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THR-687 is a potent, small molecule pan-RGD integrin antagonist developed for the treatment of retinal vascular disorders, particularly diabetic macular edema (DME) and diabetic retinopathy. It acts by inhibiting integrins that mediate processes such as vascular leakage, inflammation, gliosis, angiogenesis, and fibrosis in the retina. Preclinical studies demonstrated its ability to prevent retinal vascular permeability and reduce inflammation more broadly than current VEGF inhibitors. Clinical trials showed that intravitreal administration of THR-687 was safe and well tolerated with preliminary efficacy signals; however, later-stage trials failed to demonstrate sufficient efficacy on key endpoints (visual acuity and central subfield thickness), leading to discontinuation of its development for DME[1][3][4][5][8][9][10].
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