The Complement System – Aiming to Control Overactivation

For many years, scientific data have supported the role of the complement system in inflammatory diseases, such as rheumatoid arthritis and asthma. Upon activation of the complement system, the extremely potent pro-inflammatory complement component C5a is generated. Until now, no small molecule therapeutic agent with the ability to control the negative effects associated with the excessive activation of the complement system has been available. Jerini has developed both a peptidomimetic and a small organic molecule C5a receptor antagonist. These compounds have shown positive preclinical results and therapeutic potential in several indications, including age-related macular degeneration, the leading cause of blindness in the elderly, ischemia reperfusion injury, transplant rejection and kidney fibrosis.

Publications:

Boor P., Konieczny A., Villa L., Schult A.L., Bucher E., Rong S., Kunter U., van Roeyen C.R., Polakowski T., Hawlisch H., Hillebrandt S., Lammert F., Eitner F., Floege J., Ostendorf T. Complement C5 Mediates Experimental Tubulointerstitial Fibrosis, J Am Soc Nephrol. 2007 May;18(5):1508-15

K. Schnatbaum, E. Locardi, D. Scharn, U. Richter, H. Hawlisch, J. Knolle, T. Polakowski. Peptidomimetic C5a receptor antagonists with hydrophobic substitutions at the C-terminus: increased receptor specificity and in vivo activity, Bioorg. Med. Chem. Lett. 2006, 16, 5088–5092

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