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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
来源： ClinicalTrials.gov, Senju

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

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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PubMedSouth Dakota medicine : the journal of the South Dakota State Medical Association2026-07-29

Abstract: Recognizing Early Signs of Primary Congenital Glaucoma in Infancy.

Withrow Alexander D M ADM, Schuch Jeffrey J, Frick Michael M, Withrow David W M DWM

Primary congenital glaucoma (PCG) is a rare and vision-threatening condition caused by abnormal development of the anterior chamber angle, leading to impaired aqueous humor outflow and subsequent elevated intraocular pressure. Although uncommon, PCG remains an important cause of irreversible visual impairment in the pediatric population. Early recognition is critical, as delayed diagnosis may result in optic nerve damage, amblyopia, and permanent vision loss. Classic clinical findings include epiphora, photophobia, blepharospasm, corneal clouding, and increased corneal diameter. This report describes an early presentation of PCG in a previously healthy infant and emphasizes the importance of prompt referral and surgical management. A three-month-old male with no significant past medical history presented to pediatric clinic with a one-day history of progressive eye swelling, cloudy pupils, and fussiness. Patient's mother denied respiratory symptoms, fever, or ocular discharge. Patient was born at term via uncomplicated vaginal delivery. Prior examinations documented normal pupillary responses and bilateral red reflex. On examination, the right eye appeared cloudy with an absent red reflex, prompting same-day referral to pediatric ophthalmology. Evaluation revealed right corneal clouding and elevated intraocular pressures of 26 and 24 mmHg. The patient was started on topical brinzolamide. At follow-up two days later, the corneal clouding had improved; however, intraocular pressures increased to 37 and 45 mmHg. The patient was diagnosed with primary congenital glaucoma and referred to a tertiary pediatric glaucoma center for surgical management. He subsequently underwent bilateral canaloplasty and trabeculotomy with additional revisions and continued ophthalmologic follow-up. This case highlights the importance of rapid identification of primary congenital glaucoma in early infancy. Subtle findings, including corneal clouding and abnormal red reflex, should prompt urgent ophthalmologic evaluation. Early diagnosis and surgical intervention are essential to reduce intraocular pressure, prevent optic nerve damage, and preserve visual function.

PMID 42525993
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PubMedThe Enzymes2026-07-23

Challenges and opportunities for developing selective carbonic anhydrase inhibitors and activators for vertebrate isoforms.

Supuran Claudiu T CT

Carbonic anhydrase (CA, EC 4.2.1.1) inhibitors of the sulfonamide/sulfamate type, such as acetazolamide, thiazides/high-ceiling diuretics, methazolamide, ethoxzolamide, dichlorophenamide, dorzolamide, brinzolamide, antiepileptics (sulthiame, topiramate, zonisamide), or non-steroidal anti-inflammatory agents such as celecoxib and polmacoxib, are effective inhibitors of most CA isoforms present in vertebrates but their clinical use in various pathologies is associated with side effects. Significant efforts were done in the last decades for developing isoform-selective inhibitors for all 12 catalytically active mammalian isoforms, with important results being obtained by using the tail approach or by the discovery of new inhibitory chemotypes, such as the coumarins and their derivatives, the boron/selenium-containing compounds, etc. SLC-0111, an antitumor sulfonamide in clinical development is an example of a successful strategy emerged by using the tail approach, this compound being a selective inhibitor of the tumor-associated isoforms CA IX and XII. Coumarins, sulfocoumarins and some boron-containing compounds show significant levels of isoform-selective inhibition against many CA isoforms too. Few compounds, on the other hand, show selectivity for inhibiting microbial over vertebrate isoforms, which is a considerable challenge for developing anti-infectives based on CA inhibitors. At the moment, only coumarins act as class-selective inhibitors for α- and η-CAs, not inhibiting significantly other CA classes (β-, γ-, δ-, ζ-, θ- and ι-CAs). Selective CA activators for the mammalian isoforms are not available yet, although they might lead to relevant pharmacological applications for the management of neurodegenerations, emotional memory disorders, obsessive-compulsive disorders, phobias, post-traumatic stress. Finding more effective isoform-selective and more importantly, class-selective modulators of activity for vertebrate CAs might afford opportunities for innovative therapeutic/pharmacological applications.

PMID 42486552
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PubMedThe Enzymes2026-07-23

Carbonic anhydrases I and II.

Supuran Claudiu T CT, Capasso Clemente C

Carbonic anhydrase (CA, EC 4.2.1.1) isoforms I (CA I) and II (CA II) are widespread cytosolic proteins in most vertebrates. They are abundant in the red blood cells and many other tissues, being involved in physiological processes such as pH regulation, CO₂/bicarbonate homeostasis, respiration, and secretion of electrolytes rich in acid or bicarbonate in the stomach, kidneys, cerebrospinal fluid, eyes, and bones. The genetics, biochemistry, expression, localization in tissues and organs, kinetic properties, and catalytic mechanisms of these enzymes are well understood at the molecular level. At least five different inhibition mechanisms were described with more than 50 chemotypes acting as inhibitors. The activation with amine/amino acid activators was also well studied. The physiological role of CA I is poorly understood, whereas CA II is a physiologically dominant isoform, playing crucial functions in a host of tissues/organs. Interfering with its activity by means of inhibitors has been and is currently exploited in therapy for the management of edema, glaucoma, epilepsy, obesity, acute mountain sickness, and idiopathic intracranial hypertension. Promising preclinical data pointed to the potential use of CA II inhibitors for the management of other conditions, such as neuropathic pain, cerebral ischemia, rheumatoid arthritis, Alzheimer's disease, osteoporosis, and obstructive sleep apnea. Many CA inhibitors are in clinical use for the management of such conditions, among which are acetazolamide, thiazides and high-ceiling diuretics, methazolamide, ethoxzolamide, dichlorophenamide, dorzolamide, brinzolamide, and antiepileptics such as sulthiame, topiramate and zonisamide, whereas SLC-0111 is in clinical development as an antitumor agent. CA activators are not yet used clinically, but they might have pharmacological applications in the management of neurodegeneration, emotional memory disorders, obsessive-compulsive disorders, phobias, generalized anxiety, and post-traumatic stress. Finding novel modulators of activity for these enzymes may lead to innovative therapeutic applications and deepen our understanding of enzymes, their inhibitors, and their activators.

PMID 42486551
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