eye disease

SPHINX31 is a potent inhibitor of serine/arginine-rich protein kinase 1 (SRPK1; IC50: 5.9 nM).

Lifitegrast (SAR 1118) is an antagonist of lymphocyte function-associated antigen-1.

Soraprazan (BYK61359) is a selective potassium channel inhibitor that inhibits gastric acid secretion and ameliorates age-related eye disease by removing lipofuscin from retinal pigment epithelial (RPE) cells.

CBS-1114 HCl (N-Phenylbenzamidrazone hydrochloride) is a 5-lipoxygenase inhibitor and an anti-inflammatory compound in a good eye-permeable model.CBS-1114 HCl maintains and improves cardiac function, attenuates cardiac dysfunction, as well as reduces epicardial adipose tissue and/or pericardial adipose tissue in subjects with cardiovascular disease.

EYE-003 is an orally active RPE65 inhibitor with an IC50 value of 102 nM. It regulates the visual cycle in mice by decreasing the synthesis of 11-cis-Retinal (11cRAL) and increasing all-trans-retinyl esters (atREs). EYE-003 also inhibits dark-adapted electroretinogram (ERG) b-wave amplitudes and provides protection against retinal degeneration in Abca4⁻/⁻Rdh8⁻/⁻ mice by dose-dependently reducing retinal autofluorescent spots and preserving outer nuclear layer (ONL) thickness. EYE-003 is applicable for researching retinal disorders related to the visual cycle, such as Stargardt disease type 1 (STGD1).

EYE-002 is an RPE65 inhibitor with an IC50 of 69 nM. It enhances the recovery of dark-adapted electroretinogram (ERG) a-/b-wave amplitudes in mice. EYE-002 regulates the visual cycle in mice by reducing 11-cisretinal (11cRAL) synthesis and increasing all-trans-retinyl esters (atREs). It offers protective effects against light-induced retinal damage in mice. EYE-002 is valuable for research on retinal disorders related to the visual cycle, such as Stargardt disease type 1 (STGD1).

R-932348 choline, a dual JAK/SYK inhibitor, is used potentially for treatment of dry eye disease.

Sequifenadine has the potential in researching of inflammatory eye disease with allergic symptoms that is a H1-antihistamine [1] [2].

TOP1362 is a Narrow Spectrum Kinase Inhibitors Demonstrate Promise for the Treatment of Dry Eye Disease and Other Ocular Inflammatory Disorders. TOP1362 strongly inhibited the kinase targets p38α, Syk, Src, and Lck, blocked the rise in p38α expression in hyperosmolar Chang cells, and potently reduced inflammatory cytokine release in cellular models of innate and adaptive immunities. In the EIU model, TOP1362 dose-dependently attenuated the LPS-induced rise in inflammatory cell infiltration and ocular cytokine levels with efficacy comparable to that of dexamethasone.

Diquafosol Tetrasodium is a P2Y2 receptor agonist that stimulates the secretion of mucins from ocular tissues Diquafosol tetrasodium (INS365) improves tear film stability and visual function, as a topical treatment of dry eye disease.

UBX1325, a Bcl-xL inhibitor, enhances apoptosis in senescent cells, serving as an effective anti-aging agent. It holds potential for age-related eye disease research, including diabetic macular oedema (DME), age-related macular degeneration (AMD), and diabetic retinopathy (DR) [1].

Lonigutamab (hz208F2-4) is a humanized monoclonal antibody targeting the insulin-like growth factor-1 receptor (IGF-1R) for the study of thyroid eye disease.

Batoclimab (RVT-1401) is a fully humanized immunoglobulin G1 (IgG1) monoclonal antibody that specifically targets the neonatal Fc receptor (FcRn) with high affinity for the IgG-binding site on FcRn, and by competitively binding to this site, Batoclimab effectively blocks FcRn-mediated recycling of immunoglobulin G (IgG), resulting in the enhanced degradation of IgG and subsequent reductions in circulating IgG levels, making it a candidate compound for research in autoimmune diseases such as myasthenia gravis and thyroid eye disease.

JAK-IN-30 (compound 31) is a water-soluble Janus kinase (JAK) inhibitor with IC50 values of 2 nM for JAK2, 15 nM for JAK1, 18 nM for JAK3, and 2 nM for TYK2, identified for its research potential in treating dry eye disease (DED) [1].

Veligrotug is an intravenously administered anti-insulin-like growth factor-1 receptor antibody developed for the treatment of thyroid eye disease (TED). Veligrotug has demonstrated rapid reductions in diplopia as well as improvements in orbital inflammation, thereby highlighting its potential as a targeted biologic research tool in autoimmune ophthalmopathy.

Kynurenic acid, an active metabolite of tryptophan, is synthesized through a kynurenine intermediate by kynurenine aminotransferases (KATs). It acts as an antagonist of both NMDA and AMPA receptors, as well as α7 nicotinic acetylcholine receptors (nAChRs; EC50s = 235, 101, and 7 µM, respectively), and functions as an agonist for the aryl hydrocarbon receptor (AhR) and G protein-coupled receptor 35 (GPR35; EC50s = 1.4 and 39 µM, respectively). In a neonatal rat model of cerebral hypoxic-ischemia, induced by carotid artery ligation, administration of kynurenic acid at 300 mg/kg prevents weight loss in the lesioned hemisphere. Additionally, at concentrations of 1 and 5 mg/ml, it protects against neurodegeneration in the rhabdomere of the eye in an Htt93QtransgenicDrosophila model of Huntington's disease. Elevated levels of kynurenic acid in the cerebrospinal fluid have been observed in patients with schizophrenia.

VRDN-002 is a humanized monoclonal antibody (mAb) targeting IGF1R/CD221. It is designed to reduce inflammation and exophthalmos associated with thyroid eye disease (TED). Additionally, VPI-2690B is utilized in research related to Graves' ophthalmopathy.

Elegrobart is an immunoglobulin G1-κ monoclonal antibody that targets the human insulin-like growth factor 1 receptor (IGF1R). It shows potential for research into diseases linked to abnormal IGF1R signaling, particularly thyroid eye disease.

Vezocolmitide, a collagen-mimicking peptide, is a component of ST-100. It is applicable in the study of dry eye disease (DED).