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timolol (timolol, Merck / Timoptol)

✓ Approved

Teva Pharmaceutical Industries Ltd. · ADRB1 · 小分子

什么是 timolol？

timolol 是一种小分子，由Teva Pharmaceutical Industries Ltd.研发。该药已获批，用于治疗相关适应症，给药途径：Others。

药物档案

商品名timolol, Merck, Timoptol
公司Teva Pharmaceutical Industries Ltd.
药物类别小分子
分子靶点ADRB1, ADRB2
给药途径Others
状态Approved
来源： ClinicalTrials.gov, Teva Pharmaceutical Industries Ltd.

作用机制

分子靶点

timolol 作用于 2 个分子靶点：

ADRB1adrenoceptor beta 1 (B1AR, RHR)
ADRB2adrenoceptor beta 2 (B2AR, ADRBR)
需要更深入的分析？Noah AI 可解释复杂机制并与同类药物比较。

治疗适应症

timolol 针对 1 个适应症，涉及 1 个治疗领域。

治疗领域疾病/病症分期
Eye disordersGlaucoma✓ Approved

相关研究文献

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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PubMedInternational ophthalmology2026-09-01

Five-year trends in primary open-angle glaucoma surgery: baseline characteristics preferences, and the impact of emerging techniques.

Gumus Akgun Gulsah G, Erbas Gozdenur G, Dogruel Ece E, Alagoz Nese N et al.

To evaluate the baseline characteristics of patients with open-angle glaucoma (OAG) who underwent primary glaucoma surgery between 2020 and 2024, and to analyze trends in surgical preferences. Medical records of patients older than 18 years who underwent primary glaucoma surgery were reviewed retrospectively. Surgical procedures included trabeculectomy, Ahmed Glaucoma Valve (AGV) implantation, gonioscopy-assisted transluminal trabeculotomy (GATT), Kahook Dual Blade (KDB), XEN Gel Stent implantation, and diode laser cyclophotocoagulation. A total of 1,192 eyes were included, and the annual number of operated eyes was 158 in 2020, 231 in 2021, 245 in 2022, 326 in 2023, and 232 in 2024. Age, IOP, BCVA, and glaucoma stage were similar across the years (all p > 0.05), whereas the number of preoperative medications was higher in 2020 than in the following years (p < 0.01). Across all years, surgery was performed most frequently in eyes with severe glaucoma, and trabeculectomy remained the most common procedure. In 2023 and 2024, the frequencies of trabeculectomy and AGV implantation decreased, whereas GATT increased and became the third most commonly performed procedure. The minimally invasive glaucoma surgery (MIGS) group included more mild-to-moderate cases and fewer severe cases, and had better BCVA and lower IOP than the non-MIGS group (all p < 0.05). Baseline characteristics remained largely stable over the five-year period, except for higher preoperative use of antiglaucoma medications in 2020. Surgical practice shifted toward GATT and MIGS in 2023 and 2024. Compared with the non-MIGS group, the MIGS group included a higher proportion of eyes with mild-to-moderate disease, while trabeculectomy remained the most commonly performed procedure overall.

PMID 42675196
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PubMedBiochemistry. Biokhimiia2026-08-30

Inorganic Nanoparticles: Applications in Ophthalmology.

Popova Ekaterina V EV, Tikhomirova Victoria E VE, Kost Olga A OA

This review summarizes current data on potential applications of the main classes of inorganic nanoparticles in ophthalmology, as well as their advantages and limitations, and systematizes data on the most studied inorganic nanoparticles, including gold and silver nanoparticles, metal oxides (e.g., iron oxide, zinc oxide), silica, and insoluble calcium salts. Particular attention is paid to their toxicity to eye tissues and the use as carriers for encapsulation and controlled release of various biologically active substances, such as antiglaucoma drugs, antibiotics, anti-inflammatory and antitumor agents. The review examines the results of in vivo experiments using nanoparticles, demonstrating their physiological effects, capacity to increase the bioavailability of drugs, and ability to prolong their therapeutic effect.

PMID 42669552
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PubMedBiochemistry. Biokhimiia2026-08-30

Dopaminergic System of the Eye and Its Role in Glaucoma Pathogenesis.

Chesnokova Natalya B NB, Pavlenko Tatyana A TA, Beznos Olga V OV, Petrov Sergey Y SY et al.

Glaucoma is a multifaceted disease characterized by optic nerve damage and retinal ganglion cell (RGC) degeneration, leading to optic neuropathy and vision loss. Neurodegenerative processes in the retina underlie glaucoma pathogenesis. Elevated intraocular pressure (IOP) is a contributing factor in the development and progression of most types of glaucoma, making IOP reduction the standard treatment approach, while existing neuroprotective therapies remain largely ineffective. Dopaminergic system (DS) of the eye and its role in ocular pathology are insufficiently studied, yet available data suggest that DS is one of the most significant regulatory systems in the eye. It is widely represented in ocular structures and participates in regulation of visual function, circadian rhythms, blood circulation, and aqueous humor dynamics, as well as in eye development. Both IOP elevation and retinal ganglion cell neurodegeneration in glaucoma are critically influenced by an imbalance in the DS components. In the vertebrate retina, dopamine serves as the primary neurotransmitter and neuromodulator. It is also a precursor to sympathetic nervous system mediators - epinephrine and norepinephrine - expanding its role in physiological processes, including IOP regulation. This review presents recent and foundational studies on the presence of dopamine and its receptors in various ocular structures, their significance in normal eye function, mechanisms of involvement in neurodegenerative processes in glaucoma, and in IOP regulation. Based on analysis of the DS role in glaucoma pathogenesis, the prospects for developing antiglaucoma drugs for neuroprotection, IOP reduction, and combined mechanisms of action are discussed. Additionally, potential use of the analysis of DS components in the tear fluid as a non-invasive test for early diagnosis, prognosis, and therapeutic justification is considered.

PMID 42669553
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PubMedInternational ophthalmology2026-08-28

Impact of prostaglandin-related antiglaucoma medication use on levator aponeurosis advancement outcomes.

Ono Takashi T, Matsuda Hitomi H, Matsushima Kota K, Ota Mami M et al.

To evaluate postoperative eyelid height at 3 months after levator aponeurosis advancement with or without concomitant skin excision in eyes with and without prostaglandin-related antiglaucoma medication use. This retrospective single-center study included patients who underwent levator aponeurosis advancement with or without concomitant skin excision for acquired ptosis. The primary outcome was postoperative margin reflex distance 1 (MRD-1) at 3 months. A linear mixed-effects model was used to evaluate factors associated with postoperative MRD-1, including prostaglandin-related antiglaucoma medication use and previous glaucoma surgery. Seventy-two eyes from 46 patients were analyzed; 35 received prostaglandin-related antiglaucoma medication, and 37 did not. Mean preoperative MRD-1 was significantly lower in the medication group (0.30 ± 0.82 mm vs 0.85 ± 0.83 mm, P = 0.006). Postoperative MRD-1 at three months did not differ significantly between groups. MRD-1 improvement was greater in the medication-use group (P = 0.024). Prostaglandin-related medication use was not significantly associated with postoperative MRD-1 after adjustment for preoperative MRD-1, age, sex, concomitant skin excision, and previous glaucoma surgery. Eyes administered prostaglandin-related antiglaucoma medication had a lower preoperative MRD-1 than eyes without such medication use. However, postoperative MRD-1 at 3 months was comparable between the groups. Prostaglandin-related medication use was not significantly associated with postoperative MRD-1 after adjustment for previous glaucoma surgery and other covariates.

PMID 42663761
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