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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

PubMedAmerican journal of physiology. Regulatory, integrative and comparative physiology2026-05-11

Intracardiac neuromodulation of pacemaker rate in the adult zebrafish heart in vitro.

O'Shea Keegan P D KPD, Long Zachary D ZD, Smith Frank M FM

Heart rate (HR) in vertebrates is determined by the discharge frequency of cardiac pacemaker cells, which are innervated by the autonomic nervous system. The portion of this system located within the heart, the intracardiac nervous system (ICNS), transmits impulses to cardiac effectors for control of cardiac output. Central autonomic neurons modulate the heart through sympathetic (acceleratory) and parasympathetic (inhibitory) axons in the vagosympathetic trunks. In the classical model of cardiac control, the balance between sympathetic and parasympathetic efferent signals determines HR. Recent evidence of spontaneous neural activity within the ICNS in isolated hearts suggests a local regulatory element incardiac control. We examined the potential for ICNS modulation of HR in the isolated zebrafish heart, using atropine to block parasympathetic drive to the pacemaker, and timolol to block sympathetic drive. Atropine (3, 10, 30 µM) evoked tachycardia of similar magnitude at 22 and 28 ° C. Timolol (3, 10 and 30 µM) caused bradycardia at both temperatures, with greater proportional HR responses to all doses at the higher temperature. Our results suggest that both sympathetic and parasympathetic outputs from the ICNS influence the pacemaker, with the degree of sympathetic drive being temperature-sensitive. Intrinsic HR, obtained after dual antagonist application, was not significantly different from HR before drug application so the effects of sympathetic and parasympathetic drive on pacemaker rate appeared to be evenly balanced. We propose that the ICNS in the isolated zebrafish heart is capable of modulating HR in the absence of extracardiac autonomic inputs.

PMID 42113566
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PubMedCureus2026-05-11

Importance of History in the Management of New-Onset Hyperkalemia.

Kagan Igor I, Sarmosyan Kristine K, Lei Sean S, Hwang Michelle M

Hyperkalemia is a life-threatening disorder with a multitude of causes. We present a case of a 64-year-old woman with new-onset hyperkalemia. A patient with a documented history of normokalemia developed consistent hyperkalemia on repeat blood testing. The patient was initially managed by her primary care physician, then referred to nephrology for persistent hyperkalemia, at which point sodium polystyrene sulfonate was initiated. The patient presented for a second opinion on the hyperkalemia, and after a thorough history and chart review, it was determined that the patient's dorzolamide-timolol eye drops were the cause of the hyperkalemia. Discontinuation of the eye drops resolved the hyperkalemia.

PMID 42110035
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PubMedDermatology and therapy2026-05-10

Therapies for Infantile Haemangiomas: Current Practice and Evolving Perspectives.

Nolan B B, O'Connor C C

Infantile haemangiomas (IH) are the most common vascular tumours of infancy, characterised by a predictable trajectory of rapid proliferation, plateau, and slow spontaneous involution. Although most regress uneventfully, a significant minority risk ulceration, functional compromise, or disfigurement, and therefore require timely intervention. The therapeutic landscape was once dominated by corticosteroids, interferon, and cytotoxic chemotherapeutics of modest efficacy and considerable toxicity. Management was revolutionized in 2008 by the discovery that the beta-blocker propranolol induced prompt and sustained regression. Propranolol has since become the established first-line therapy for IH, with efficacy and safety confirmed by randomized controlled trials and corroborated by observational cohorts. Mechanistically there are multiple temporally stratified actions: immediate vasoconstriction, suppression of angiogenic signalling pathways, induction of endothelial apoptosis, and ultimately the promotion of adipogenic differentiation in keeping with natural involution. Safety is favourable under expert supervision, though hypoglycemia remains the principal preventable hazard, necessitating caregiver education on feeding regimens and "sick day" rules. Rebound growth, encountered in roughly one-fifth of cases, usually responds to re-treatment. Alternative beta-blockers such as atenolol and nadolol provide comparable efficacy with potential advantages in tolerability or dosing convenience. Topical timolol has limited effectiveness for small superficial lesions, while sirolimus, becaplermin gel, laser devices, and surgery may have circumscribed adjunctive roles. Corticosteroids and cytotoxic agents are now confined to salvage use. Contemporary perspectives extend beyond pharmacology to encompass caregiver experience and health-system burden. Recent work highlights the low burden of treatment with propranolol, while digital innovations such as photo-triage during the COVID-19 pandemic illustrate opportunities to reduce healthcare exposure and improve equity of access. This review describes the evolution of drug therapy for IH and integrates mechanistic insights, clinical pragmatism, and patient-centred innovations to chart the current trajectory of care.

PMID 42105055
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PubMedSurvey of ophthalmology2026-05-09

The role of adjunctive aqueous suppressants for anti-vascular endothelial growth factor therapy: A systematic review.

Sadek Kareem K, Yu Philip P, Al-Burak Salem Abu SA, Osman Rahma R et al.

Our goal is to determine whether adjunctive aqueous suppressants (topical β-blockers, carbonic anhydrase inhibitors, or oral acetazolamide) enhance outcomes of anti-vascular endothelial growth factor (anti-VEGF) therapy for diabetic macular edema (DME), retinal vein occlusion (RVO), and neovascular age-related macular degeneration (nAMD), focusing on retinal thickness, visual acuity, injection burden, intraocular pressure (IOP), and safety. DME, RVO, and nAMD are leading causes of vision loss treated with repeated intravitreal injections, yet many eyes show persistent fluid. Aqueous suppressants are inexpensive and widely available, with potential to prolong intravitreal drug residence and improve outcomes, but their clinical value remains uncertain. Following a registered protocol, we searched 4 databases (January, 2000 toMay, 2025) for randomized and comparative studies evaluating adjunct aqueous suppressants with anti-VEGF therapy. Primary outcome was change in retinal thickness; secondary outcomes included visual acuity, injection burden, IOP, and adverse events. Risk of bias was assessed and findings synthesized narratively. Twelve studies (7 randomized trials; 495 eyes) met inclusion criteria. In DME, 3 of 4 trials showed greater thickness reduction with adjunctive dorzolamide (±timolol), although visual gains were inconsistent. In RVO, 1 trial suggested transient anatomical benefit, whereas oral acetazolamide showed no added effect. In nAMD, adjunctive dorzolamide-timolol reduced residual fluid in refractory cases without visual or treatment-sparing benefit. Topical therapy produced modest IOP reductions without serious adverse events. Adjunct aqueous suppressants may provide limited short-term anatomical benefit, particularly in DME and refractory nAMD, but consistent functional or durability effects are not found in this study. Larger, longer-term randomized studies are needed.

PMID 42103030
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PubMedFrontiers in gastroenterology (Lausanne, Switzerland)2026-05-04

Primary prevention in liver cirrhosis patients with esophageal varicesa: a systematic review and network meta-analysis.

Li Feng F, Zhang Xiaoyi- X, Chi Jia-Li JL, Zhang Xuemei X et al.

To compare the efficacy and safety of different primary preventive measures for esophageal variceal bleeding using a network meta-analysis. Randomized controlled trials (RCTs) on primary prevention were retrieved from PubMed, Cochrane Library, Embase, and Web of Science. Primary outcomes were the incidence of variceal bleeding, all-cause mortality, All-Cause Bleeding and Bleeding-Related Mortality. Secondary outcomes included adverse events and other decompensation events. Study quality was assessed with the Cochrane Risk of Bias tool. Data were analyzed using Revman 5.4 and Stata 16.0. A total of 50 RCTs (6510 patients) evaluating 16 interventions were included. For reducing bleeding incidence, the combinations Midodrine + Propranolol (Mido+PPL), Carvedilol + Endoscopic Variceal Band Ligation (Carv+EVBL), and Fuzheng Huayu Capsule + Propranolol (FZHYJN+PPL) were superior. For lower all-cause mortality, Carv+EVBL, Mido+PPL, and Nadolol + Isosorbide Mononitrate (Nado+ISMN) were favorable. Carv+EVBL, EVBL, and Endoscopic Injection Sclerotherapy (EIS) were better for reducing bleeding-related mortality. Regarding safety, Mido+PPL, Nadolol (Nado), and Carvedilol (Carv) had fewer general adverse events, while Isosorbide Mononitrate (ISMN), Mido+PPL, and Carv had lower rates of other decompensation events. Based on low-certainty evidence, Mido+PPL demonstrated a favorable balance of efficacy and safety and is recommended as a preferred option. Mido+PPL, Carv+EVBL, and FZHYJN+PPL are recommended for primary prophylaxis in cirrhosis. For Child-Pugh A/B patients, Mido+PPL, Carv+EVBL, and FZHYJN+PPL are suggested, with EVBL as an alternative for those intolerant to drugs. EVBL may be considered for Child-Pugh C patients. Mido+PPL is recommended for prophylaxis within one year, FZHYJN+PPL for up to two years, and Carvedilol (alone or with EVBL) for long-term management beyond two years. Carvedilol and Propranolol showed superior net clinical benefit over Nadolol and Timolol. Although Nadolol (alone or with ISMN) may reduce mortality, its higher adverse event rate precludes it as a first-line strategy. FZHYJN, while effective, may increase the risk of other decompensation events.

PMID 42077388
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PubMedThe Journal of dermatology2026-04-27

Efficacy of 0.5% Timolol Maleate Eye Drops for the Treatment of Facial Rosacea: A Randomized, Triple-Blind, Placebo-Controlled Clinical Trial.

Moradi Ali A, Shakoei Safoura S, Hamzelou Shahin S, Nasimi Maryam M et al.

Rosacea is a chronic skin condition with limited effective and well-tolerated treatment options. This study investigated the efficacy of 0.5% timolol maleate eye drops in treating facial rosacea lesions. A randomized, triple-blind, placebo-controlled clinical trial was conducted at Razi Hospital in Tehran, involving 42 participants diagnosed with erythematotelangiectatic rosacea (ETR). Participants were randomized to receive either 0.5% timolol maleate eye drops or a placebo (distilled water) administered once daily for 4 weeks. The participants were evaluated in three visits (at baseline, after 4 weeks of treatment, and 4 weeks after stopping treatment) using a Mexameter MX18 device (for lightness and erythema), Clinician Erythema Assessment Scale (CEA), Global Flushing Severity Score (GFSS), Patient Self-Assessment (PSA), and Visioface device (for ΔL and ΔE criteria). The primary outcome was the change in erythema severity, assessed by the Mexameter MX18 device. The timolol group significantly reduced Erythema Index (p  <  0.001) and other secondary outcomes, including CEA, PSA, and GFSS. No significant adverse effects were reported. In addition, MANOVA revealed a significant time × group interaction across outcomes, indicating that the pattern of changes over time was significantly different between the intervention and placebo groups. This study provides preliminary evidence that 0.5% timolol eye drops could be an effective and well-tolerated treatment for facial rosacea. However, the small sample size and short follow-up duration limited our results.

PMID 42041192
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