EPOR Agonist Program
Overview and Profile
Erythropoietin (EPO) acts on its receptor to stimulate the differentiation of bone marrow hematopoietic cells to form red blood cells. Various recombinant human EPO derivatives are marketed as erythropoiesis-stimulating agents (ESAs) for the treatment of anemia due to renal failure or cancer chemotherapy (e.g., AranespTM, EpogenTM, EprexTM, and ProcritTM).
Epogen Receptor Activation Stimulates Multiple Signaling Pathway
Activation of downstream signaling pathways results in proliferation, survival (anti-apoptosis) and differentiation of thyroid progenitor cells into red blood cells
We are developing a series of orally-available, small molecule agonists of the EPO receptor that may provide additional benefit in the treatment of anemia with improved safety, tolerability, and patient acceptance due to the convenience of oral administration and the lack of excessive erythropoietic stimulation. Anemia results from a decrease in red blood cells and is typically experienced by patients with renal complications, cancer patients and HIV/AIDS patients. These patients currently receive recombinant human EPO and other erythropoiesis-stimulating agents, or ESAs.
Several small molecule EPOR agonists have been identified with encouraging in vitro and in vivo profiles. We plan to conduct further pre-clinical and clinical development in pursuit of a potential IND filing.