The present disclosure relates to the discovery that certain diseases of the eye that profoundly affect the human visual system and, as a result, quality of life, may be treated using Edonentan or A-182086. Edonentan or A-182086 can be used alone or in combination with an intra-ocular pressure (IOP) reducing agent, a neuroprotective agent, an anti-VEGF agent, or all, for example. Using Edonentan or A-182086, alone or in combination with an additional agent, provides increased perfusion to the retina in certain diseases and reduces damage to retinal cells.The present disclosure relates to the discovery that certain ocular diseases may be treated using Edonentan crystalline forms. Specific Edonentan crystalline form can be used alone or in combination with an intra-ocular pressure (TOP) reducing agent, a neuroprotective agent, or an anti-VEGF agent. Using Edonentan crystalline forms, alone or in combination with an additional agent, provides increased perfusion to the retina or reduced IOP in certain ocular diseases and reduces damage to retinal cells.
Edonentan is a drug that belongs to the group of endothelin receptor antagonists. It has been shown to inhibit the activity of endothelin-A receptors and prevent binding to collagen, which in turn prevents the development of cardiac hypertrophy and heart failure. Edonentan also acts as an analog for sodium-dependent glucose co-transporters (SGLT1), inhibiting glucose reabsorption in the kidney, thereby lowering blood pressure. The effects of edonentan on amines are not yet known. Edonentan has been shown to be effective in treating symptoms of inflammatory bowel disease in CD-1 mice.
Edonentan, also known as BMS-207940, is a highly potent and orally active ET(A) selective antagonist. Edonentan is an extremely potent (ET(A) K(i) = 10 pM) and selective (80,000-fold for ET(A) vs ET(B)) antagonist. It is also 150-fold more potent and >6-fold more selective than BMS-193884. The bioavailability of Edonentan was 100% in rats and the systemic clearance and volume of distribution are higher than that of BMS-193884. In rats, intravenous Edonentan blocks big ET pressor responses with 30-fold greater potency than 1. After oral dosing at 3 micromol/kg, Edonentan displays enhanced duration relative to BMS-193884.
Edonentan monohydrate is a chemical compound that has gained significant attention in the scientific community due to its potential therapeutic and environmental applications. It is a small molecule inhibitor of the endothelin receptor, which plays a crucial role in regulating blood pressure and vascular tone.
The present disclosure relates to the discovery that certain diseases of the eye that profoundly affect the human visual system and, as a result, quality of life, may be treated using Edonentan or A-182086. Edonentan or A-182086 can be used alone or in combination with an intra-ocular pressure (TOP) reducing agent, a neuroprotective agent, an anti-VEGF agent, or all, for example. Using Edonentan or A-182086, alone or in combination with an additional agent, provides increased perfusion to the retina in certain diseases and reduces damage to retinal cells.