Drug Database
TI

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

PubMedJournal of the Chinese Medical Association : JCMA2026-10-14

Nonselective beta-blockers and hepatic encephalopathy in liver cirrhosis:A meta-analysis of randomized controlled trials.

Kuo Tai-Hui TH, Chen Yu-Jen YJ, Lee Pei-Chang PC, Yang Tsung-Chieh TC et al.

Liver cirrhosis leads to portal hypertension and related complications, including ascites, esophageal varices, and hepatic encephalopathy (HE). Non-selective beta blockers (NSBBs) decrease portal pressure, but it is not yet clear whether they contribute to HE development. Therefore, we examined the association between NSBB therapy and HE in randomized controlled trials (RCTs) involving patients with cirrhosis. We systematically searched PubMed, Web of Science, ScienceDirect, and the Cochrane Library (from inception to December 31, 2024) for RCTs comparing NSBBs with a placebo, endoscopic band ligation, or injection sclerotherapy for variceal bleeding prevention in relation to HE. The risk ratios (RRs) and 95% confidence intervals (CIs) were pooled using a random-effects model. Subgroups were defined according to the comparator, NSBB type, and hepatic function status (weighted mean Child-Pugh score ≤6 vs. >6). The risk of bias was assessed using the revised Cochrane risk-of-bias tool for randomized trials (RoB 2). There were 12 relevant studies, which included 775 NSBB-treated and 771 comparator patients (54 and 57 HE events). NSBB therapy was not associated with a statistically significant change in HE risk (RR 1.04, 95% CI 0.73-1.47; p = 0.84; I² = 0%). Estimates were consistent across all subgroups of hepatic function statuses (compensation, RR 1.18, 0.44-3.14; decompensation, RR 1.02, 0.70-1.48; p = 0.79), comparators (placebo, RR 1.19, 0.79-1.80; endoscopic therapy, RR 0.72, 0.38-1.39; p = 0.20), and NSBB types (propranolol/timolol, RR 1.06, 0.72-1.55; carvedilol, RR 0.95, 0.42-2.15; p = 0.82). Current evidence does not indicate a statistically significant association between NSBB therapy and HE development in patients with cirrhosis, regardless of disease severity.

PMID 42870342
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PubMedActa paediatrica (Oslo, Norway : 1992)2026-10-10

Oral Propranolol Versus Topical Timolol for the Treatment of Infantile Haemangiomas: A Systematic Review and Meta-Analysis of Randomized Controlled Trials.

Weng Liwen L, Zuo Hongli H, Zhao Min M, Dong Jialin J

This systematic review and meta-analysis aimed to compare the efficacy and safety of oral propranolol versus topical timolol for the treatment of superficial infantile haemangiomas. We systematically searched PubMed, Cochrane Library, Embase, Web of Science and China National Knowledge Infrastructure from inception to April 23, 2026. Only randomized controlled trials comparing oral propranolol with topical timolol for superficial infantile haemangiomas were included. Two reviewers independently screened studies, extracted data and assessed risk of bias using the Cochrane risk of bias 2.0 tool. The primary outcomes were overall response rate and incidence of systemic adverse events. Pooled risk ratios (RRs) with 95% confidence intervals (CIs) were calculated using fixed-effect models. Seven randomized controlled trials comprising 428 infants were included. Topical timolol was comparable to oral propranolol in overall response rate (RR = 1.09, 95% CI 0.97-1.23, p = 0.17; I2 = 0%). Topical timolol significantly reduced the risk of systemic adverse events compared with oral propranolol (RR = 0.35, 95% CI 0.20-0.59, p < 0.0001; I2 = 9%). Topical timolol demonstrates comparable efficacy to oral propranolol for superficial infantile haemangiomas and has a significantly superior safety profile with a 65% reduction in systemic adverse events.

PMID 42855991
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PubMedMedicina (Kaunas, Lithuania)2026-09-26

Effect of Latanoprost and Timolol-Dorzolamide Therapy on Aqueous Humor Cytokine Concentrations in Patients with Pseudoexfoliative Glaucoma.

Valković Antić Ivana I, Juranić Lisnić Vanda V, Sotošek Vlatka V, Bertović Ivana I et al.

Background and Objectives: Pseudoexfoliative glaucoma (PEXG) is a secondary glaucoma caused by the deposition of abnormal flaky protein-like material inside the eye, leading to blockage of the drainage system, increased intraocular pressure (IOP), and optic nerve damage. This study aimed to evaluate the effects of latanoprost and timolol-dorzolamide therapy on the concentrations of interleukin (IL)-1β, IL-6, IL-8, IL-10, IL-12p70, and tumor necrosis factor-alpha (TNF-α) in the aqueous humor and serum samples of patients with PEXG. Materials and Methods: This prospective observational study included 60 patients allocated to three age-matched groups (n = 20 per group). Group 1 received latanoprost therapy, Group 2 received timolol-dorzolamide therapy, and Group 3 comprised patients with cataracts without PEXG who were not receiving antiglaucoma medication (control group). All participants underwent a comprehensive ophthalmological examination, including visual acuity assessment, specular microscopy, IOP measurement, and intraocular lens (IOL) measurement. Peripheral venous blood was taken from each patient before the surgical procedure and aqueous humor samples were collected during cataract surgery. Concentrations of IL-1β, IL-6, IL-8, IL-10, IL-12p70, and TNF-α were determined using a Cytometric Bead Array and flow cytometry. Results: No significant differences were observed in the aqueous humor and serum concentrations of IL-6 and IL-8 between the treatment groups, while IL-1β, IL-10, IL-12p70, and TNF-α did not reach detection. A significant positive correlation was found between IOL and aqueous humor IL-6 concentration in group 1 and between IL-6 and IL-8 serum concentration and IOP in controls. Conclusions: Latanoprost and timolol-dorzolamide therapy were not associated with significant differences in aqueous humor or serum IL-6 and IL-8 concentrations in patients with PEXG. IL-1β, IL-10, IL-12p70, and TNF-α were not detectable in the analyzed samples. These findings support the presence of low-grade inflammation in patients with PEXG that does not differ according to the therapy administered. Corneal endothelial alterations are disease-related rather than treatment-induced.

PMID 42796240
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PubMedMedicina (Kaunas, Lithuania)2026-09-26

Ocular Surface Symptoms, Objective Redness, and Intraocular Pressure After a Switch from Fixed Dorzolamide/Timolol to Netarsudil in Latanoprost-Treated Glaucoma and Ocular Hypertension: A Prospective Real-World Cohort Study.

Zanutigh Virginia V, Logioco Celina C, Galetto Leila L, Perrone Franco F et al.

Background and Objectives: Conjunctival hyperemia is common with netarsudil, but redness may not reflect the overall patient experience when treatment burden is reduced. We evaluated ocular surface symptoms, objective redness, tear-film parameters, intraocular pressure (IOP), and treatment preference after a routine-care switch from twice-daily fixed dorzolamide/timolol to once-daily netarsudil 0.02%, while continuing latanoprost. Materials and Methods: This prospective, single-center observational cohort included 30 consecutive adults with primary open-angle glaucoma or ocular hypertension and controlled IOP. Outcomes were assessed at baseline and months 1 and 2. The primary outcome was the Ocular Surface Disease Index (OSDI). Continuous eye-level outcomes were analyzed using mixed-effects models accounting for fellow-eye and repeated-measures correlation; grade ≥ 2 hyperemia was analyzed using participant-clustered logistic regression. Results: Twenty-seven participants (54 eyes) completed evaluable 2-month follow-up. Median OSDI decreased from 7.50 at baseline to 6.25 at month 1 and 5.00 at month 2 (Friedman p = 0.0015). The mean baseline-to-month 2 change was -2.95 points (95% CI, -4.80 to -1.10), and 6/27 participants (22.2%) improved by at least 7 points. Serle grade ≥ 2 hyperemia increased from 7.4% of eyes at baseline to 51.9% at month 1 and 44.4% at month 2. Estimated mean bulbar redness index increased from 1.57 to 2.14 (p < 0.0001), tear meniscus height increased modestly, and non-invasive keratograph break-up time showed no significant longitudinal change. Estimated mean IOP changed from 14.50 to 13.65 mmHg (p = 0.0083), with no eye showing an increase of at least 4 mmHg. Burning improved after multiplicity adjustment, and 17/27 participants with available month-2 preference data (63.0%) preferred netarsudil. Conclusions: The switch was associated with modest OSDI improvement and maintained short-term IOP control despite increased objective redness. Patient preference appeared to reflect factors beyond redness alone.

PMID 42796375
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PubMedMedicine2026-09-26

Concomitant limaprost use and intraocular pressure response to latanoprost in normal-tension glaucoma: A retrospective cohort study.

Bae Heewon H, Kang Tae Gu TG

Normal-tension glaucoma (NTG) is a progressive optic neuropathy in which intraocular pressure (IOP) reduction is important for limiting disease progression. Latanoprost is commonly used as first-line therapy, but treatment response varies. We investigated whether concomitant oral limaprost use was associated with the IOP response to latanoprost in patients with NTG. We retrospectively reviewed patients with NTG treated between January 2015 and August 2021 at the Veterans Health Service Medical Center. The final matched cohort included 446 patients: 223 patients receiving latanoprost with concomitant limaprost and 223 age- and sex-matched controls receiving latanoprost alone. Three-month IOP was analyzed at the patient level.Multivariable linear regression was performed with 3-month IOP as the outcome, adjusting for baseline IOP, age, sex, nonsteroidal anti-inflammatory drug use, systemic beta-blocker use, diabetes, and hypertension. Baseline IOP was similar between groups. The median IOP reduction at 3 months was 1.0 mm Hg [interquartile range (IQR), -0.5 to 2.5] in the limaprost group and 2.0 mm Hg [IQR, 0.5-3.0] in controls. In the adjusted analysis, concomitant limaprost use was associated with a 0.91-mm Hg higher IOP at 3 months (95% confidence interval, 0.54 to 1.27; P < .001). In a secondary exploratory subgroup of 63 patients who subsequently received add-on dorzolamide/timolol, 35 were in the limaprost group and 28 were controls; no statistically significant between-group difference in IOP reduction was detected. Concomitant limaprost use was associated with a modestly smaller observed IOP reduction after latanoprost treatment in patients with NTG. Because of the retrospective design and the modest magnitude of the association, prospective studies are needed to determine whether a clinically meaningful pharmacologic interaction exists.

PMID 42798066
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PubMedFrontiers in pharmacology2026-09-24

Comparative efficacy and safety of pharmacologic, laser, and combination therapies for infantile hemangioma: a systematic review and network meta-analysis with evidence certainty assessment.

Kong Mingxuan M, Zhang Shijie S, Ren Dan D, Chang Jian J

Infantile hemangiomas (IH) are the most common childhood vascular tumors, potentially complicated by ulceration and permanent functional or aesthetic sequelae. Current treatments include corticosteroids, β-blockers, and lasers, among others, existing evidence relies predominantly on direct pairwise comparisons. Consequently, the relative benefits and risks across these modalities remain inadequately defined. We conducted a systematic review and network meta-analysis (NMA) evaluating pharmacologic, laser, and combination therapies for IH to establish treatment hierarchies and inform clinical practice and future guidelines. Following a PROSPERO-registered protocol (CRD420261388356), we searched PubMed, Embase, the Cochrane Library, and Web of Science from inception to 1 March 2026, for randomized controlled trials comparing various interventions for IH. The primary endpoint was excellent response rate. Secondary outcomes included other response rates, VAS/HAS changes, healing time, treatment emergent adverse events, and recurrence. After independent risk-of-bias assessment (RoB2) and data extraction, we performed a random-effects NMA. Treatments were ranked using SUCRA probabilities, and evidence certainty was appraised via GRADE and CINeMA. The synthesis comprised 25 trials (2044 patients) evaluating 16 distinct interventions. Risk of bias was low in six trials, raised "some concerns" in 14, and high in 5. Overall, the evidence body was of moderate certainty. Regarding the primary endpoint, intralesional bleomycin combined with oral propranolol yielded significantly higher excellent response rates than oral propranolol alone (RR = 1.55, 95% CI 1.28-1.89; high certainty). Topical timolol with intralesional lauromacrogol (RR = 7.98, 95% CI 1.52-41.79) and oral propranolol with corticosteroids (RR = 2.00, 95% CI 1.03-3.88) showed higher excellent response rates, supported by moderate-certainty evidence. No statistically significant differences in adverse-event incidence were detected across evaluated regimens, but the safety data were limited. Oral atenolol was associated with numerically lower recurrence rates compared to oral propranolol, but the difference did not reach statistical significance (RR = 0.64, 95% CI 0.32-1.28; moderate certainty). Oral propranolol remains the standard of care for IH. However, our analysis shows that some combination regimens showed favorable efficacy for excellent clinical response. Still, sparse comparative data and low-certainty evidence currently obscure the optimal combination strategy. Defining precise risk-benefit profiles requires rigorous head-to-head trials utilizing uniform outcome measures. https://www.crd.york.ac.uk/PROSPERO/view/CRD420261388356; Identifier: CRD420261388356.

PMID 42780340
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