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 E
2, leukotriene B
4, and lipoxins and prevents lipopolysaccharide-
stimulated IL-
1β expression.
1 The IC
50 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