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brimonidine + brinzolamide (SJP0135 / Ailamide / SJP 0135)

✓ Approved

Senju · ADRA2A · Small Molecule

What is brimonidine + brinzolamide?

brimonidine + brinzolamide is a small molecule developed by Senju. It is approved for therapeutic indications via others.

Drug Profile

Brand NamesSJP0135, Ailamide, SJP 0135
CompanySenju
Drug ClassSmall Molecule
Molecular TargetADRA2A, CA2
RouteOthers
StatusApproved
Sources: ClinicalTrials.gov, Senju

Mechanism of Action

Molecular Targets

brimonidine + brinzolamide acts on 2 molecular targets:

ADRA2Aadrenoceptor alpha 2A (ADRAR, ADRA2R)
CA2carbonic anhydrase 2 (CAII, HEL-S-282)
Want deeper analysis?Noah AI can explain complex mechanisms and compare to similar drugs.

Therapeutic Indications

brimonidine + brinzolamide is developed for 1 unique indication across 1 therapeutic area.

Therapeutic AreaConditionPhase
Eye disordersGlaucoma✓ Approved

Related Research Articles

PubMedMolecules (Basel, Switzerland)2026-08-27

Latanoprost Acid-Brimonidine, a New Amide Prodrug for Glaucoma Management Based on the Concept of Sustained Release.

Lin Hong-Jia HJ, Su Shih-Horng SH, Wu Wen-Chung WC

Glaucoma is an ocular disease caused by the improper management of elevated intraocular pressure (IOP). IOP-lowering via topical administration is the first choice to prevent further progression. However, patients may forget to administer their medication, compromising IOP control. To address this problem, a prolonged active pharmaceutical ingredient (API) release system is proposed. A new prodrug (latanoprost acid-brimonidine conjugate, LBJ) was designed and expected to achieve potential long-lasting release of APIs. LBJ was synthesized by two methods. First, Steglich esterification without protecting the hydroxyl group led to a yield of 34.24%. However, the integral ratio between LPA and BM obtained from NMR was 1.25:1, indicating a potential side product resulting from further coupling through the unprotected hydroxyl group in LBJ. As an alternative route, Steglich esterification with a protecting agent, tert-butyldimethylchlorosilane (TBDMSCl), resulted in a yield of 39.35%, and the integral ratio between LPA and BM obtained from NMR was 1:1. The hydrolysis time of LBJ was investigated and compared with that of latanoprost (LP). In the presence of esterase (0.4 U/mL), the hydrolysis times of LP and LBJ were 4 h and 28 days, respectively. The prolonged hydrolysis time results in sustained APIs release, which is beneficial for the development of a sustained drug release system.

PMID 42653864
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PubMedExperimental eye research2026-08-20

Intraocular pressure reduction attenuates form-deprivation myopia by modulating scleral extracellular matrix remodeling via the TGF-β1/Smad signaling pathway.

Ju Hong H, Wang Hao H

This study aimed to investigate whether intraocular pressure (IOP) reduction achieved separately using two mechanistically distinct IOP-lowering agents, brinzolamide and latanoprost, attenuates form-deprivation myopia (FDM) by regulating scleral extracellular matrix (ECM) dynamics and to elucidate the underlying involvement of the TGF-β1/Smad signaling pathway. We established a murine model of unilateral FDM with the contralateral untreated eye serving as an intra-individual control and assessed key ocular parameters, including IOP, axial length (AL), and refractive error (RE). Scleral tissues were subjected to hematoxylin and eosin (H&E) staining and Western blot analysis. Primary human scleral fibroblasts (HSFs) were exposed to hypoxia to mimic myopic stress, and cell viability, proliferation, and apoptosis were evaluated using Cell Counting Kit-8 (CCK-8), 5-ethynyl-2'-deoxyuridine (EdU), flow cytometry, and terminal deoxynucleotidyl transferase dUTP nick end labeling (TUNEL) assays. Protein expression of ECM-related markers and key components of the TGF-β1/Smad pathway was analyzed by Western blot. The functional role of the TGF-β1/Smad axis was further examined using the selective inhibitor LY2109761. IOP reduction induced separately by brinzolamide and latanoprost (via distinct mechanisms of action) effectively attenuated IOP elevation, axial elongation, and myopic shift in FDM mice, accompanied by preserved scleral architecture and normalized expression of type I collagen, matrix metalloproteinase-2 (MMP2), tissue inhibitor of metalloproteinase-2 (TIMP-2), and α-smooth muscle actin (α-SMA). In HSFs under hypoxia, both IOP-lowering agents exerted consistent protective effects, restoring cell viability and proliferation, suppressed apoptosis, and reversed hypoxia-induced ECM dysregulation. These protective effects were associated with upregulation of TGF-β1, phosphorylated Smad2 (p-Smad2), and phosphorylated Smad3 (p-Smad3) in both in vivo and in vitro models. Co-treatment with LY2109761 completely abolished the beneficial effects of IOP reduction on ocular biometry, scleral structure, cellular function, and ECM protein expression. Intraocular pressure reduction achieved separately via two mechanistically distinct pharmacological approaches mitigates FDM by preserving scleral integrity through modulation of ECM remodeling, an effect mediated via activation of the TGF-β1/Smad signaling pathway.

PMID 42624236
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PubMedSeminars in ophthalmology2026-08-10

Efficacy and Safety of Aceclidine in Presbyopia, a Systematic Review and Meta -Analysis.

Ibrahim Taha T, Burhan Muhammad M, Bin Shafiq Shaheer S, Razzak Muhammad Junaid MJ et al.

Presbyopia is a prevalent age-related visual disorder affecting approximately 1.8 billion individuals worldwide, with many lacking access to effective correction. Topical pharmacologic therapies such as aceclidine have emerged as potential noninvasive treatments, though their efficacy and safety remain incompletely established. A systematic review and meta-analysis of randomized controlled trials was conducted in accordance with PRISMA guidelines (PROSPERO: CRD420261353653). Databases were searched till March 2026. Adults with presbyopia treated with topical aceclidine, alone or in combination, were included. The primary outcome was ≥ 3-line improvement in distance-corrected near visual acuity (DCNVA). Random-effects models were used to calculate pooled risk ratios (RR) with 95% confidence intervals (CI). Five trials involving 883 randomized participants were included. In the primary analysis of parallel-group trials, aceclidine significantly increased the likelihood of achieving a ≥ 3-line improvement in distance-corrected near visual acuity compared with placebo (RR 6.28, 95% CI 4.22-9.35; I2 = 2.4%) and compared with aceclidine plus brimonidine (RR 5.05, 95% CI 3.04-8.38; I2 = 28.2%). Secondary analyses of crossover trials demonstrated similar superiority over placebo (RR 14.92, 95% CI 6.77-32.86; I2 = 0%), whereas no significant difference was observed versus combination therapy (RR 1.11, 95% CI 0.90-1.38; I2 = 24.6%). Aceclidine was associated with a higher incidence of treatment-emergent adverse events than placebo (RR 2.23, 95% CI 1.61-3.09). No significant differences were observed in serious adverse events. Aceclidine provides significant short-term improvement in near vision with an acceptable safety profile. Monotherapy may offer slight efficacy benefits over combination regimens. However, limited study numbers and short follow-up necessitate further large-scale, long-term trials.

PMID 42574210
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PubMedInternational journal of pharmaceutics2026-08-04

Solid-state effects of Brinzolamide on sustained intravitreal release from hot-melt extruded PLGA implants.

Sorsa Teemu T, Pilipenko Iuliia I, Valkama Eetu E, Kähärä Helena H et al.

Intravitreal (IVT) injections treat diseases of the posterior eye segment, but frequent dosing limits patient compliance and increases costs. Some long-acting IVT implants are available but further understanding of polymer behavior and solid-state properties is required to expand this space for more drug molecules and generic formulations. We evaluated four poly(D,L-lactide-co-glycolide) (PLGA) polymers varying in lactide content and molecular weight, and one poly(D,L-lactide) (PLA), as rod-shaped IVT implants. Brinzolamide (BRZ) was used as a model drug because its melting point (130°C) enables production of hot-melt extruded implants containing amorphous (Textrusion > Tm) or crystalline (Textrusion < Tm) drug. Implants (0.2 × 20 mm) were characterized for impurities, endotoxin levels, solid-state properties, and microstructure. Drug release was assessed using in vitro model with artificial vitreous and saline compartments. IVT elimination of BRZ solution in rabbits (n = 12) occurred mostly via posterior route (aqueous humor (AH)/ vitreous humor (VH) AUC ratio 0.0053). In vitro release data, combined with in silico simulations, guided implant selection and dosing for the in vivo study. Two selected amorphous implants were administered intravitreally via trocar into rabbits (n = 8/implant). BRZ release was sustained over 42 days in vitro and in vivo, with AH levels < 1 % of VH. The in vitro model produced good in vitro-in vivo correlation. Crystalline implants exhibited faster, dissolution-driven release from a porous, non-uniform structure. Amorphous implants showed slower, PLGA degradation-limited release from a homogeneous matrix. These findings demonstrate that drug solid-state critically determines implant microstructure and release mechanisms in PLGA-based IVT systems.

PMID 42546989
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PubMedAdvanced materials (Deerfield Beach, Fla.)2026-08-03

An E-interwoven Therapeutic Contact Lens System for Rapid Drug Delivery and Precision Dose Monitoring.

Yang Huan H, Zhu Hengtian H, Teng Wenyu W, Huang Heyu H et al.

Precise intraocular pressure (IOP) management and rapid intervention preserve glaucoma vision, yet current ocular delivery systems lack in situ dosage verification, causing treatment blind spots. Here, we develop a wireless therapeutic smart contact lens (SCL) containing a rapid voltage-triggered drug delivery system with a real-time dosage monitoring sensor. The e-interwoven design integrates drug delivery and sensing electrodes in an ultra-thin (17.4 µm) tri-interdigital configuration, which enables the electric field to interact with the drug-loaded hydrogel in the same spatial region. A frequency-matching strategy boosts voltage coupling to drive a brimonidine tartrate-loaded hydrogel to achieve high concentrations in the aqueous humor in 20 min, significantly faster than topical eye drops. The built-in drug dose sensor has a high accuracy <2.8 µg, benefiting from the great linear correlation between wireless frequency drift and release dosage. In acute glaucoma rabbit models, this SCL suppresses peak IOP elevation by 85.7% compared to eye drops. This SCL presents a highly integrated therapeutic platform demonstrating potential for rapid and precise glaucoma treatment.

PMID 42544728
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PubMedIndian journal of ophthalmology2026-07-31

Evaluation of the effect of brinzolamide 1% ophthalmic suspension on nystagmus using videonystagmography.

Kassem Rehab Rashad RR, Hamdy Hussein Sherif HS, Hassanein Dina Hossameldin DH, El-Mofty Randa Mohamed Abdel-Moneim RMA

To evaluate the effect of topical brinzolamide (Azopt) eye drops on nystagmus using videonystagmography in infants and children. Setting: Institutional (Cairo University Hospitals). Study population: Both eyes of 40 patients, presenting with nystagmus, with a maximal age of 14 years, were included in this prospective, nonrandomized, unmasked study. Intervention: Clinical evaluation and videonystagmography were carried out on entry, at 1 month, and 6 months of Azopt instillation and 1 month after its discontinuation. Azopt was stopped at 1 month in case of deterioration. Main outcome measures: The primary outcome of the study was the change in nystagmus intensity at 4 weeks of Azopt treatment, based on videonystagmography. Mean age was 5.7 ± 3.3 years. There was a significant decrease in mean nystagmus amplitude from 8.39 ± 7.67, on entry, to 5.95 ± 5.31, 5.27 ± 4.64, and 4.18 ± 3.65 degrees at 1 month, 6 months, and 1 month after discontinuation ( P < 0.05). There was a significant decrease in slow phase velocity (SPV) from 29.53 ± 22.19, on entry, to 20.43 ± 18.62 degrees/second at 6 months, and in nystagmus intensity from 1018.4 ± 1530.9, on entry, to 319.3 ± 322.05 at 6 months ( P < 0.05). Decrease in nystagmus frequency and visual improvement were insignificant ( P > 0.05). At 1 month, nystagmus intensity decreased in 62.5%, but increased in 32.5%. No side effects were documented. Azopt eye drops significantly reduced nystagmus in infants and children, without side effects. Worsening of nystagmus was, however, noted in around one-third of the cases, so close follow-up is essential for timely discontinuation.

PMID 42535814
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