OAG) is a progressive optic neuropathy and a major cause of irreversible blindness worldwide. Lowering Intraocular Pressure (IOP) remains the most effective approach for slowing disease progression. Latanoprostene bunod (LBN) ophthalmic solution 0.024% (Vyzulta®) is a nitric oxide (NO)-donating prostaglandin analogue developed to enhance aqueous humor drainage through two complementary pathways. Following topical administration, LBN is converted into latanoprost acid and a nitric oxide-releasing metabolite. Latanoprost acid increases uveoscleral outflow, whereas nitric oxide improves conventional outflow by relaxing the trabecular meshwork and Schlemm's canal. Clinical studies have shown that LBN provides significant reductions in IOP in patients with OAG and ocular hypertension. In the phase III APOLLO and LUNAR trials, LBN demonstrated efficacy comparable to, and in some analyses greater than, timolol 0.5%. Long-term data from the JUPITER study further confirmed sustained IOP reduction during 12 months of treatment. LBN is generally well tolerated, with conjunctival hyperemia, mild ocular irritation, and instillation-site discomfort being the most frequently reported adverse events. Beyond its clinical utility, several synthetic approaches have been reported for the preparation of LBN. These include esterification and alkylation strategies involving nitrooxyalkyl derivatives, as well as routes based on bromobutyl intermediates followed by nitrate substitution. Patent literature has further described process improvements aimed at enhancing purity, scalability, and manufacturing efficiency. Overall, current evidence supports LBN as an effective and well-tolerated therapeutic option for patients with OAG or ocular hypertension. Continued improvements in synthetic methodologies may facilitate cost-effective production and broader clinical accessibility.

PMID 42473219
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PubMedAsia-Pacific journal of ophthalmology (Philadelphia, Pa.)2026-07-17

Glaucoma prevalence and prescribing trends in New Zealand: A 10-year study.

Shi Jane J, Singh Vidit V, Nunns Brandon B, Danesh-Meyer Helen H et al.

To evaluate dispensing trends of publicly funded glaucoma medications in New Zealand from 2012 to 2021, and to assess disparities in prescribing across demographic groups. This study provides population-level insights into real-world glaucoma care and treatment equity in a universal healthcare setting. In New Zealand, although limited information exists on prescribing practices, there has been no comprehensive analysis of national dispensing data. This distinction is critical, as dispensing data more accurately reflect medication access, patient uptake, and treatment adherence than prescribing data alone. A retrospective observational study was conducted using de-identified national pharmacy dispensing data from the New Zealand Ministry of Health. Dispensing trends for eleven glaucoma medications were analysed by year, medication, sex, and self-identified ethnicity. Age-adjusted per capita dispensing rates were compared using ANOVA with post-hoc analysis. Over 3 million glaucoma prescriptions were dispensed, representing 27.6% of all ocular medications. The number of treated individuals rose from 39,725 in 2012-50,048 in 2021 (a 25.9% increase), outpacing national population growth. The prevalence of pharmacologically treated glaucoma or ocular hypertension increased from 0.90% in 2012-0.98% in 2021. The annual incidence of newly treated glaucoma was estimated at 125 per 100,000 people per year. Latanoprost was the most frequently dispensed glaucoma medication (40%), followed by timolol (13%) and bimatoprost (11%). Disparities in dispensing patterns were evident. Europeans received 87% of glaucoma prescriptions, Māori and Pasifika peoples, who represent 17.8% and 8.9% of the population, received only 1.9% and 1.4% of glaucoma prescriptions, respectively (p < 0.001), even after adjusting for age. This nationwide study provides the most comprehensive analysis to date of glaucoma medication dispensing in Aotearoa New Zealand, capturing real-world treatment patterns across a ten-year period. It offers critical insight into the treated prevalence and incidence of pharmacologically treated glaucoma and ocular hypertension at a population level. Latanoprost has clearly emerged as the dominant first-line therapy, consistent with international clinical guidelines, followed by Timolol. However, the findings also expose significant inequities: Māori-the Indigenous people of New Zealand-and Pasifika populations remain markedly under-represented among those receiving glaucoma treatment, even after adjusting for age. Further research is needed to understand the underlying reasons for these disparities and to ensure equitable access to glaucoma care for all New Zealanders.

PMID 42462910
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PubMedPediatric dermatology2026-07-16

Topical Sirolimus Therapy for Agminated Pyogenic Granulomas: A Two-Case Report.

Van Matre Stetson S, Hicks Evan E, Richter Gresham T GT, Mack Joana J

Pyogenic granulomas (PGs) are benign vascular tumors that present as rapidly growing, friable papules that often bleed and cause cosmetic disfigurement. PGs generally respond well to treatments such as excision, laser, cryotherapy, topical imiquimod, and topical timolol, but agminated PGs can be distressing to patients and challenging to treat. Topical sirolimus, an mTOR inhibitor, is used in the treatment of other vascular anomalies but has not been previously investigated for use in PGs. We report two patients with agminated PGs who demonstrated improvement in size, color, and bleeding following treatment with topical sirolimus.

PMID 42457560
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