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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 dermatology2026-09-17

Clinical Characteristics, Management, and Complications of Infantile Hemangiomas Involving the Ear and Periauricular Region.

Matarneh Bayan B, Stefanko Nicole N, Mancini Anthony J AJ, Chamlin Sarah L SL et al.

Despite advances in IH research across various anatomical sites, studies focusing on IH involving the ear and periauricular areas remain scarce. To analyze the clinical characteristics, management, and outcomes of IH involving the ear and periauricular area. Multicenter, retrospective study of patients with IH involving the ear and periauricular area across seven tertiary referral centers between 2001 and 2021. Data analyzed included patient demographics, IH location, management practices, Hemangioma Severity Scale (HSS) scores, and American Academy of Pediatrics (AAP) IH risk categories. A total of 305 patients met the inclusion criteria. Management decision information was available in 250 patients. Active intervention was pursued in 80% of the patients with available management information. The risk of anatomic deformity was the most common indication for treatment (72%), followed by ulceration (18%) and the risk of functional impairment (17%). Systemic beta-blockers were used in 48% of patients, followed by topical corticosteroids (46%) and topical timolol (32%). Treatment with a systemic beta-blocker was associated with a significantly higher HSS score (median 15.5, IQR: 12-20) compared to patients treated with topical therapy (median 10, IQR: 8-12). Given their location and potential for anatomic deformity and functional impairment, ear and periauricular IH may require intervention. A majority of patients in this cohort required treatment, most commonly for risk of anatomic deformity. The study is limited by the retrospective design and inclusion of patients seen before beta-blockers were available for IH management.

PMID 42751730
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PubMedBiomacromolecules2026-09-14

Mucoadhesive Carboxymethyl Chitosan Hydrogel Eyedrops via Dual Dynamic Covalent Chemistry for Long-Acting Glaucoma Therapy.

Pan Jin J, Gong Huangkun H, Shao Qiuyun Q, Zhang Xuehan X et al.

Glaucoma, a leading cause of irreversible blindness, is commonly treated with topical eye drops that reduce intraocular pressure (IOP), but their efficacy is limited by rapid precorneal clearance. To address this, we developed a dynamic hydrogel (CSFP) via Schiff base bonding between carboxymethyl chitosan (CMCS) and 4-formylphenylboronic acid (FPBA) as an advanced delivery vehicle for brimonidine (BRI) and timolol (TIM), two common IOP-lowering agents. The mechanical properties were tunable by adjusting CMCS and FPBA concentrations. The optimized hydrogel exhibited a storage modulus of ∼38.8 Pa (at 1 Hz, 1% strain), excellent self-healing ability, and shear-thinning behavior, facilitating easy administration and resistance to blink-induced clearance. It also achieved near 100% transmittance and a refractive index of 1.339, ensuring optical clarity. Notably, the incorporated phenylboronic acid (PBA) groups enabled selective binding to sialic acid residues on ocular mucins via dynamic phenylboronic ester bonding, prolonging precorneal retention beyond 30 min compared to less than 5 min for the solution control. In a magnetic bead-induced ocular hypertensive rat model, CSFP hydrogel loaded with either BRI or TIM induced greater and long-lasting IOP reduction than the free drug solutions. This work highlights the potential of mucoadhesive dynamic covalent hydrogels for advanced ocular drug delivery.

PMID 42734286
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PubMedThe AAPS journal2026-09-13

Engineering and Characterisation of 3D-Printed Timolol Maleate Implants for Long-Acting Glaucoma Treatment.

Annuryanti Febri F, Adhami Masoud M, Larrañeta Eneko E, Vora Lalitkumar L et al.

Timolol maleate (TM) is a nonselective β-blocker commonly used to treat ocular hypertension and glaucoma. Traditional formulations, such as eye drops and gel-forming solutions, often require frequent administration and may lead to systemic side effects and poor patient compliance. To address these challenges, this study investigated the fabrication and characterization of TM-loaded ocular implants via vat-polymerization 3D printing. The implants were fabricated using polyethylene glycol diacrylate (PEGDA) alone or in combination with polylactic acid/polyurethane acrylate (PLA/PUA) or poly(lactic-co-glycolic acid) (PLGA). The implants were characterized for their thermal properties, drug-release profiles, and biocompatibility. Fourier transform infrared (FTIR) spectroscopy confirmed the absence of significant chemical interactions between the TM and the polymers. Differential scanning calorimetry (DSC) and thermogravimetric analysis (TGA) revealed the thermal stability of the TM-loaded implants, with drug loading influencing the thermal properties. In vitro release studies over 180 days showed that drug release was proportional to the surface area-to-volume (SA/V) ratio of the implant. The release kinetics followed a diffusion-controlled mechanism, as described by the Korsmeyer-Peppas model. The biocompatibility study showed no significant cytotoxicity, with fibroblast viability exceeding 80%. These findings suggest that TM-loaded implants could provide a more effective, sustained-release alternative for glaucoma treatment.

PMID 42728498
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PubMedTherapeutic delivery2026-09-11

Soluble ocular insert of brinzolamide and timolol maleate: in-vitro, ex-vivo and in-vivo characterization.

Prajapati Nikunj N, Vaghela Priyal P, Thakkar Hetal H

The present study aimed to formulate and evaluate a novel transparent and soluble ocular insert containing a fixed-dose combination of Brinzolamide (210 µg) and Timolol maleate (105 µg). The soluble ocular inserts were formulated using hydroxypropyl methylcellulose (HPMC) and polyvinyl alcohol (PVA) as film-forming polymers. Optimization of the parameters was done using a D-optimal design. The optimized soluble ocular inserts were found to be transparent, homogeneous, flexible and demonstrated acceptable surface pH (7.21 ± 0.12), bioadhesive strength (11.88 ± 0.89 g), and tensile strength (1.016 ± 0.13 MPa). In-vitro studies demonstrated sustained drug release up to 24 h following Higuchi kinetics. Ex-vivo permeation across goat cornea and in-vivo pharmacodynamic studies demonstrated enhanced and prolonged intraocular pressure reduction compared to the marketed suspension. The short-term stability testing indicated that the ocular insert retained the characteristics of %Transmittance, pH, Assay and % drug release. Overall, the results suggest that for better therapeutic efficacy and adherence in glaucoma treatment, the dual-drug loaded ocular insert provides a new, patient-friendly substitute for traditional ophthalmic dosage forms.

PMID 42725422
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PubMed[Zhonghua yan ke za zhi] Chinese journal of ophthalmology2026-09-07

[Tafluprost/timolol fixed-dose combination versus tafluprost monotherapy for open-angle glaucoma and ocular hypertension: a multicenter, randomized, double-blind, parallel-group trial].

Wang K D KD, Zhao P P, Wu L L LL, Zhang T H TH et al.

Objective: To evaluate the efficacy and safety of a preservative-free tafluprost/timolol maleate fixed-dose combination compared with preservative-free tafluprost monotherapy in Chinese patients with open-angle glaucoma (OAG) or ocular hypertension (OHT). Methods: This was a multicenter, randomized, double-blind, parallel-controlled clinical trial conducted across 25 centers, including the Eye & ENT Hospital of Fudan University, from January 2019 to November 2022. Patients diagnosed with OAG or OHT who required enhanced intraocular pressure (IOP) reduction after a 4-week washout period were enrolled. Participants were randomized 1∶1 to receive either tafluprost/timolol or tafluprost once daily for 3 months. The primary endpoint was the change from baseline in mean diurnal IOP (the average of measurements at 8:00, 10:00, and 16:00) at Month 3. Secondary endpoints included IOP changes at individual time points and the proportion of responders achieving predefined IOP reduction thresholds. Safety was assessed via the incidence of adverse events (AEs). Analysis of covariance (ANCOVA) using the Markov Chain Monte Carlo (MCMC) method was employed for the primary endpoint; superiority was established if the upper limit of the 95% confidence interval (CI) was<0 mmHg (1 mmHg=0.133 kPa). Continuous variables in secondary endpoints were compared using ANCOVA, and responder rates were analyzed using Fisher's exact test. Results: A total of 219 patients were enrolled (tafluprost/timolol group: n=110; tafluprost group: n=109). The primary efficacy analysis set included 215 patients (tafluprost/timolol: n=107; tafluprost: n=108). Baseline characteristics were well-balanced between the two groups. The majority of patients were male [127 (59.1%)] with a mean age of (44.80±15.71) years at screening. At Month 3, the mean diurnal IOP reduction from baseline was (6.56±3.44) mmHg in the tafluprost/timolol group and (5.36±2.94) mmHg in the tafluprost group. After adjusting for baseline IOP, the between-group difference was -1.312 mmHg (95%CI: -2.010 to -0.696); as the upper limit was<0 mmHg, tafluprost/timolol demonstrated superior IOP-lowering efficacy to tafluprost. Responder rates for IOP reductions of≥15%,≥25%, and≥30% were significantly higher in the tafluprost/timolol group (P=0.016, 0.028, and 0.032, respectively). The incidence of ocular AEs was 20.0% (22/110) in the tafluprost/timolol group and 26.6% (29/109) in the tafluprost group. The most common AE was conjunctival hyperemia, occurring in 2.7% (3/110) and 8.3% (9/109) of the groups, respectively. Conclusion: Compared with preservative-free tafluprost monotherapy, the tafluprost/timolol combination provides significantly greater IOP reduction in patients with OAG and OHT, while maintaining a favorable safety profile.

PMID 42706141
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PubMedPediatric annals2026-09-03

Recognition and Management of Ulcerative Infantile Hemangioma: Risk Factors, Diagnosis, and Prognosis.

Veronica Elvina E, Cai Qiushuang Q, Shen Qin Q, Jiang Yijing Y et al.

Infantile hemangioma (IH) is a benign tumor that appears in the first year of life and typically involutes within 3 to 4 years. Ulcerative IH, the most common complication, poses a significant burden to patients. Early referral of high-risk cases reduces morbidity. Current literature on risk factors and prognosis is limited. Segmental and mixed IH in urogenital, head, neck, and lip areas show higher ulceration risk. Diagnosis is typically clinical; histopathology is rarely performed. Atypical cases require positive glucose transporter-1 immunohistochemistry. Larger lesions, delayed intervention, and bacterial infection worsen prognosis, prolong healing, and increase recurrence. Condition-dependent treatments, including oral propranolol (starting at 1 mg/kg or less daily, maintenance at 2 to 3 mg/kg daily), timolol prophylaxis, and wound management care combined with laser therapy, shorten therapy duration and minimize recurrence. Empiric antibiotics are indicated for infected ulcerative IH. Surgery is indicated for life-threatening cases (eg, chest wall hemangiomas requiring transfusion or airway obstruction) and high-morbidity cases (eg, lip lesions affecting speech or periorbital lesions impairing vision). The Infantile Hemangioma Referral Score helps clinicians identify high-risk patients who require prompt referral, thereby preventing delayed treatment.

PMID 42692987
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