Licofelone

Cross-talk between lipoxygenase (LO) and cyclooxygenase (COX) pathways has been observed in human osteoarthritic synovial explants which creates an arachidonic acid shunting phenomenon, stimulating interleukin-1β (IL-1β) synthesis. Licofelone is a dual inhibitor of cyclooxygenase (COX) and lipoxygenase (LO) pathways, that decreases levels of prostaglandin E₂, leukotriene B₄, and lipoxins and prevents lipopolysaccharide-stimulated IL-1β expression.¹ The IC₅₀ values for inhibition of human thrombocyte COX and human 5-LO are 0.16 µM and 0.23 µM, respectively.² Unlike other non-steroidal anti-inflammatory drugs, licofelone causes little or no damage to the gastric mucosa in rabbit parietal cells. This is presumably the result of licofelone’s affects on acid-secretory mechanisms, mediated by the inhibition of 5-LO activity.³

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1. Marcouiller, P., Pelletier, J.P., Guévremont, M., et al. Leukotriene and prostaglandin synthesis pathways in osteoarthritic synovial membranes: Regulating factors for interleukin 1β synthesis. J. Rheumatol. 32(4), 704-712 (2005).

2. Laufer, S.A., Augustin, J., Dannhardt, G., et al. (6,7-Diaryldihydropyrrolizin-5-yl)acetic acids, a novel class of potent dual inhibitors of both cyclooxygenase and 5-lipoxygenase. J. Med. Chem. 37, 1894-1897 (1994).

3. Smolka, A.J., Goldenring, J.R., Gupta, S., et al. Inhibition of gastric H,K^-ATPase activity and gastric epithelial cell IL-8 secretion by the pyrrolizine derivative ML 3000. BMC Gastroenterol. 4(4), (2004).