Zedira’s drug discovery approach targets dysregulated transglutaminase activity in disease states.
In the human body, eight transglutaminase iso-enzymes (TG1-TG7 and coagulation factor XIII) fulfill a broad variety of physiological functions. However, transglutaminases are also involved in the pathophysiology of various disorders.
In celiac disease Zedira’s drug candidate ZED12271
, an irreversible direct-acting and specific inhibitor of human tissue transglutaminase (TG2), showed the proof of concept in a phase 2a study. The groundbreaking results have been published in the New England Journal of Medicine
. An overview is given in our press release
This proof of concept is of utmost importance not only for celiac disease, but beyond: for the first time a transglutaminase was validated as a druggable target. Moreover, our transglutaminase inhibitor ZED1227 was proven to be save and well tolerated.
This remarkable success has a favorable effect on several other transglutaminase related disorders. Especially fibrotic disorders affecting the lung, liver, or kidney may be addressed with our compounds. Our newest class of reversible direct-acting and specific inhibitors of tissue transglutaminase (TG2) are orally bioavailable proprietary compounds. An overview is given in our press release
Transglutaminase blocker drug candidates are also available to target coagulation factor XIII (F13, plasma transglutaminase). This novel and unique approach dissociates an antithrombotic effect from increased bleeding tendency in anticoagulation. Results obtained in an in vivo study of the direct-acting FXIIIa inhibitor ZED3197 have been published in the Journal of Thrombosis and Haemostasis
. For detailed information we refer to the respective open access scientific publication.
Zedira’s drug candidate ZED1227 targeting dysregulated TG2 in celiac disease
showed the proof of concept in a phase 2a clinical trial. read more
Latest Drug Discovery program targeting active TG2 in organs. read more
1 Gluten Sensitive Neurological Disorders
Auto-antibodies specific for neuronal transglutaminase (TG6) can be measured with our proprietary ELISA-kits. New:
Analytical service for measurement of TG6-autoantibodies in human serum samples. read more
Thrombosis / Anticoagulation
Proof-of-principle for safe anticoagulation,
meaning anticoagulation without increased bleeding risk using blood coagulation factor FXIIIa-blockers has recently been shown. read more
Büchold C, Hils M, Gerlach U, Weber J, Pelzer C, Heil A, Aeschlimann D, Pasternack R. Features of ZED1227: The First-In-Class Tissue Transglutaminase Inhibitor Undergoing Clinical Evaluation for the Treatment of Celiac Disease. Cells. 2022; 11(10):1667. https://doi.org/10.3390/cells11101667