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

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 to 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 to 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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PubMedThe Journal of dermatology2026-07-14

Topical β-Blocker as a Novel Treatment Option for Periungual Pyogenic Granuloma: A Retrospective Study of Lesion Size Reduction and Pain Improvement.

Watanabe Yoshinori Y, Ogawa-Tominaga Minako M, Katsuta Michie M, Dekio Itaru I et al.

Periungual pyogenic granuloma (PG) is a benign reactive vascular lesion commonly associated with trauma and/or drug exposure, including anticancer therapies such as epidermal growth factor receptor (EGFR) inhibitors and other targeted agents. These lesions often cause pain, bleeding, and functional impairment, and may lead to interruption or dose reduction of relevant anticancer treatment. However, there remains a need for effective and noninvasive treatment options that can be easily administered in clinical practice. This study aimed to evaluate the clinical effectiveness and safety of topical timolol in patients with periungual PG. A total of 12 patients were treated with topical timolol 0.5% applied twice daily. Clinical outcomes, including lesion size, pain visual analog scale (VAS), and Dermatology Life Quality Index (DLQI), were assessed at baseline, Week 4, and Week 8. Lesion size decreased significantly over time (p = 0.003), with a significant reduction observed at Week 8 compared with baseline (p = 0.002), corresponding to a mean reduction of 60.3% at week 8. Pain VAS significantly improved at both Week 4 (p = 0.043) and Week 8 (p < 0.001), with a mean reduction of 65.5% at Week 8 compared with baseline. DLQI also improved but did not show a statistically significant change. No significant adverse events, including significant changes in blood pressure or heart rate, were observed. In conclusion, the study suggests that topical timolol is a safe and effective treatment for periungual PG, making it a valuable supportive care strategy for patients undergoing anticancer therapy.

PMID 42444061
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PubMedBMC nephrology2026-07-07

Severe metabolic acidosis with renal tubular acidosis features attributed to topical brinzolamide in a patient with stage 3 chronic kidney disease: a case report.

Chao Ming-Yuan Victor MV, Wang Yi-Chun YC

Metabolic acidosis is common in chronic kidney disease (CKD). However, when the severity of acidosis is disproportionate to renal dysfunction, exogenous causes must be excluded. Topical carbonic anhydrase inhibitors (CAIs) used for glaucoma are commonly perceived as locally acting; in patients with normal renal function their plasma free-drug concentrations are far below those required for systemic effects. In CKD, however, reduced clearance and reduced renal acid-excretory reserve can unmask systemic toxicity. Individual recognition of the syndrome remains uncommon at the bedside, particularly when it presents in the context of acute-on-chronic kidney injury, where its laboratory features can be obscured by acute kidney injury(AKI)-related acidosis. A 73-year-old Asian male with stage 3 CKD and glaucoma presented with progressive dyspnea, anorexia, and a 3-kg weight loss one month after starting fixed-combination brinzolamide 1% / timolol 0.5% eye drops. Laboratory evaluation revealed severe metabolic acidosis (pH 7.29; serum bicarbonate 8.9 mmol/L, from a pre-exposure baseline of 20.3 mmol/L) and acute-on-chronic kidney injury (creatinine 3.9 mg/dL versus baseline ~ 2.0 mg/dL). The disturbance was mixed: a delta-delta ratio of 0.42 (calculated using a reference normal serum bicarbonate of 24 mmol/L) indicated a substantial non-anion-gap (hyperchloremic) component superimposed on a smaller high-anion-gap component, with hypokalemia (K+ 3.3 mmol/L), hyperchloremia (Cl- 107 mmol/L), positive urine anion gap (+ 33.4 mmol/L), and a fractional excretion of bicarbonate of 4.3% measured during established acidosis (without bicarbonate loading). Other causes of metabolic acidosis were systematically excluded. Causality assessment by the Naranjo Adverse Drug Reaction Probability Scale yielded a score of 7 (probable). Discontinuation of the ophthalmic solution and alkali therapy resulted in the resolution of acidosis and recovery of renal function to baseline within one week, sustained at one-year follow-up. Topical CAIs can undergo significant systemic absorption, bypassing first-pass metabolism, and precipitate life-threatening acidosis in patients with reduced renal reserve. Clinicians must maintain a high index of suspicion for ophthalmic medications as hidden causes of mixed acid-base disorders in patients with CKD.

PMID 42410525
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PubMedJournal of AOAC International2026-06-25

ICRF-Assisted Box-Behnken Design and Optimization for Rapid UPLC-PDA Determination of Dorzolamide Hydrochloride and Timolol Maleate in an Ophthalmic Preparation.

Dinç Erdal E, Büker Eda E

Simultaneous optimization of chromatographic resolution and analysis time constitutes a significant analytical challenge in multicomponent pharmaceutical analysis, as resolution-driven optimization strategies may improve peak separation without providing explicit control over retention time, often resulting in unnecessarily prolonged runtimes. To address this limitation, an optimization strategy based on a Box-Behnken experimental design was implemented in conjunction with the Improved Chromatographic Response Function (ICRF), which integrates separation quality and analysis time within a single mathematical objective function. This strategy describes the development of a rapid, chemometrically optimized UPLC-PDA method for the simultaneous determination of dorzolamide hydrochloride (DH) and timolol maleate (TI) in a commercial ophthalmic preparation. A Box-Behnken experimental design and optimization approach was employed in combination with an Improved Chromatographic Response Function (ICRF), which integrates resolution, peak overlap, peak width, and runtime into a single composite objective function. This strategy enabled short runtime (or short retention time of analytes in a chromatogram) while preserving adequate peak separation. Under the optimized conditions, complete chromatographic separation was achieved within 3 min using a BEH C18 column and a mobile phase consisting of acetonitrile and 4 × 10-4 M CCl3COOH (60:40, v/v) at a flow rate of 0.32 mL/min with detection at 275 nm. The method demonstrated excellent linearity over the range of 5.0-40.0 µg/mL (r > 0.999), with limits of detection of 0.51 µg/mL for DH and 0.61 µg/mL for TI. Mean recoveries were 99.9% and 99.5% for DH and TI, respectively, with satisfactory precision and robustness. The proposed ICRF-assisted optimization approach provided high-resolution separation within minimal runtime and was successfully applied to the routine quality-control analysis of a commercial ophthalmic formulation. The study demonstrates the effectiveness of composite response-based chemometric optimization in enhancing analytical efficiency in pharmaceutical drug analysis.

PMID 42348236
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PubMedEuropean journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V2026-06-18

Moisture-responsive smart hydrogel for adaptive regulation of timolol delivery kinetics under variable wound exudate conditions.

Wiedemann Y Y, Pflumm S S, Ludwigs S S, Lunter D J DJ

Effective wound therapy requires systems that respond to dynamic moisture conditions while enabling controlled drug delivery. This work focuses on the application of a previously developed programmable, humidity responsive hydrogel for exudate management in combination with targeted delivery of timolol, a β-adrenergic antagonist with emerging therapeutic relevance in wound healing. The influence of predefined hydrogel hydration and exudate levels on drug release and skin permeation across wounded and non-wounded skin was evaluated. The hydrated state of the hydrogel exhibited rapid diffusion-controlled drug release, whereas the conditioned hydrogel showed a biphasic swelling-controlled release behavior with initial polymer relaxation followed by predominantly diffusional transport. Higher exudate levels accelerated swelling and shifted the inflection point up to 2.7-fold earlier. Wounded skin showed rapid permeation, while non-wounded skin exhibited pronounced lag phases and up to 77-fold lower permeation. The steady-state flux across wounded skin from the conditioned hydrogel was 1.7-fold lower compared to the hydrated hydrogel. The hydrogel exhibits a fluid handling capacity comparable to superabsorbent dressings while maintaining high moisture vapor transmission. Combining timolol with this smart and self-adjusting material paves the way for a novel category of personalized wound therapy adaptable to a broad range of wound states.

PMID 42309265
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