About Optina for the Oral Treatment of Diabetic Macular Edema
Optina is a novel, ultra-low dose of danazol being developed for the oral treatment of diabetic macular edema.
Danazol is an established, synthetic derivative of modified testosterone ethisterone that affects vascular endothelial cell linkage in a biphasic manner. Ultra-low dose danazol (as formulated in Optina) decreases vascular permeability by increasing the barrier function across endothelial cells, indicating the potential to treat multiple angiopathies. Further, danazol increases intracellular cyclic adenosine monophosphate (cAMP) levels through the rapid activation of membrane-associated androgen, steroid binding globulin, and calcium channel receptors. With the ultra-low dose contained in our novel Optina formulation, danazol binds to androgen and steroid binding globulin receptors stimulating the formation of a cortical actin ring to enhance endothelial cell barrier function. When organized into a cortical ring, filamentous actin (f-actin) increases the barrier function of endothelial cells by tethering adhesion molecule complexes to the cytoskeleton. In this orientation, increased cortical actin improves tight junctions which strengthen cell-to-cell adhesions, thereby restricting leakage (edema) across the cell membrane. A large, late-stage clinical trial is identified to start in the US for the oral treatment of diabetic macular edema. Additional future indications for Optina are being researched. One hundred thirty four patents are currently issued for Optina with 50 pending applications worldwide.