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SIROLIMUS INJECTION (DE-109) is an intravitreally administered immunoregulator being investigated for the treatment of non-infectious uveitis of the posterior segment, a progressive and chronic inflammatory disease of the eye. Sirolimus Injection regulates the immune system through the inhibition of mTOR which acts by 1) interrupting the inflammatory cascade that leads to T-cell activation, differentiation and proliferation, and production of interleukin-2 (IL-2), as well as other pro-inflammatory cytokines; and 2) promoting immune tolerance by inducing T regulatory cells (Tregs). Sirolimus Injection was granted orphan drug designation by the U.S. Food and Drug Administration (FDA) and the European Commission (EC) in 2011.

DE-117, a non-prostanoid selective EP2 receptor agonist, is currently being investigated in a topical ophthalmic solution for the reduction of elevated IOP in patients with ocular hypertension or open-angle glaucoma. DE-117 is thought to mediate IOP-lowering by relaxing the ciliary muscle and increasing outflow of aqueous humor through the uveoscleral pathway.

DE-120 is a small molecule dual inhibitor of vascular endothelial growth factor (VEGF) and Platelet-derived growth factor (PDGF) receptor tyrosine kinases which may be an important therapeutic advance for retinal diseases involving angiogenesis and vascular leakage such as exudative age-related macular degeneration (AMD) and diabetic macular edema (DME). The inhibition of VEGF by blocking the receptor or binding the VEGF protein to a soluble decoy receptor has been shown to be effective in the treatment of and AMD and DME. Numerous compounds which inhibit the activation of the receptor tyrosine kinase activity are under evaluation for the treatment of cancer and other diseases. PDGF is also important in the pathogenesis of AMD. Through binding of PDGF to its receptor and activation of its tyrosine kinase, new blood vessels in the eye are stabilized by attachment of pericytes.

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