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timolol (Ophtim / timolol, Thea)

✓ Approved

Takeda · ADRB1 · 小分子

什么是 timolol？

timolol 是一种小分子，由Takeda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Ophtim, timolol, Thea
公司Takeda
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, Takeda

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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PubMedGenes2026-08-27

Exploratory Analysis of Glaucoma-Associated SNPs in a Colombian Cohort Highlights Potential Involvement of Oxidative, Vascular, and Neurodegenerative Pathways.

Casanova Carlos C, Valencia-Peña Claudia C, Saldarriaga-Gil Wilmar W, Lozano-Cruz Edgar E et al.

Primary open-angle glaucoma (POAG) is a complex multifactorial optic neuropathy involving genetic, vascular, oxidative, inflammatory, and neurodegenerative mechanisms. Despite advances in genome-wide studies, the contribution of genetic variants remains incompletely characterized in underrepresented Latin American populations. This study aimed to characterize the genetic landscape of POAG in a Colombian cohort by identifying previously reported glaucoma-associated variants, rare candidate variants, and pharmacogenomic markers and integrating these findings into biologically relevant pathways. An exploratory descriptive study was conducted in 21 Colombian patients with confirmed POAG. Whole-exome sequencing (WES) was performed at an average sequencing depth of approximately 100×. Variants were quality-filtered, functionally annotated, and prioritized within 446 POAG-associated genes retrieved from DisGeNET. Previously reported glaucoma-associated variants and rare candidate variants were identified, while pharmacogenomic variants related to latanoprost and timolol response were evaluated using ClinPGx/PharmGKB. Identified genes were classified according to major biological pathways relevant to glaucoma pathophysiology. Of the 446 POAG-associated genes, 381 were detected in the patients' exomes. A total of 10,220 molecular variants were identified, of which 1,187 synonymous variants were excluded, leaving 9,033 variants for downstream analysis. Among these, 955 were non-synonymous SNVs, including 26 variants previously reported in association with glaucoma and 929 potentially novel coding variants. Previously reported variants included loci in SIX6, LOXL1, CYP1B1, NOS3, and SOD2. Two rare candidate variants (minor allele frequency <1%) were identified in FMNL2 and C3. Pharmacogenomic variants in PTGS1, ADRB1, and ABCC4 with potential implications for response to latanoprost or timolol were also detected. Functional integration highlighted pathways involving oxidative stress, extracellular matrix remodeling, vascular regulation, neurodegeneration, and inflammation. This exploratory analysis identifies known glaucoma-associated variants, rare candidate variants, and pharmacogenomic markers in Colombian patients with POAG. The findings support a multifactorial biological framework involving interconnected oxidative, structural, vascular, neurodegenerative, and inflammatory pathways. The FMNL2 and C3 variants represent candidates for further investigation, while the identified pharmacogenomic variants highlight the potential relevance of genomic profiling for personalized glaucoma management. Larger ancestry-informed case-control studies are required to validate these observations and determine their clinical significance.

PMID 42650112
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PubMedNaunyn-Schmiedeberg's archives of pharmacology2026-08-11

Can pilocarpine effectively and safely manage glaucoma in the modern era? A systematic review and meta-analysis.

Chen Kai-Yang KY, Chan Hoi-Chun HC, Chan Chi-Ming CM

This study systematically evaluates the efficacy, safety, tolerability, and contemporary clinical positioning of topical pilocarpine in the management of glaucoma and ocular hypertension. This systematic review and meta-analysis followed the Preferred Reporting Items for Systematic Reviews and Meta-Analyses (PRISMA) 2020 guidelines. PubMed/MEDLINE, EMBASE, Cochrane CENTRAL via the Cochrane Library, Scopus, Web of Science Core Collection, and Google Scholar were searched from inception to 1 May 2026 without language restrictions. Randomized controlled trials and controlled observational studies in adults with glaucoma or ocular hypertension were eligible when topical pilocarpine, used alone or in combination, was compared with placebo, no treatment, laser trabeculoplasty, or other intraocular pressure (IOP)-lowering therapies. The primary outcome was mean change in IOP, and secondary outcomes included responder outcomes, ocular adverse events, discontinuation, visual field outcomes, medication burden, post-laser pressure spikes, and postoperative outcomes. Risk of bias was assessed with the Cochrane Risk of Bias 2.0 tool (RoB 2.0) for randomized studies and the Risk of Bias in Nonrandomized Studies of Interventions (ROBINS-I) tool for nonrandomized studies. We performed random-effects meta-analysis using raw mean difference in mmHg for continuous outcomes and risk ratio (RR) for binary safety outcomes, each reported with a 95% confidence interval (CI); certainty of evidence was assessed using the Grading of Recommendations Assessment, Development and Evaluation (GRADE) approach. Of the 38 studies that met the inclusion criteria, 34 contributed data to the quantitative meta-analysis. In the primary analysis, pilocarpine-containing regimens reduced IOP by an additional 1.16 mmHg compared to all comparators (95% CI 0.84 to 1.47; P < 0.001; I2 = 50.7%). Subgroup analyses suggested larger pooled effects in placebo/no-treatment comparisons, ocular hypertension, primary open-angle glaucoma, and monotherapy studies; however, comparisons with beta-blockers and prostaglandin analogs require cautious interpretation because several large individual trials favored timolol or latanoprost for daily clinical use, tolerability, or dosing convenience. Pilocarpine was associated with a sevenfold higher risk of blurred vision (RR 7.33; 95% CI 3.30 to 16.29) and a sixfold higher risk of discontinuation due to adverse events (RR 6.07; 95% CI 3.69 to 10.00). Egger's test pointed to funnel plot asymmetry (P = 0.003), although the trim and fill method did not impute any missing studies. Pilocarpine lowers IOP effectively, but its modern role is limited by frequent dosing, miosis, blurred vision, accommodative symptoms, brow ache, and higher discontinuation. In current glaucoma care, prostaglandin analogs and selective laser trabeculoplasty are generally more consistent with first-line open-angle glaucoma management, whereas pilocarpine is better positioned for selected clinical scenarios, including angle-closure mechanisms, post-laser pressure-spike prophylaxis, selected postoperative angle-surgery settings, intolerance or nonresponse to other drug classes, and resource-limited settings where newer therapies are unavailable or unaffordable.

PMID 42578995
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PubMedInternational journal of pharmaceutics: X2026-08-10

Liposomal Gel for enhancing topical efficacy of timolol maleate against proliferating superficial infantile hemangiomas.

Hang Xiaoxing X, Jin Taiwei T, Hua Jun J, Zhang Xuenong X et al.

Conventional timolol maleate (TM) eye drops are limited by low transdermal bioavailability and short dermal residence time for the treatment of superficial infantile hemangioma (IH). To address this, a novel 0.5% TM-loaded liposomal gel (TM-lipogel) was developed by embedding optimized liposomes within a carbomer gel matrix. The TM-liposomes exhibited a desirable particle size of 139.5 ± 2.1 nm, a polydispersity index (PDI) of 0.051, a zeta potential of -38.7 mV, and an encapsulation efficiency of 64.76 ± 3.2%. Ex vivo permeation studies revealed a 1.9-fold increase in cumulative transdermal delivery compared to the TM-gel, and 4-fold compared to the TM solution (p < 0.05). Furthermore, confocal laser scanning microscope imaging revealed that TM-lipogel achieved a penetration depth of 400 μm, while the TM-gel and TM-eyedrop only reached 200 μm and 75 μm, respectively, highlighting the superior penetration of the liposomal gel. In a murine xenograft hemangioma model, 0.5% TM-lipogel achieved superior tumor regression (81.09%, p < 0.01 vs.control) compared to 0.5% TM-eyedrop (29.85%) and 0.5% TM-gel (61.69%) by simultaneously downregulating HIF-1α, VEGF, MMP-9 and eNOS. Critically, the optimized formulation exhibited no skin irritation and no systemic toxicity. These findings highlight that the TM-lipogel provides enhanced transdermal delivery with deeper tissue penetration, representing a highly effective and safe transdermal strategy for IH therapy.

PMID 42572560
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PubMedInternational journal of clinical pharmacy2026-08-08

Medicine shortages and glaucoma care: a time-series analysis indicating population-level consequences of a national timolol eye drop shortage.

Fawcett Erin E, Ellett Lisa Kalisch LK, Sarin Simi S, Haines Cassandra C et al.

Medicine shortages can disrupt glaucoma management and necessitate therapeutic substitution. Understanding how shortages affect access to first-line treatments for glaucoma is important for optometrists when monitoring intraocular pressure control, and pharmacists when counselling patients and coordinating care during periods of limited medicine availability. Timolol, a non-selective beta-blocker, is a first-line treatment for glaucoma and ocular hypertension and has experienced international shortages in recent years. Between August 2024 and May 2025, Australia experienced a nationwide shortage of timolol-containing eye drops, raising concerns regarding continuity of care, access to treatment, and therapeutic substitution. To descriptively examine the impact of the 2024-2025 timolol eye drop shortage on dispensing patterns of antiglaucoma medicines in Australia and assess the contribution of imported products in mitigating the shortage. A retrospective drug utilisation study was conducted using publicly available aggregate Pharmaceutical Benefits Scheme (PBS) and Repatriation PBS dispensing data from January 2020 to August 2025. Monthly dispensings of antiglaucoma preparations (ATC S01E) were standardised per 100,000 population and analysed using descriptive time-series methods. Dispensing trends were compared before, during, and after the shortage, with stratification by timolol formulation, therapeutic class, and product type (locally supplied versus overseas imports). The late 2024 and early 2025 timolol shortage was associated with a sustained decline in dispensing of single-ingredient extended-release timolol, decreasing from approximately 40 dispensings per 100,000 population per month before the shortage to 1.07 by March 2025. Dispensing of standard-release timolol increased temporarily in October 2024 before declining in a similar pattern. Overseas imports accounted for 24.3% of all timolol dispensings during the shortage period and peaked at 87% of timolol dispensings in March 2025. Despite regulatory approval of imported products, overall timolol utilisation remained below pre-shortage levels. Alternative therapeutic classes, including prostaglandin analogues and carbonic anhydrase inhibitors, showed modest increases in dispensing, suggesting potentially limited therapeutic substitution. The timolol shortage disrupted access to a cornerstone first-line treatment for glaucoma. Regulatory intervention through the approval of imported products partially mitigated the shortage but did not restore utilisation to pre-shortage levels in Australia. Future shortage management strategies should prioritise rapid policy activation and closer alignment of imported products with formulations routinely available in Australia.

PMID 42570054
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