LEUVEN, Belgium—ThromboGenics NV, a biotechnology company developing novel medicines for diabetic eye disease, recently announced that positive preclinical data on plasma kallikrein (PKal) inhibitors in diabetic macular edema (DME) have been published in The Journal of Medicinal Chemistry under the title “Stable and Long-Lasting, Novel Bicyclic Peptide Plasma Kallikrein Inhibitors for the Treatment of Diabetic Macular Edema.”
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), reportedly support 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 exhibited prolonged retention in the eye, together with in-vivo efficacy in diabetic models of retinal vascular permeability.
“We are pleased that our cutting-edge research has been published in the prestigious Journal of Medicinal Chemistry,” said Dr. Jean Feyen, chief scientific officer of ThromboGenics. “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.”
According to ThromboGenics, the company is on track to start a Phase 1 study evaluating THR-149 for DME in the first half of 2018.
ThromboGenics is a biopharmaceutical company focused on developing innovative treatments for eye disease, with a focus on diabetic eye disease. In addition to THR-149, the company is developing THR-317, a PLGF inhibitor, for the treatment of diabetic macular edema—with plans to initiate a Phase 2 clinical study in the second quarter of this year—and THR-687, an integrin antagonist that is expected to enter the clinic around mid-2018. In addition, ThromboGenics owns the global rights to Jetrea (ocriplasmin), the only pharmacological vitreolysis drug approved for the treatment of symptomatic vitreomacular adhesion (in the United States) and vitreomacular traction (in Europe and elsewhere).