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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

Mechanism of Action

Molecular Targets

timolol acts on 2 molecular targets:

ADRB1adrenoceptor beta 1 (B1AR, RHR)
ADRB2adrenoceptor beta 2 (B2AR, ADRBR)
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Therapeutic Indications

timolol is developed for 1 unique indication across 1 therapeutic area.

Therapeutic AreaConditionPhase
Eye disordersGlaucoma✓ Approved

Related Research Articles

PubMedCirugia pediatrica : organo oficial de la Sociedad Espanola de Cirugia Pediatrica2026-11-06

Topical timolol in the treatment of pediatric pyogenic granuloma: A 23-case series.

Sánchez Pulido L J LJ, Vega Mata N N, Enríquez Zarabozo E M EM, Granell Suárez C C et al.

Pyogenic granuloma (PG) is a common benign vascular lesion in pediatric patients, characterized by rapid growth and a tendency to bleed. Surgical excision allows immediate resolution and histological confirmation, with low recurrence when including the base of the lesion, although it may require anesthesia and leave a scar. Topical timolol has emerged as a conservative alternative in selected patients. To evaluate the efficacy and safety of topical timolol 0.5% in the treatment of PG in pediatric patients. Retrospective case series of 23 pediatric patients (4 months-13 years) diagnosed with PG and treated between 2018 and 2024 with a 0.5% timolol formulation applied topically over the lesion as an off-label use. Demographic and clinical variables, treatment duration, final response, need for surgery, recurrence, and documented adverse events were analyzed. Ten patients (43.5%) achieved complete or near-complete resolution of the lesion, 6 (26.1%) showed a partial response at the end of treatment or prior to surgery, 5 (21.7%) did not respond or exhibited progression, and 2 (8.7%) were still receiving treatment at data cutoff. Twelve patients completed treatment without surgery; at cutoff, 14 (60.9%) had not undergone surgery, including the 2 cases still under treatment. Nine patients (39.1%) required surgery. No recurrences were documented among patients with complete or near-complete resolution during available follow-up, and no adverse events attributable to treatment were recorded. Topical timolol 0.5% can be considered an initial conservative alternative in selected pediatric patients, especially when avoiding or deferring surgery or anesthesia is desired. Surgery remains a definitive option, offering immediate resolution and the possibility of histological confirmation. Prospective comparative studies are needed to define more precisely the role of timolol compared to surgical treatment.

PubMedIndian journal of pediatrics2026-11-05

Vision-Threatening Giant Hemifacial Infantile Hemangioma Successfully Treated with Oral Propranolol and Topical Timolol.

Sarkar Sumantra S, Bandyopadhyay Rakhi R, Raza Arsalan A

PubMedPediatric dermatology2026-11-04

Clinical Outcomes of Nasal Tip Infantile Hemangiomas: A Retrospective Cohort Study.

Belmesk Lina L, Coulombe Jerome J, Powell Julie J, Tehrany Yassaman Alipour YA et al.

Infantile hemangiomas (IH) are the most common vascular tumors in infancy. Nasal tip infantile hemangiomas (NTIH) are associated with high-risk disfigurement and long-term sequelae. Despite widespread use of propranolol, optimal management of NTIH remains incompletely defined. A retrospective cohort study included patients with NTIH evaluated between 2003 and 2019 at a pediatric referral center. Inclusion required confirmed diagnosis by two pediatric dermatologists, available clinical photographs, and ≥ 6 months of follow-up. Data collected included demographics, IH subtype, treatments, adverse events, and sequelae at 3 years old. Propranolol-treated patients were stratified by dose (≤ 2.5 vs. > 2.5 mg/kg/day). Fifty-eight patients met inclusion criteria. Propranolol was prescribed in 72.4% (n = 42), with a mean duration of 16.0 months. Adverse effects were predominantly mild (sleep disturbances, 20.7%). At 3 years of age, sequelae, particularly fibroadipose tissue, were significantly less frequent in propranolol-treated patients compared to those untreated (42.9% vs. 91.8%, p = 0.005; overall sequelae: 67.9% vs. 100%, p = 0.037). Sequelae rates did not differ between low- and high-dose propranolol groups. Combined propranolol and topical timolol was associated with increased telangiectatic sequelae, likely reflecting treatment selection bias. No association was found between IH subtype and sequelae. Systemic propranolol was associated with fewer long-term sequelae in NTIH, particularly fibroadipose tissue. A lower dose of 2 mg/kg/day appears sufficient in most cases. Topical timolol may provide limited additional benefit and should not delay propranolol initiation. These findings support early systemic propranolol as the standard of care in NTIH management.

PubMedArchives of medical research2026-10-27

Locus Coeruleus Stimulation Enhances Object Recognition Memory Persistence After Early-Life Stress Independent of Hippocampal Noradrenergic Signaling.

Neves Ben-Hur Souto das BSD, Lima Karine Ramires KR, Rosa Ana Carolina de Souza da ACSD, Gomes Gabriela Cristiane Mendes GCM et al.

Early-life stress, such as maternal deprivation (MD), is a stressor that can lead to cognitive deficits in adulthood. Among the neurochemical mechanisms involved in MD-induced pathophysiology are alterations in the dopaminergic and noradrenergic systems. We recently demonstrated that pharmacological stimulation of dopaminergic neurons in the ventral tegmental area (VTA) improves novel object recognition (NOR) memory in rats subjected to MD. Furthermore, projections from the locus coeruleus (LC) to the dorsal hippocampus (DH) are important for memory consolidation. From postnatal day (PND) 1-PND10, male and female rats were either subjected to MD or left undisturbed. In adulthood, the animals underwent stereotaxic surgery for bilateral cannulation of the DH and LC. Following recovery and habituation, the animals were trained in the NOR task and immediately received vehicle or timolol in the DH, and either vehicle or NMDA in the LC. NOR memory was assessed at 24 h, as well as 7 and 14 d after training, to evaluate memory consolidation and persistence, respectively. MD impaired NOR memory in male rats, but not in females. Pharmacological stimulation of the LC with NMDA promoted NOR memory persistence in both non-MD and MD males and females. In males, LC stimulation also reversed the MD-associated memory impairment. These effects were maintained despite hippocampal β-adrenergic receptor blockade with timolol. These findings suggest that LC-related pathways contribute to the processing of NOR memory persistence following early-life stress in a sex-dependent manner. This effect appears to be independent of hippocampal β-adrenergic signaling.

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.

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.

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