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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

PubMedBiomacromolecules2026-09-14

Mucoadhesive Carboxymethyl Chitosan Hydrogel Eyedrops via Dual Dynamic Covalent Chemistry for Long-Acting Glaucoma Therapy.

Pan Jin J, Gong Huangkun H, Shao Qiuyun Q, Zhang Xuehan X et al.

Glaucoma, a leading cause of irreversible blindness, is commonly treated with topical eye drops that reduce intraocular pressure (IOP), but their efficacy is limited by rapid precorneal clearance. To address this, we developed a dynamic hydrogel (CSFP) via Schiff base bonding between carboxymethyl chitosan (CMCS) and 4-formylphenylboronic acid (FPBA) as an advanced delivery vehicle for brimonidine (BRI) and timolol (TIM), two common IOP-lowering agents. The mechanical properties were tunable by adjusting CMCS and FPBA concentrations. The optimized hydrogel exhibited a storage modulus of ∼38.8 Pa (at 1 Hz, 1% strain), excellent self-healing ability, and shear-thinning behavior, facilitating easy administration and resistance to blink-induced clearance. It also achieved near 100% transmittance and a refractive index of 1.339, ensuring optical clarity. Notably, the incorporated phenylboronic acid (PBA) groups enabled selective binding to sialic acid residues on ocular mucins via dynamic phenylboronic ester bonding, prolonging precorneal retention beyond 30 min compared to less than 5 min for the solution control. In a magnetic bead-induced ocular hypertensive rat model, CSFP hydrogel loaded with either BRI or TIM induced greater and long-lasting IOP reduction than the free drug solutions. This work highlights the potential of mucoadhesive dynamic covalent hydrogels for advanced ocular drug delivery.

PMID 42734286
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PubMedTherapeutic delivery2026-09-11

Soluble ocular insert of brinzolamide and timolol maleate: in-vitro, ex-vivo and in-vivo characterization.

Prajapati Nikunj N, Vaghela Priyal P, Thakkar Hetal H

The present study aimed to formulate and evaluate a novel transparent and soluble ocular insert containing a fixed-dose combination of Brinzolamide (210 µg) and Timolol maleate (105 µg). The soluble ocular inserts were formulated using hydroxypropyl methylcellulose (HPMC) and polyvinyl alcohol (PVA) as film-forming polymers. Optimization of the parameters was done using a D-optimal design. The optimized soluble ocular inserts were found to be transparent, homogeneous, flexible and demonstrated acceptable surface pH (7.21 ± 0.12), bioadhesive strength (11.88 ± 0.89 g), and tensile strength (1.016 ± 0.13 MPa). In-vitro studies demonstrated sustained drug release up to 24 h following Higuchi kinetics. Ex-vivo permeation across goat cornea and in-vivo pharmacodynamic studies demonstrated enhanced and prolonged intraocular pressure reduction compared to the marketed suspension. The short-term stability testing indicated that the ocular insert retained the characteristics of %Transmittance, pH, Assay and % drug release. Overall, the results suggest that for better therapeutic efficacy and adherence in glaucoma treatment, the dual-drug loaded ocular insert provides a new, patient-friendly substitute for traditional ophthalmic dosage forms.

PMID 42725422
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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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