LeukoTriene Synthesis Inhibitor (LTSI) Program: 5-Lipoxygenase Inhibitors

The company’s first program is based on a biochemical target, 5-lipoxygenase (5-LO), which is involved in the conversion of arachidonic acid to the first leukotriene, LTA4. By blocking 5-LO in an inflammatory response, levels of leukotrienes are reduced such that their availability to drive the inflammatory cycle involved in disease is limited.

Peptidase Activator Leukotriene Inhibitor (PALI) Program: LTA4H product mediators

Naegis' second most advanced program is directed towards modulating inflammatory products and substrates associated with the LTA4H enzyme.  Recent understanding of the dual pro-inflammatory and anti-inflammatory role of LTA4 hydrolase has prompted efforts to discover novel selective inhibitors that block the production of LTB4 while maintaining or even promoting the ability of the enzyme to break down the pro-inflammatory molecule (Proline–Glycine-Proline) PGP (through its peptidase activity). This quest for selective inhibitors that have the unique potential to block inflammatory processes involved in disease while promoting intrinsic anti-inflammatory mechanisms has lead to the genesis of Naegis' PALI program.  In early testing Naegis has discovered molecules that block production of LTB4 in cells and promote peptidase activity of the LTA4H enzyme. Molecules within this program are currently being studied with the objective of optimizing a potential drug candidate for further development for COPD.