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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

PubMedMedicine2026-11-11

Staged surgical management of an acute angle-closure crisis with medically refractory intraocular pressure elevation: A case report and literature review.

Yin Yuecong Y, Chen Yingjie Y, Zhang Xiaofeng X, Yao Yu-Feng YF

Acute angle closure with markedly elevated intraocular pressure (IOP) is an ocular emergency. Initial management aims to lower IOP, reduce corneal edema and inflammation, and permit definitive relief of pupillary block, usually by laser peripheral iridotomy (LPI). When IOP remains uncontrolled and corneal edema or an extremely shallow anterior chamber precludes safe LPI, urgent surgical intervention may be required. A 61-year-old woman presented with a 7-hour history of pain, redness, and blurred vision in the right eye (RE), accompanied by headache. Acute primary angle closure in the RE and primary angle-closure suspect status in the left eye (LE). During initial treatment with topical pilocarpine, carteolol, and brinzolamide, IOP in the RE increased from 32 to 58 mm Hg. It remained markedly elevated despite 2 intravenous infusions of 20% mannitol (50 grams each), and emergency surgical peripheral iridectomy was performed. After the acute episode stabilized, the RE underwent phacoemulsification with intraocular lens implantation; the fellow eye subsequently underwent lens extraction with intraocular lens implantation. After peripheral iridectomy, IOP in the RE decreased from 58 to 11 mm Hg without additional IOP-lowering medication, and central anterior chamber depth increased from 1.24 to 1.60 mm. At 6 months after subsequent bilateral lens extraction, IOP was 14 mm Hg in the RE and 15 mm Hg in the LE without IOP-lowering medication. Central anterior chamber depth increased from 1.24 to 4.36 mm in the RE and from 2.27 to 4.35 mm in the LE. Uncorrected visual acuity was 20/20 in the RE and 20/33 in the LE, and best-corrected visual acuity was 20/20 in both eyes. Emergency surgical peripheral iridectomy may serve as a rescue procedure in selected patients with medically uncontrolled acute angle closure when LPI is not feasible. Subsequent lens extraction may relieve residual lens-related anterior-segment crowding. However, this single case cannot establish the comparative effectiveness of the staged approach or whether peripheral iridectomy followed by lens extraction is the optimal treatment sequence.

PMID 43012846
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PubMedElectrophoresis2026-11-04

Exploring Elimination Profiles and Metabolite Patterns of Brinzolamide and Dorzolamide After Transdermal Exposure for Doping Control Purposes.

Jin Yao Y, Thomas Andreas A, Thevis Mario M

Brinzolamide (BA) and dorzolamide (DA) are carbonic anhydrase inhibitors (CAIs), commonly used for glaucoma treatment via topical application. Under the World Anti-Doping Agency Prohibited List, both substances are prohibited in- and out-of-competition, except when administered ophthalmically. In anti-doping testing, adverse analytical findings (AAFs) may arise not only from intentional misuse but also from unintentional exposure or contamination. Although elimination characteristics after oral or ocular administration have been described, little is known about the systemic uptake and metabolic behaviour of these substances following dermal exposure. Therefore, the present study investigates the transdermal absorption of BA and DA under controlled conditions to characterize elimination profiles and metabolite patterns. Two groups of 12 volunteers received dermal applications of AZOPT brinzolamide (10 mg/mL) and TRUSOPT dorzolamide (20 mg/mL) at doses of 1 and 6 mg per substance, applied to the lower forearm skin. Urine samples were collected before application and up to 168 h post-application, and dried blood spot (DBS) samples were collected for up to 3 weeks. Samples were analysed by liquid chromatography-high-resolution tandem mass spectrometry (LC-HRMS/MS) for parent compounds and selected metabolites. Concentrations in DBS and urine samples were corrected for haematocrit (Hct) and urine specific gravity (SG), respectively. Subsequently, relative metabolite-to-parent ratios were calculated to describe matrix-dependent metabolic profiles after dermal exposure. BA and DA were detectable in both urine and DBS after transdermal application, with detection windows increasing in a dose-dependent manner. In the low-dose group, only four participants showed detectable urinary concentrations within the first 2 days post-application, whereas both compounds remained detectable in DBS for up to 3 weeks. High doses resulted in greater peak concentrations and prolonged detectability. Parent compounds and N-desethyl metabolites were identified, with matrix-dependent differences in detectability and relative abundance. Systemic absorption was confirmed at concentration levels that may lead to AAFs in routine doping controls.

PMID 42978470
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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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