Verseon’s oral plasma kallikrein inhibitors successfully reduce retinal thickness and retinal leakage, two hallmarks of the disease
Verseon presented new efficacy results on its diabetic macular edema drug candidates at the Association for Research in Vision and Ophthalmology (ARVO) 2018 annual meeting in Honolulu this week. The preclinical data show that Verseon’s oral plasma kallikrein inhibitors successfully reduce retinal thickness and retinal leakage, two hallmarks of the disease.
Diabetic macular edema (DME) is a leading cause of blindness in today’s growing diabetic population. In diabetics, chronically high blood sugar can weaken blood vessels in the eye and cause fluids to leak. Fluid accumulating in the macula (the central region of the retina responsible for keenest vision) can result in swelling, blurred vision, and eventually central vision loss. The current standard of care for DME includes regular injections into the eye of repurposed anticancer agents or corticosteroids, treatments associated with side effects such as inflammation and infection.
At ARVO, Verseon’s Dr Melissa Calton presented comprehensive preclinical data for one of Verseon’s new, potent and selective small-molecule plasma kallikrein inhibitors, VE-3539. In contrast to current DME drugs, Verseon’s compound shows pharmacokinetics suitable for oral administration. Results from a well-established efficacy model, the retinal vascular permeability model, show that VE-3539 successfully reduces retinal leakage and restores mean circulation times. “VE-3539 is the first orally dosed plasma kallikrein inhibitor to demonstrate efficacy in this preclinical model of DME,” said Dr Calton. Additionally, Verseon’s candidate is efficacious in another widely used model of DME, the human plasma kallikrein injection model, that mimics the retinal thickening observed in patients.
“Verseon’s DME drugs could offer a safe and convenient alternative to intravitreal injections,” said Dr Calton. “With their oral route of administration, our drug candidates are especially well-suited for prophylaxis, providing an important benefit for the growing number of diabetics who are at risk of losing their eye sight through DME.”
Verseon uses a computer-driven drug discovery platform embedded in a comprehensive chemistry and biology workflow to design new drug candidates for a wide range of diseases. In addition to the diabetic macular edema program, the company currently has drug programs in anticoagulation, hereditary angioedema, and oncology.