Date: 2018-04-06
Type of
information: Publication of results in a medical journal
phase: preclinical
Announcement: publication of results in The Journal of Medicinal Chemistry
Company: Thrombogenics (Belgium)
Product: THR-149
Action
mechanism:
- kallikrein inhibitor/peptide. THR-149 is a novel plasma kallikrein inhibitor. This bicyclic peptide (Bicycle®) has been identified as a lead candidate in the alliance between ThromboGenics and Bicycle Therapeutics. Bicycles are a novel class of small molecule medicines designed to overcome many of the limitations of existing drug modalities. They can be used as standalone therapeutic entities or coupled to deliver a variety of therapeutic payloads, and exhibit the affinity and exquisite target specificity usually associated with antibodies but in a small molecule format enabling rapid tissue penetration and flexible routes of administration.
Disease: diabetic macular edema
Therapeutic
area: Ophtalmological diseases
Country:
Trial
details:
Latest
news:
- • On April 6, 2018, ThromboGenics announced that positive preclinical data on plasma kallikrein (PKal) inhibitors in diabetic macular edema (DME) have been published in The Journal of Medicinal Chemistry ('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), 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.
- ThromboGenics is on track to start a Phase I study evaluating THR-149 for DME in H1 2018.
- • On April 20, 2017, ThromboGenics announced it has achieved an important milestone in the advancing of the pre-clinical development of its THR-149, a novel plasma kallikrein inhibitor, which the company is developing for the treatment of diabetic macular edema. Following this announcement, ThromboGenics will now start pivotal tox studies which are a last step before starting the clinical development which is expected for early 2018
Is
general: Yes
