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timolol (Timpilo / timolol, ophthalmic)

✓ Approved

Merck & Co. · ADRB1 · 小分子

什么是 timolol?

timolol 是一种小分子,由Merck & Co.研发。该药已获批,用于治疗相关适应症。

药物档案

商品名Timpilo, timolol, ophthalmic
公司Merck & Co.
药物类别小分子
分子靶点ADRB1, ADRB2, CHRM3
状态Approved

作用机制

分子靶点

timolol 作用于 3 个分子靶点:

ADRB1adrenoceptor beta 1 (BETA1AR, ADRB1R)
ADRB2adrenoceptor beta 2 (ADRBR, B2AR)
CHRM3cholinergic receptor muscarinic 3 (EGBRS, m3AChR)
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

PubMedFrontiers in immunology2026-08-05

FAERS database reveals latent signals of neuro-ophthalmic toxicity associated with immune checkpoint inhibitors: feature mining and clinical warnings.

Li Jiewen J, Zhang Wen W, Lin Jing J, Kong Lingjun L et al.

To perform signal mining of neuro-ophthalmic immune-related adverse events (irAEs) associated with immune checkpoint inhibitors (ICIs) using the FDA Adverse Event Reporting System (FAERS), and to synthesize their clinical manifestations and temporal patterns, thereby providing evidence-based insights for optimizing clinical drug safety. Reports of neuro-ophthalmic irAEs associated with ICIs were extracted from the FAERS (Q1 2011 to Q4 2025). Signal detection was performed using disproportionality analysis methodologies, specifically the Reporting Odds Ratio (ROR) and Information Component (IC) algorithms, with predefined statistical thresholds for signal significance. A total of 521 reports identified neuro-ophthalmic irAEs with ICIs as primary suspect drugs, predominantly affecting males and elderly patients At the High-Level Group Term (HLGT) level, positive signals were detected for pembrolizumab and avelumab. Preferred Term (PT) analysis revealed six significant signals, with eyelid ptosis being the most frequently reported event. The median time to onset was 28-38 days, with acute presentations (≤24 hours post-infusion) observed for pembrolizumab and nivolumab; both agents exhibited elevated case fatality proportions, with a higher proportion of male patients among fatal cases. This study delineated potential neuro-ophthalmic positive disproportionality signals across seven ICIs, revealing demographic variations in signal reporting frequency with higher susceptibility among males and elderly patients. Pembrolizumab and avelumab were associated with higher reporting frequencies of neuro-ophthalmic adverse events, which were related to poor visual outcomes. Consequently, prompt recognition and management of neuro-ophthalmic irAEs are imperative to enhance ICI safety profiles in clinical practice.

PMID 42553366
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PubMedClinical case reports2026-08-05

Bilateral IgG4-Related Dacryoadenitis.

Song Yan Y, Ding Lin L, Shen Tao T

Chronic dacryoadenitis is an uncommon inflammation of the lacrimal gland that may have various etiologies with similar presentations. IgG4-related ophthalmic disease most often manifests as painless lacrimal gland enlargement, so the clinicians should consider IgG4-related disease as a diagnostic possibility for dacryoadenitis.

PMID 42553466
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PubMedWorld journal of pediatric surgery2026-08-05

Intra-arterial chemotherapy for retinoblastoma: a structured narrative review.

Ren Yan Hong YH, Kang Daohuan D, Shi Caiping C, Sun Wen W

Retinoblastoma (Rb) is the most common primary intraocular malignancy in children. Intra-arterial chemotherapy (IAC), often termed ophthalmic artery chemosurgery, has emerged as an important globe-preserving treatment modality for advanced intraocular Rb. We focused on technical delivery, clinical indications, regimen selection, oncological safety, globe salvage, functional preservation and complications. Current evidence indicates that, in appropriately selected patients and experienced centers, IAC can improve local tumor control and globe salvage while reducing systemic toxicity when compared with intravenous chemotherapy. While melphalan remains the backbone chemotherapeutic agent, escalation to topotecan and/or carboplatin should be guided by tumor burden, vitreous or subretinal seeding, prior treatment response, evidence strength and expected functional potential. Functional preservation should be defined as more than anatomical globe retention; it should include age-appropriate visual acuity or fixation, electroretinography, macular and foveal integrity, avoidance of retinal or choroidal ischemia, amblyopia management, binocular visual development and quality-of-life outcomes. IAC remains associated with ocular and vascular risks, including retinal or choroidal ischemia, cataract formation and ophthalmic artery stenosis or occlusion. Future multicenter prospective studies should use standardized outcome measures, scenario-specific recommendations and molecular monitoring, including aqueous humor cell-free DNA analysis, to refine patient selection and support function-preserving care.

PMID 42553724
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PubMedAdvanced healthcare materials2026-08-05

Engineering Concentration-Dependent Intravitreal Mobility via Cyclic Arginine-Enriched Nanocarrier Surface Modification: In Vivo Proof-of-Concept in a Porcine Large Animal Model.

Hammer Maximilian M, Ackermann Bryan Calder BC, Stoß Anna A, Junker Niklas N et al.

Nanoparticulate drug delivery systems represent a promising platform for sustained intraocular drug release following intravitreal administration, leveraging low metabolic turnover of the vitreous to maintain therapeutic drug levels over extended periods. Despite this potential, nanoparticle diffusion toward the visual axis can induce light scattering and visual disturbance. Given the negative charge of the vitreous, surface-engineered nanoparticles provide a strategy to modulate particle mobility and restrict off-target migration. Here, we performed a 6-week in vivo evaluation in pigs of an intravitreally applied, positively charged, cyclic-arginine surface-functionalized liposomal nanocarrier designed to reduce intravitreal mobility. Three formulations containing 0.1%, 0.5%, or 1% cyclic-arginine-modified phospholipid were compared with unmodified control liposomes in a large animal pig model. A multimodal biocompatibility and performance assessment was conducted, including intraocular pressure monitoring, fundus imaging, structural and angiographic OCT, dye-based angiography, and post-mortem retinal immunostainings. Cyclic-arginine surface functionalization of the liposomes resulted in a concentration-dependent reduction in intravitreal mobility, quantified by vitreous haze and fundus-based distribution analyses. All surface-engineered nanoparticles demonstrated excellent ocular biocompatibility without structural or vascular adverse effects. These data establish cyclic-arginine surface modification as a robust design principle to modulate intravitreal mobility and support the development of next-generation nanoparticle biomaterials for long-acting ophthalmic drug delivery.

PMID 42554203
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PubMedBest practice & research. Clinical obstetrics & gynaecology2026-08-04

How to measure ophthalmic artery Doppler for pre-eclampsia screening.

Hanton Thomas T, Khalil Asma A

Pre-eclampsia remains a leading cause of maternal and perinatal morbidity, affecting 3-5% of pregnancies globally. Screening in most hospital settings relies on risk factors, and only a few hospitals perform individualised risk screening using maternal factors, mean arterial pressure, uterine artery Doppler, and biochemical markers. Maternal ophthalmic artery (OA) Doppler has emerged as a significant marker of cerebrovascular and systemic hemodynamic adaptation. The peak systolic velocity (PSV) ratio reflects an integrated measure of cardiac output and peripheral vascular resistance. To provide a standardised, practical guide for acquiring high-quality ophthalmic artery Doppler measurements to be incorporated into clinical pre-eclampsia screening protocols. The guide outlines a nine-step acquisition technique using a high-frequency (7-18 MHz) linear-array transducer. Following a 5-min rest period, measurements are taken with the patient supine, and the probe is gently placed on the closed eyelid. The ophthalmic artery is identified superior and medial to the optic nerve, with the sample gate positioned 10-15 mm posterior to the globe. To ensure accuracy and reproducibility, an insonation angle of <20° is required, and measurements should be averaged from both eyes. Ophthalmic artery Doppler provides significant incremental value to screening algorithms. In the second trimester, adding the PSV ratio improves preterm pre-eclampsia detection from 72% to 89% at a 10% false-positive rate. The technique is particularly advantageous in resource-limited settings due to its low equipment requirements and rapid learning curve. Safety is maintained by adhering to the ALARA principle, specifically keeping the Mechanical Index (MI) < 0.23 and Thermal Index (TI) < 1.0. Ophthalmic artery Doppler is an accessible, safe, and reproducible tool for assessing maternal haemodynamics. Adhering to a standardised acquisition technique is essential for its successful integration into multimodal pre-eclampsia screening.

PMID 42546611
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PubMedSeminars in neurology2026-08-04

Neuro-ophthalmic Manifestations of Immunotherapy Toxicity.

Al-Abdulghani Abdulaziz A, Dugue Andrew A, Grossman Scott N SN, Gold Doria M DM

PMID 42546745
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