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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

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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PubMedFrontiers in medicine2026-09-24

Ectropion uveae in a pediatric patient with refractory NF1-associated glaucoma: a 4-year case report.

Geng Yulei Y, Li Weijia W, Shi Kuitang K, Li Yawen Y et al.

Glaucoma secondary to neurofibromatosis type 1 (NF1) is a vision-threatening complication characterized by variable phenotypic expression. The prognostic significance of specific anterior segment signs, particularly ectropion uveae (EU), remains unclear. We report a 7-year-old girl with NF1 who presented with unilateral refractory glaucoma and prominent EU in the affected eye. Despite maximal medical therapy and sequential surgical interventions, including microcatheter-assisted transluminal trabeculotomy, subsequent scar tissue excision with goniotomy, and two sessions of transscleral cyclophotocoagulation, intraocular pressure (IOP) remained uncontrolled. Implantation of a glaucoma drainage device (GDD) resulted in initial IOP reduction, with IOP maintained at 16/18 mmHg during the first 3 months. At 1 year post-GDD, IOP was 23 mmHg, and brinzolamide was subsequently added. This 4-year longitudinal case highlights an association between prominent ectropion uveae and a refractory surgical course in this patient. Traditional angle surgeries appeared to carry a high risk of failure, whereas GDD implantation provided IOP reduction from 42 to 23 mmHg at 1 year, although adjunctive medication was subsequently required. This observation raises the question of whether earlier GDD implantation might prove beneficial in similar patients. However, this hypothesis requires validation in a larger series.

PMID 42780616
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PubMedInvestigative ophthalmology & visual science2026-09-22

Adrenergic Pathways Mediate Circadian IOP Rhythm in Rats.

Zamitalo-Pomares Alexandra A, Passaglia Christopher L CL

This study sought to define adrenergic receptor mechanisms underlying circadian intraocular pressure (IOP) regulation in rats. IOP was monitored continuously via wireless telemetry in adult Brown-Norway rats entrained to the ambient light/dark (LD) cycle and then maintained in constant darkness (DD). Agonists and antagonists of β- (isoproterenol and timolol), α1- (phenylephrine and bunazosin), and α2- (brimonidine and yohimbine) receptors were applied topically to the cornea during subjective day (SD) and subjective night (SN) in DD. Drug effects were quantified by short-term changes in mean IOP and long-term changes in IOP rhythmicity. Animals exhibited a pronounced IOP rhythm in LD that persisted in DD. IOP was significantly reduced after SN instillation of timolol (DSN% = -110% ± 24%), bunazosin (DSN% = -107% ± 13%), yohimbine (DSN% = -106% ± 12%), and brimonidine (DSN% = -94% ± 18%) and was unchanged after SD instillation. Conversely, IOP was significantly elevated after SD instillation of phenylephrine (DSD% = 143% ± 62%) and isoproterenol (DSD% = 62% ± 19%) and was unchanged after SN instillation. None of the drugs altered IOP rhythm period or phase, but bunazosin abolished the rhythm for several days. Multiple adrenergic receptor pathways participate in the circadian regulation of rat IOP. All are necessary to raise IOP during SN since inactivation of any individual pathway drops IOP fully back to daytime levels. β- and α1-receptor activation is also singularly sufficient to raise IOP during SD to nighttime levels, whereas α2-receptors play a more complex role in IOP regulation.

PMID 42770657
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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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