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brimonidine + brinzolamide (SJP0135 / Ailamide / SJP 0135)

✓ Approved

Senju · ADRA2A · 小分子

什么是 brimonidine + brinzolamide?

brimonidine + brinzolamide 是一种小分子,由Senju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SJP0135, Ailamide, SJP 0135
公司Senju
药物类别小分子
分子靶点ADRA2A, CA2
给药途径Others
状态Approved

作用机制

分子靶点

brimonidine + brinzolamide 作用于 2 个分子靶点:

ADRA2Aadrenoceptor alpha 2A (ADRAR, ADRA2R)
CA2carbonic anhydrase 2 (CAII, HEL-S-282)
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

brimonidine + brinzolamide 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

PubMedCureus2026-10-25

Topical Carbonic Anhydrase Inhibitors in Macular Edema: A Systematic Review.

Sadr Ata A, Maleki Alireza A, Asadollahi Mohammadreza M, Maleki Shahaboddin S et al.

In order to systematically evaluate the efficacy and safety of topical carbonic anhydrase inhibitors (CAIs) in the treatment of macular edema across different retinal disorders, a systematic review was conducted in accordance with the Preferred Reporting Items for Systematic Reviews and Meta-Analyses (PRISMA) guidelines. PubMed, Scopus, Web of Science, and the Cochrane Library were searched from inception to June 13, 2026, without language or publication date restrictions. Clinical studies evaluating topical dorzolamide or brinzolamide for macular edema of any etiology were included. Data regarding study characteristics, treatment protocols, visual and anatomical outcomes, and follow-up were extracted independently by two reviewers. Twenty-eight studies met the inclusion criteria, comprising randomized controlled trials, quasi-experimental studies, cohort studies, case series, and one analytical cross-sectional study. Overall, the included studies were of moderate-to-high methodological quality. Retinitis pigmentosa-associated cystoid macular edema was the most frequently investigated condition (13 studies), followed by X-linked retinoschisis (10 studies), diabetic macular edema (four studies), and one macular edema following vitrectomy and epiretinal membrane removal. Topical dorzolamide was the most commonly evaluated agent, whereas topical brinzolamide was investigated less frequently. Across retinal disorders, topical CAIs consistently reduced central macular thickness and improved retinal morphology as assessed by optical coherence tomography. Functional outcomes were more variable, with improvements in best-corrected visual acuity observed primarily in selected patients with retinitis pigmentosa and diabetic macular edema, whereas visual gains were generally modest in X-linked retinoschisis. Long-term studies reported recurrence of macular edema despite continued treatment, particularly in retinitis pigmentosa. Topical CAIs were well tolerated, with no serious ocular or systemic adverse events reported. Topical CAIs provide consistent anatomical improvement in macular edema, particularly in inherited retinal disorders, while functional benefits are less predictable. This discrepancy between anatomical and functional outcomes may be attributed to prolonged photoreceptor loss, retinal pigment epithelium dysfunction, and irreversible disruption of the ellipsoid zone. Their favorable safety profile and non-invasive administration support their use as a therapeutic option, especially for retinitis pigmentosa-associated cystoid macular edema and selected cases of X-linked retinoschisis and diabetic macular edema. However, the current evidence is limited by predominantly observational studies and clinical heterogeneity. Well-designed multicenter randomized controlled trials are needed to establish their optimal role in the management of macular edema.

PMID 42923813
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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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PubMedBMJ case reports2026-10-20

Management of brimonidine-associated uveitis and conjunctivitis.

Amrani Yasmina Y, Ameli Shervine S, Verhulst Karen K, Dugauquier Artemise A

PMID 42901699
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PubMedCureus2026-10-19

Post-acne Erythema: A Systematic Review of Randomized Controlled Trials on the Comparative Efficacy and Safety of Interventions Across Clinical, Instrumental, and Patient-Reported Outcomes.

Alhussain Ahmed A, Majrashi Mohammad M, Omar AlMubarak Khalid K, Faleh Alqahtani Rayan R et al.

Post-acne erythema (PAE) is a persistent acne sequela without an established standard treatment. This systematic review evaluated the comparative efficacy and safety of interventions tested in randomized trials. PubMed/MEDLINE, Scopus, and Web of Science were searched from inception through August 1, 2026. Randomized parallel-group and split-face trials reporting erythema outcomes were eligible. Risk of bias was assessed with the Cochrane Risk of Bias 2 (RoB 2) tool. Heterogeneity precluded meta-analysis, and available findings were synthesized narratively. Nine trials involving 301 participants contributed 11 pairwise comparisons. Against untreated or blank controls, favorable effects were reported for picosecond alexandrite laser, narrow-spectrum vascular intense pulsed light (IPL), and non-cross-linked hyaluronic acid mesotherapy. A 577-nm semiconductor laser showed interim instrumental benefit, but blinded assessors found no final between-side difference. In active-treatment and add-on comparisons, narrow-spectrum IPL was favored over broad-spectrum IPL, neodymium-doped yttrium aluminum garnet (Nd) laser added to low-dose isotretinoin was favored over isotretinoin alone, and 577-nm pro-yellow laser was favored over topical brimonidine. Botulinum toxin type A was favored over broadband light at the earliest assessment only. Fractional laser and pulsed dye laser did not differ significantly, while delicate pulsed light and Q-switched 1064-nm Nd laser showed no sustained difference at the final assessment. Adverse events were mild and transient, although pigmentation and blistering occurred with one broad-spectrum IPL protocol. Five trials had some concerns, and four had high overall risk of bias. Trials suggested potential benefits, but small samples, heterogeneity, short follow-up, and reporting limitations precluded identification of a preferred treatment. Larger, prospectively registered trials using blinded assessment and standardized outcomes are needed.

PMID 42894818
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PubMedPharmaceutical development and technology2026-10-07

Chitosan-modulated niosomes for improved ocular delivery of brinzolamide.

Sobhy Marina K MK, Abdelaziz Abdelaziz E AE, Mazyed Eman A EA, Youssef Ahmed A A AAA et al.

Brinzolamide (BZ) is considered a promising pharmaceutical agent for lowering elevated intraocular pressure (IOP). However, its poor aqueous solubility limits its ocular bioavailability. Niosomes showed promising potential in ophthalmic delivery. Chitosan coating may extend the benefits of niosomes by imparting mucoadhesive potential. The aim of this investigation was to explore the potential of chitosan-coated niosomes (CS-niosomes) for improving the ocular delivery of BZ. Standard niosomes composed of Span 60, cholesterol, and ursodeoxycholic acid were loaded with BZ. The same system was coated with chitosan to provide CS-niosomes. Niosomes morphology, size, BZ entrapment efficiency and release were determined. The IOP-lowering effect of BZ-loaded niosomes was monitored after ocular administration in rabbits with experimentally induced glaucoma using lab-prepared suspension and marketed eye drops (Azopt®) as control. Standard niosomes and CS-niosomes were spherical vesicles having size of 193.50 and 159.90 nm, respectively. BZ was entrapped with efficiency of 90.02% and 88.43% in both systems, respectively, with no significant difference observed in their release behaviour. With respect to IOP-lowering ability, CS-niosomes > standard niosomes > Azopt® > lab-prepared suspension with CS-niosomes preserving the efficacy even after 10 h. This study demonstrated the potential of CS-niosomes as a promising nanocarrier for enhanced ocular delivery of BZ.

PMID 42839783
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PubMedOphthalmology and therapy2026-10-06

Association of Topical Therapy and Surgical Management with Corneal Parameters in Congenital PAX6-Related Classical Aniridia: a Cross-Sectional Study.

Li Yubo Y, Grünauer-Kloevekorn Clara C, Csidey Mária M, Náray Annamária A et al.

This study aimed to investigate associations of topical therapy and surgical management with the severity of aniridia-associated keratopathy (AAK), limbal stem cell deficiency (LSCD) and corneal microstructural alterations in patients with PAX6-related congenital aniridia (CA). This cross-sectional study included eyes with genetically confirmed CA. Medical history, including preservative-free artificial tears, antiglaucoma medications (beta-blockers, brimonidine, carbonic anhydrase inhibitors, prostaglandin analogues), and ocular surgery was recorded. AAK and LSCD were graded. Anterior segment optical coherence tomography (AS-OCT) assessed epithelial and total corneal thickness, while in vivo confocal microscopy (IVCM) assessed subbasal nerve plexus parameters, Langerhans cell density (LCD), and stromal keratocyte density. Associations were analyzed using generalized estimating equations. Sixty-one eyes of 31 patients were analyzed. More advanced AAK and LSCD were associated with more frequent preservative-free artificial tear use. Antiglaucoma medications were associated with differences in corneal thickness, keratocyte and Langerhans cell densities, and subbasal nerve plexus parameters. Prostaglandin analogue use was associated with a heterogeneous pattern, including higher corneal nerve fiber density and length, higher middle stromal keratocyte density, and lower LCD. Previous ocular surgery showed limited associations with corneal microstructural parameters but was associated with lower corneal nerve network complexity. All findings were exploratory and hypothesis-generating. Topical therapy use is associated with differences in corneal structural and cellular parameters in congenital aniridia. Preservative-free artificial tear use is associated with more advanced AAK and LSCD, while antiglaucoma medications are associated with differences in corneal thickness, keratocyte and Langerhans cell densities, and corneal nerve parameters. Prostaglandin-treated eyes show a heterogeneous pattern of associations with corneal microstructural parameters. Given the cross-sectional design, whether these treatment-associated differences reflect medication effects, underlying disease severity, treatment selection, concomitant therapies, or residual confounding cannot be determined. These findings require longitudinal confirmation.

PMID 42837043
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