EPOR Agonist Program

Anemia

EPOR Agonist Program

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., Aranesp®, Epogen®, Eprex®, and Procrit®).

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.
epor
Richmond TD, Chohan M, Barber DL. 2005 Trends Cell Biol 15:146-155

We have developed 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.