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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

PubMedGenes2026-08-27

Exploratory Analysis of Glaucoma-Associated SNPs in a Colombian Cohort Highlights Potential Involvement of Oxidative, Vascular, and Neurodegenerative Pathways.

Casanova Carlos C, Valencia-Peña Claudia C, Saldarriaga-Gil Wilmar W, Lozano-Cruz Edgar E et al.

Primary open-angle glaucoma (POAG) is a complex multifactorial optic neuropathy involving genetic, vascular, oxidative, inflammatory, and neurodegenerative mechanisms. Despite advances in genome-wide studies, the contribution of genetic variants remains incompletely characterized in underrepresented Latin American populations. This study aimed to characterize the genetic landscape of POAG in a Colombian cohort by identifying previously reported glaucoma-associated variants, rare candidate variants, and pharmacogenomic markers and integrating these findings into biologically relevant pathways. An exploratory descriptive study was conducted in 21 Colombian patients with confirmed POAG. Whole-exome sequencing (WES) was performed at an average sequencing depth of approximately 100×. Variants were quality-filtered, functionally annotated, and prioritized within 446 POAG-associated genes retrieved from DisGeNET. Previously reported glaucoma-associated variants and rare candidate variants were identified, while pharmacogenomic variants related to latanoprost and timolol response were evaluated using ClinPGx/PharmGKB. Identified genes were classified according to major biological pathways relevant to glaucoma pathophysiology. Of the 446 POAG-associated genes, 381 were detected in the patients' exomes. A total of 10,220 molecular variants were identified, of which 1,187 synonymous variants were excluded, leaving 9,033 variants for downstream analysis. Among these, 955 were non-synonymous SNVs, including 26 variants previously reported in association with glaucoma and 929 potentially novel coding variants. Previously reported variants included loci in SIX6, LOXL1, CYP1B1, NOS3, and SOD2. Two rare candidate variants (minor allele frequency <1%) were identified in FMNL2 and C3. Pharmacogenomic variants in PTGS1, ADRB1, and ABCC4 with potential implications for response to latanoprost or timolol were also detected. Functional integration highlighted pathways involving oxidative stress, extracellular matrix remodeling, vascular regulation, neurodegeneration, and inflammation. This exploratory analysis identifies known glaucoma-associated variants, rare candidate variants, and pharmacogenomic markers in Colombian patients with POAG. The findings support a multifactorial biological framework involving interconnected oxidative, structural, vascular, neurodegenerative, and inflammatory pathways. The FMNL2 and C3 variants represent candidates for further investigation, while the identified pharmacogenomic variants highlight the potential relevance of genomic profiling for personalized glaucoma management. Larger ancestry-informed case-control studies are required to validate these observations and determine their clinical significance.

PMID 42650112
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PubMedNaunyn-Schmiedeberg's archives of pharmacology2026-08-11

Can pilocarpine effectively and safely manage glaucoma in the modern era? A systematic review and meta-analysis.

Chen Kai-Yang KY, Chan Hoi-Chun HC, Chan Chi-Ming CM

This study systematically evaluates the efficacy, safety, tolerability, and contemporary clinical positioning of topical pilocarpine in the management of glaucoma and ocular hypertension. This systematic review and meta-analysis followed the Preferred Reporting Items for Systematic Reviews and Meta-Analyses (PRISMA) 2020 guidelines. PubMed/MEDLINE, EMBASE, Cochrane CENTRAL via the Cochrane Library, Scopus, Web of Science Core Collection, and Google Scholar were searched from inception to 1 May 2026 without language restrictions. Randomized controlled trials and controlled observational studies in adults with glaucoma or ocular hypertension were eligible when topical pilocarpine, used alone or in combination, was compared with placebo, no treatment, laser trabeculoplasty, or other intraocular pressure (IOP)-lowering therapies. The primary outcome was mean change in IOP, and secondary outcomes included responder outcomes, ocular adverse events, discontinuation, visual field outcomes, medication burden, post-laser pressure spikes, and postoperative outcomes. Risk of bias was assessed with the Cochrane Risk of Bias 2.0 tool (RoB 2.0) for randomized studies and the Risk of Bias in Nonrandomized Studies of Interventions (ROBINS-I) tool for nonrandomized studies. We performed random-effects meta-analysis using raw mean difference in mmHg for continuous outcomes and risk ratio (RR) for binary safety outcomes, each reported with a 95% confidence interval (CI); certainty of evidence was assessed using the Grading of Recommendations Assessment, Development and Evaluation (GRADE) approach. Of the 38 studies that met the inclusion criteria, 34 contributed data to the quantitative meta-analysis. In the primary analysis, pilocarpine-containing regimens reduced IOP by an additional 1.16 mmHg compared to all comparators (95% CI 0.84 to 1.47; P < 0.001; I2 = 50.7%). Subgroup analyses suggested larger pooled effects in placebo/no-treatment comparisons, ocular hypertension, primary open-angle glaucoma, and monotherapy studies; however, comparisons with beta-blockers and prostaglandin analogs require cautious interpretation because several large individual trials favored timolol or latanoprost for daily clinical use, tolerability, or dosing convenience. Pilocarpine was associated with a sevenfold higher risk of blurred vision (RR 7.33; 95% CI 3.30 to 16.29) and a sixfold higher risk of discontinuation due to adverse events (RR 6.07; 95% CI 3.69 to 10.00). Egger's test pointed to funnel plot asymmetry (P = 0.003), although the trim and fill method did not impute any missing studies. Pilocarpine lowers IOP effectively, but its modern role is limited by frequent dosing, miosis, blurred vision, accommodative symptoms, brow ache, and higher discontinuation. In current glaucoma care, prostaglandin analogs and selective laser trabeculoplasty are generally more consistent with first-line open-angle glaucoma management, whereas pilocarpine is better positioned for selected clinical scenarios, including angle-closure mechanisms, post-laser pressure-spike prophylaxis, selected postoperative angle-surgery settings, intolerance or nonresponse to other drug classes, and resource-limited settings where newer therapies are unavailable or unaffordable.

PMID 42578995
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PubMedInternational journal of pharmaceutics: X2026-08-10

Liposomal Gel for enhancing topical efficacy of timolol maleate against proliferating superficial infantile hemangiomas.

Hang Xiaoxing X, Jin Taiwei T, Hua Jun J, Zhang Xuenong X et al.

Conventional timolol maleate (TM) eye drops are limited by low transdermal bioavailability and short dermal residence time for the treatment of superficial infantile hemangioma (IH). To address this, a novel 0.5% TM-loaded liposomal gel (TM-lipogel) was developed by embedding optimized liposomes within a carbomer gel matrix. The TM-liposomes exhibited a desirable particle size of 139.5 ± 2.1 nm, a polydispersity index (PDI) of 0.051, a zeta potential of -38.7 mV, and an encapsulation efficiency of 64.76 ± 3.2%. Ex vivo permeation studies revealed a 1.9-fold increase in cumulative transdermal delivery compared to the TM-gel, and 4-fold compared to the TM solution (p < 0.05). Furthermore, confocal laser scanning microscope imaging revealed that TM-lipogel achieved a penetration depth of 400 μm, while the TM-gel and TM-eyedrop only reached 200 μm and 75 μm, respectively, highlighting the superior penetration of the liposomal gel. In a murine xenograft hemangioma model, 0.5% TM-lipogel achieved superior tumor regression (81.09%, p < 0.01 vs.control) compared to 0.5% TM-eyedrop (29.85%) and 0.5% TM-gel (61.69%) by simultaneously downregulating HIF-1α, VEGF, MMP-9 and eNOS. Critically, the optimized formulation exhibited no skin irritation and no systemic toxicity. These findings highlight that the TM-lipogel provides enhanced transdermal delivery with deeper tissue penetration, representing a highly effective and safe transdermal strategy for IH therapy.

PMID 42572560
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PubMedInternational journal of clinical pharmacy2026-08-08

Medicine shortages and glaucoma care: a time-series analysis indicating population-level consequences of a national timolol eye drop shortage.

Fawcett Erin E, Ellett Lisa Kalisch LK, Sarin Simi S, Haines Cassandra C et al.

Medicine shortages can disrupt glaucoma management and necessitate therapeutic substitution. Understanding how shortages affect access to first-line treatments for glaucoma is important for optometrists when monitoring intraocular pressure control, and pharmacists when counselling patients and coordinating care during periods of limited medicine availability. Timolol, a non-selective beta-blocker, is a first-line treatment for glaucoma and ocular hypertension and has experienced international shortages in recent years. Between August 2024 and May 2025, Australia experienced a nationwide shortage of timolol-containing eye drops, raising concerns regarding continuity of care, access to treatment, and therapeutic substitution. To descriptively examine the impact of the 2024-2025 timolol eye drop shortage on dispensing patterns of antiglaucoma medicines in Australia and assess the contribution of imported products in mitigating the shortage. A retrospective drug utilisation study was conducted using publicly available aggregate Pharmaceutical Benefits Scheme (PBS) and Repatriation PBS dispensing data from January 2020 to August 2025. Monthly dispensings of antiglaucoma preparations (ATC S01E) were standardised per 100,000 population and analysed using descriptive time-series methods. Dispensing trends were compared before, during, and after the shortage, with stratification by timolol formulation, therapeutic class, and product type (locally supplied versus overseas imports). The late 2024 and early 2025 timolol shortage was associated with a sustained decline in dispensing of single-ingredient extended-release timolol, decreasing from approximately 40 dispensings per 100,000 population per month before the shortage to 1.07 by March 2025. Dispensing of standard-release timolol increased temporarily in October 2024 before declining in a similar pattern. Overseas imports accounted for 24.3% of all timolol dispensings during the shortage period and peaked at 87% of timolol dispensings in March 2025. Despite regulatory approval of imported products, overall timolol utilisation remained below pre-shortage levels. Alternative therapeutic classes, including prostaglandin analogues and carbonic anhydrase inhibitors, showed modest increases in dispensing, suggesting potentially limited therapeutic substitution. The timolol shortage disrupted access to a cornerstone first-line treatment for glaucoma. Regulatory intervention through the approval of imported products partially mitigated the shortage but did not restore utilisation to pre-shortage levels in Australia. Future shortage management strategies should prioritise rapid policy activation and closer alignment of imported products with formulations routinely available in Australia.

PMID 42570054
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PubMedCase reports in ophthalmological medicine2026-07-31

Choroidal Detachment in a Patient on a CPAP Therapy.

Żurowska Emilia E, Zwolińska Emilia E, Rospond-Kubiak Iwona I

The aim of the study is to present a rare case of choroidal detachment in a patient on continuous positive airway pressure (CPAP) therapy. A 76-year-old man on CPAP therapy due to obstructive sleep apnea presented to the ocular oncology clinic with a suspicion of an intraocular tumor. He complained of tunnel vision in red, floaters and flashes in the visual field, and irritation of the left eye since 13 weeks. On initial assessment, the best corrected visual acuity (BCVA) of the left eye was 1.0, and the intraocular pressure (IOP) was 21 mmHg. The examination revealed dilated, tortuous episcleral vessels and a massive choroidal effusion. The patient was diagnosed with choroidal detachment and was treated with topical dexamethasone 0.1% and cyclopentolate. On a follow-up visit 3 weeks later, the BCVA got worse to hand movements and IOP increased to 27 mmHg. The patient received a combination of dorzolamide and timolol in addition to the aforementioned treatment. Over the following 16 weeks, a gradual resolution of the choroidal detachment was documented. The CPAP treatment is a possible, though unproven, contributor to the choroidal detachment. The patient improved during corticosteroid, cycloplegic, and IOP-lowering treatment.

PMID 42534308
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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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