Research & Development

Diabetic Retinopathy (DR) 
DR is a most common cause of vision loss among diabetic patients. Non-proliferative diabetic retinopathy (NPDR) is the early stage of DR during which patients exhibit no obvious symptoms to mild symptoms such as weakened blood vessels. Chronically elevated blood glucose in diabetes can render tiny blood vessels in the eye "leaky", causing fluid to build up in light-sensing tissue called the retina. This phenomenon, known as edema, can greatly affect the central vision when occurs at the region of the retina known as the macula, which is responsible for sharp, color vision. In fact, Diabetic Macular Edema (DME) is the most common cause of vision loss in DR population. More advanced stage of DR, known as proliferative diabetic retinopathy (PDR), is characterized by abnormal blood vessel growth (i.e. neovascularization). Abnormal vessel function and growth may contribute to retinal inflammation, ischemia (i.e. inadequate blood flow), and neuronal cell death, all of which can ultimately lead to substantial vision loss or complete blindness. 
Although few treatment options exist for DR, current standard of care suffers from critical challenges: 1) anti-VEGF therapy (the golden standard) has limited patient coverage (<40%); 2) current anti-VEGF treatments are cost-prohibitive for many patients (~$1000/shot) and require repetitive (e.g., monthly) intravitreal injections; 3) secondary approaches like laser photocoagulation create irreversible damage to the retina; and 4) complementary corticosteroid therapy can trigger local/systemic side effects. Hence, we believe finding a new therapeutic target and new therapeutic agents are critical to improving current standard of care for DR. 
 
Our approach to DR
Growing body of evidence point out that pharmacological activation of Peroxisome Proliferator-Activated Receptor-α (PPAR-α) with fibrate drugs ameliorate symptoms of DR in both pre-clinical and clinical studies. We are developing structurally unique, non-fibrate small-molecule drugs with improved potency, target specificity, efficacy and safety. By optimizing our drug designs for non-invasive systemic delivery, our approach will offer diabetic patients a revolutionary therapeutic modality. 
Research & Development 
Empowered by the academic collaboration with University of Oklahoma, Excitant is fully capable of novel drug discovery.
Medicinal Chemistry

We integrate computational methods, chemical and structural biology, and synthetic/medicinal chemistry, to develop SAR-driven therapeutic leads for various ophthalmic diseases. We employ custom designed assays, as well as commercial kits, to analyze and validate chemical hits. 

Bioactivity assays

We perform in vitro assays to evaluate bioactivity of therapeutic leads by examining target gene expression at both the transcriptional and translational levels . In addition, we employ various cell-based assay models that mimic pathogenic conditions observed in ocular diseases.

In vivo efficacy studies

Our animal models for ophthalmic research include: Streptozotocin-induced diabetic rats (STZ), Vldlr KO mice, Laser-induced Choroidal Neovascularization model (CNV), Light-induced retinal damage (LIRD) model, and Oxygen-induced retinopathy model (OIR). 

© 2018 by Excitant Therapeutics, LLC. All rights reserved. 

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