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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

PubMedAmerican journal of ophthalmology case reports2026-10-25

Recurrent delayed hyphema following latanoprost/netarsudil initiation in an eye with a XEN 63 gel stent: a case report.

Greco Antonio A, Calabresi Valerio V, Marenco Maria M, Garavelli Fabio F et al.

To describe recurrent delayed hyphema following initiation of fixed-dose latanoprost/netarsudil in an eye with a previous XEN 63 gel stent, and to discuss whether the associated IOP reduction may have unmasked a pre-existing peri-implant reflux pathway. A 72-year-old woman with advanced primary open-angle glaucoma and previous ab interno XEN 63 gel stent implantation developed recurrent spontaneous hyphema shortly after bimatoprost/timolol was replaced with latanoprost/netarsudil. Intraocular pressure decreased from 17-19 mmHg to 8-9 mmHg after treatment initiation. The first episode occurred nine days later, with blurred vision, a small anterior chamber hyphema, and fine endothelial blood deposits. Gonioscopy showed active blood reflux from tissue surrounding the proximal intracameral XEN segment, without bleeding from other angle structures. Recurrent episodes occurred despite conservative management and, subsequently, despite discontinuation of latanoprost/netarsudil. Because the peri-implant region was repeatedly identified as the reflux site, the XEN stent was eventually removed. No further bleeding episodes were observed after explantation. The clinical course is consistent with a susceptible peri-implant anatomical configuration contributing to recurrent blood reflux. The temporal association between latanoprost/netarsudil initiation, marked IOP reduction, and the first hyphema suggests a possible precipitating or unmasking role, but does not establish drug causality. Delayed or recurrent hyphema after XEN implantation should prompt review of recent medication changes and careful gonioscopic inspection of the proximal XEN segment.

PMID 42927338
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PubMedActa ophthalmologica2026-10-24

Therapeutic efficacy and systemic pharmacokinetics of a dual-drug hydrogel contact lens for sustained glaucoma therapy.

Varshitha Vangol V, Sankararajan Umadevi U

Conventional topical therapy for glaucoma is limited by poor ocular bioavailability, rapid precorneal drug loss, frequent dosing and systemic absorption through the nasolacrimal pathway, which may reduce therapeutic efficacy and increase the risk of adverse effects. Drug-eluting hydrogel contact lenses have emerged as a promising strategy to overcome these limitations by enabling sustained ocular drug delivery. This study aimed to evaluate the therapeutic efficacy, ocular biocompatibility and systemic pharmacokinetic profile of an optimized dual-drug-loaded HEMA-based hydrogel contact lens delivering timolol maleate (TM) and brimonidine tartrate (BT) for sustained glaucoma management. Optimized hydrogel contact lenses composed of 2-hydroxyethyl methacrylate (HEMA), N, N-dimethylacrylamide (DMA), N-vinylpyrrolidone (NVP) and ethylene glycol dimethacrylate (EGDMA) were fabricated by UV photopolymerization and loaded with TM and BT (4 mg/mL each). Ocular biocompatibility was assessed using the modified Draize irritation test. Therapeutic efficacy was evaluated in a steroid-induced ocular hypertension New Zealand White rabbit model by monitoring intraocular pressure (IOP) for 24 h. Systemic drug exposure was determined by validated high-performance liquid chromatography (HPLC) analysis of plasma samples, while ocular safety was further confirmed through histopathological examination. The optimized hydrogel lens exhibited excellent ocular biocompatibility, with a maximum Draize score of 0.33 ± 0.12 that resolved completely within 48 h and no histopathological evidence of ocular tissue damage. In hypertensive rabbits, the dual-drug hydrogel lens maintained normotensive IOP (16.1 ± 0.8 mmHg) for 24 h, representing a 43.5% reduction from baseline and significantly outperforming conventional eye drops beyond 4 h (p < 0.01). Plasma concentrations of both TM and BT remained below the limit of quantification (<2.0 ng/mL) throughout the study, whereas conventional eye drops produced measurable systemic exposure (TM: 18.4 ± 2.1 ng/mL; BT: 8.2 ± 1.2 ng/mL), demonstrating effective minimization of systemic drug absorption. The optimized dual-drug-loaded hydrogel contact lens provided sustained intraocular pressure reduction, excellent ocular biocompatibility and negligible systemic drug exposure compared with conventional topical therapy. These findings highlight its potential as a sustained ocular drug-delivery platform capable of improving therapeutic efficacy, reducing systemic adverse effects and enhancing long-term treatment adherence in glaucoma management. Further long-term preclinical investigations and clinical studies are warranted to support clinical translation.

PMID 42920388
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PubMedJournal of the Chinese Medical Association : JCMA2026-10-14

Nonselective beta-blockers and hepatic encephalopathy in liver cirrhosis:A meta-analysis of randomized controlled trials.

Kuo Tai-Hui TH, Chen Yu-Jen YJ, Lee Pei-Chang PC, Yang Tsung-Chieh TC et al.

Liver cirrhosis leads to portal hypertension and related complications, including ascites, esophageal varices, and hepatic encephalopathy (HE). Non-selective beta blockers (NSBBs) decrease portal pressure, but it is not yet clear whether they contribute to HE development. Therefore, we examined the association between NSBB therapy and HE in randomized controlled trials (RCTs) involving patients with cirrhosis. We systematically searched PubMed, Web of Science, ScienceDirect, and the Cochrane Library (from inception to December 31, 2024) for RCTs comparing NSBBs with a placebo, endoscopic band ligation, or injection sclerotherapy for variceal bleeding prevention in relation to HE. The risk ratios (RRs) and 95% confidence intervals (CIs) were pooled using a random-effects model. Subgroups were defined according to the comparator, NSBB type, and hepatic function status (weighted mean Child-Pugh score ≤6 vs. >6). The risk of bias was assessed using the revised Cochrane risk-of-bias tool for randomized trials (RoB 2). There were 12 relevant studies, which included 775 NSBB-treated and 771 comparator patients (54 and 57 HE events). NSBB therapy was not associated with a statistically significant change in HE risk (RR 1.04, 95% CI 0.73-1.47; p = 0.84; I² = 0%). Estimates were consistent across all subgroups of hepatic function statuses (compensation, RR 1.18, 0.44-3.14; decompensation, RR 1.02, 0.70-1.48; p = 0.79), comparators (placebo, RR 1.19, 0.79-1.80; endoscopic therapy, RR 0.72, 0.38-1.39; p = 0.20), and NSBB types (propranolol/timolol, RR 1.06, 0.72-1.55; carvedilol, RR 0.95, 0.42-2.15; p = 0.82). Current evidence does not indicate a statistically significant association between NSBB therapy and HE development in patients with cirrhosis, regardless of disease severity.

PMID 42870342
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PubMedActa paediatrica (Oslo, Norway : 1992)2026-10-10

Oral Propranolol Versus Topical Timolol for the Treatment of Infantile Haemangiomas: A Systematic Review and Meta-Analysis of Randomized Controlled Trials.

Weng Liwen L, Zuo Hongli H, Zhao Min M, Dong Jialin J

This systematic review and meta-analysis aimed to compare the efficacy and safety of oral propranolol versus topical timolol for the treatment of superficial infantile haemangiomas. We systematically searched PubMed, Cochrane Library, Embase, Web of Science and China National Knowledge Infrastructure from inception to April 23, 2026. Only randomized controlled trials comparing oral propranolol with topical timolol for superficial infantile haemangiomas were included. Two reviewers independently screened studies, extracted data and assessed risk of bias using the Cochrane risk of bias 2.0 tool. The primary outcomes were overall response rate and incidence of systemic adverse events. Pooled risk ratios (RRs) with 95% confidence intervals (CIs) were calculated using fixed-effect models. Seven randomized controlled trials comprising 428 infants were included. Topical timolol was comparable to oral propranolol in overall response rate (RR = 1.09, 95% CI 0.97-1.23, p = 0.17; I2 = 0%). Topical timolol significantly reduced the risk of systemic adverse events compared with oral propranolol (RR = 0.35, 95% CI 0.20-0.59, p < 0.0001; I2 = 9%). Topical timolol demonstrates comparable efficacy to oral propranolol for superficial infantile haemangiomas and has a significantly superior safety profile with a 65% reduction in systemic adverse events.

PMID 42855991
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PubMedMedicina (Kaunas, Lithuania)2026-09-26

Effect of Latanoprost and Timolol-Dorzolamide Therapy on Aqueous Humor Cytokine Concentrations in Patients with Pseudoexfoliative Glaucoma.

Valković Antić Ivana I, Juranić Lisnić Vanda V, Sotošek Vlatka V, Bertović Ivana I et al.

Background and Objectives: Pseudoexfoliative glaucoma (PEXG) is a secondary glaucoma caused by the deposition of abnormal flaky protein-like material inside the eye, leading to blockage of the drainage system, increased intraocular pressure (IOP), and optic nerve damage. This study aimed to evaluate the effects of latanoprost and timolol-dorzolamide therapy on the concentrations of interleukin (IL)-1β, IL-6, IL-8, IL-10, IL-12p70, and tumor necrosis factor-alpha (TNF-α) in the aqueous humor and serum samples of patients with PEXG. Materials and Methods: This prospective observational study included 60 patients allocated to three age-matched groups (n = 20 per group). Group 1 received latanoprost therapy, Group 2 received timolol-dorzolamide therapy, and Group 3 comprised patients with cataracts without PEXG who were not receiving antiglaucoma medication (control group). All participants underwent a comprehensive ophthalmological examination, including visual acuity assessment, specular microscopy, IOP measurement, and intraocular lens (IOL) measurement. Peripheral venous blood was taken from each patient before the surgical procedure and aqueous humor samples were collected during cataract surgery. Concentrations of IL-1β, IL-6, IL-8, IL-10, IL-12p70, and TNF-α were determined using a Cytometric Bead Array and flow cytometry. Results: No significant differences were observed in the aqueous humor and serum concentrations of IL-6 and IL-8 between the treatment groups, while IL-1β, IL-10, IL-12p70, and TNF-α did not reach detection. A significant positive correlation was found between IOL and aqueous humor IL-6 concentration in group 1 and between IL-6 and IL-8 serum concentration and IOP in controls. Conclusions: Latanoprost and timolol-dorzolamide therapy were not associated with significant differences in aqueous humor or serum IL-6 and IL-8 concentrations in patients with PEXG. IL-1β, IL-10, IL-12p70, and TNF-α were not detectable in the analyzed samples. These findings support the presence of low-grade inflammation in patients with PEXG that does not differ according to the therapy administered. Corneal endothelial alterations are disease-related rather than treatment-induced.

PMID 42796240
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PubMedMedicina (Kaunas, Lithuania)2026-09-26

Ocular Surface Symptoms, Objective Redness, and Intraocular Pressure After a Switch from Fixed Dorzolamide/Timolol to Netarsudil in Latanoprost-Treated Glaucoma and Ocular Hypertension: A Prospective Real-World Cohort Study.

Zanutigh Virginia V, Logioco Celina C, Galetto Leila L, Perrone Franco F et al.

Background and Objectives: Conjunctival hyperemia is common with netarsudil, but redness may not reflect the overall patient experience when treatment burden is reduced. We evaluated ocular surface symptoms, objective redness, tear-film parameters, intraocular pressure (IOP), and treatment preference after a routine-care switch from twice-daily fixed dorzolamide/timolol to once-daily netarsudil 0.02%, while continuing latanoprost. Materials and Methods: This prospective, single-center observational cohort included 30 consecutive adults with primary open-angle glaucoma or ocular hypertension and controlled IOP. Outcomes were assessed at baseline and months 1 and 2. The primary outcome was the Ocular Surface Disease Index (OSDI). Continuous eye-level outcomes were analyzed using mixed-effects models accounting for fellow-eye and repeated-measures correlation; grade ≥ 2 hyperemia was analyzed using participant-clustered logistic regression. Results: Twenty-seven participants (54 eyes) completed evaluable 2-month follow-up. Median OSDI decreased from 7.50 at baseline to 6.25 at month 1 and 5.00 at month 2 (Friedman p = 0.0015). The mean baseline-to-month 2 change was -2.95 points (95% CI, -4.80 to -1.10), and 6/27 participants (22.2%) improved by at least 7 points. Serle grade ≥ 2 hyperemia increased from 7.4% of eyes at baseline to 51.9% at month 1 and 44.4% at month 2. Estimated mean bulbar redness index increased from 1.57 to 2.14 (p < 0.0001), tear meniscus height increased modestly, and non-invasive keratograph break-up time showed no significant longitudinal change. Estimated mean IOP changed from 14.50 to 13.65 mmHg (p = 0.0083), with no eye showing an increase of at least 4 mmHg. Burning improved after multiplicity adjustment, and 17/27 participants with available month-2 preference data (63.0%) preferred netarsudil. Conclusions: The switch was associated with modest OSDI improvement and maintained short-term IOP control despite increased objective redness. Patient preference appeared to reflect factors beyond redness alone.

PMID 42796375
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