ThromboGenics nv (Euronext Brussels: THR), a biotechnology company developing novel medicines for diabetic eye disease, today announces that positive preclinical data on plasma kallikrein (PKal) inhibitors in diabetic macular edema (DME) have been published in The Journal of Medicinal Chemistry.
ThromboGenics has identified highly selective bicyclic peptide inhibitors of PKal, which were chemically modified to optimize for potency and stability. These novel PKal inhibitors were generated using Bicycle Therapeutics' Bicycles® technology platform. The positive outcomes of PKal inhibitors on tissue edema, studied in a paw swelling model and in a preclinical diabetic retinopathy (DR) disease model (streptozotocin-induced vascular leakage into the retina), supports their development as possible treatments for DME and DR via a VEGF-independent mechanism.
The preclinical study confirmed that the bicyclic peptides have nanomolar to picomolar potencies, are stable in biological matrices and reported prolonged retention in the eye together with in vivo efficacy in diabetic models of retinal vascular permeability.
The article 'Stable and Long-Lasting, Novel Bicyclic Peptide Plasma Kallikrein Inhibitors for the Treatment of Diabetic Macular Edema' can be consulted online here.
Jean Feyen, PhD, CSO of ThromboGenics nv comments: "We are pleased that our cutting-edge research has been published in the prestigious Journal of Medicinal Chemistry. These preclinical data further validate the science and potential of PKal inhibitor THR-149 in addressing edema as a key disease hallmark of DR, ahead of its planned entry into the clinic this year."
ThromboGenics is on track to start a Phase I study evaluating THR-149 for DME in H1 2018.
ThromboGenics is a biopharmaceutical company focused on developing innovative treatments for eye disease, with a focus on diabetic eye disease. The company's pipeline of disease modifying drug candidates is targeting the key segments of the diabetic eye disease market.
ThromboGenics' is developing THR-317, a PLGF inhibitor, for the treatment of diabetic macular edema and plans to initiate a Phase II clinical study by Q2 2018. ThromboGenics' late pre-clinical pipeline consists of THR-149, a plasma kallikrein inhibitor, and THR-687, an integrin antagonist. THR-149 is expected to enter the clinic in H1 2018 and THR-687 around mid-2018. Further new drug candidates are currently being progressed for the treatment of diabetic eye disease and one of these is expected to enter development in 2018.
ThromboGenics owns the global rights to JETREA® (ocriplasmin), the only pharmacological vitreolysis drug approved for the treatment of symptomatic vitreomacular adhesion (in the US) and vitreomacular traction (in Europe and elsewhere).
ThromboGenics is headquartered in Leuven, Belgium, and is listed on the NYSE Euronext Brussels exchange under the symbol THR. More information is available at www.thrombogenics.com