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Chemical Compound Review

Licofelone     2-[2-(4-chlorophenyl)-6,6- dimethyl-1...

Synonyms: CHEMBL300982, SureCN237833, AG-E-05826, CHEBI:47532, ML-3000, ...
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Disease relevance of Licofelone


High impact information on Licofelone

  • Coincubation of licofelone with TGFbeta1 plus 1,25(OH)(2)D(3) did not affect FLAP or 5-LOX levels [6].
  • In the presence of TGFbeta1 plus 1,25(OH)(2)D(3), naproxen, but not licofelone, induced MMP-1 production and both drugs decreased nitric oxide levels [6].
  • Conversely, treatment with licofelone showed no effect on 5-LOX but significantly reduced FLAP expression levels [6].
  • OBJECTIVE: To compare the effect of licofelone, NS-398 (an inhibitor of cyclooxygenase 2 [COX-2]), and BayX-1005 (an inhibitor of 5-lipoxygenase activating protein) on the production of leukotriene B(4) (LTB(4)) and prostaglandin E(2) (PGE(2)), and on cell biomarkers by human osteoarthritis (OA) subchondral osteoblasts [7].
  • Because LTB(4) can modify cell biomarkers in OA and normal osteoblasts, our results suggest licofelone could modify abnormal bone remodeling in OA [7].

Chemical compound and disease context of Licofelone

  • Preliminary results of clinical studies of licofelone in osteoarthritis indicate that the drug has a comparable or slightly better efficacy than that of naproxen but possesses a much better gastrointestinal safety [8].
  • Zileuton (25-100 mg/kg, po), a 5-LOX inhibitor, indomethacin (1-30 mg/kg, po), a non-selective COX inhibitor, and licofelone (10-100 mg/kg, po) a dual inhibitor, significantly reversed the mechanical hyperalgesia and also caused an increase in cold allodynia threshold with different pharmacologic profile [9].

Biological context of Licofelone


Anatomical context of Licofelone


Associations of Licofelone with other chemical compounds


Gene context of Licofelone

  • Licofelone is a competitive inhibitor of 5-LOX, COX-1 and COX-2 that is currently being developed for the treatment of osteoarthritis [2].
  • Novel agents include the COX-inhibiting nitric oxide donors and the lipoxygenase (LOX)/COX inhibitor licofelone [19].
  • Moreover, licofelone treatment (30 microM) attenuated expression of VCAM-1 and ICAM-1 on inflammatory EC [4].
  • The regulation of human MMP-13 by licofelone, an inhibitor of cyclo-oxygenases and 5-lipoxygenase, in human osteoarthritic chondrocytes is mediated by the inhibition of the p38 MAP kinase signalling pathway [15].
  • The aim of the present study was to investigate if there is a contribution of mechanisms other than the reduction of inflammatory prostaglandins and leukotrienes to the anti-inflammatory effect of the LOX/COX inhibitor licofelone [4].

Analytical, diagnostic and therapeutic context of Licofelone


  1. In vivo dual inhibition of cyclooxygenase and lipoxygenase by ML-3000 reduces the progression of experimental osteoarthritis: suppression of collagenase 1 and interleukin-1beta synthesis. Jovanovic, D.V., Fernandes, J.C., Martel-Pelletier, J., Jolicoeur, F.C., Reboul, P., Laufer, S., Tries, S., Pelletier, J.P. Arthritis Rheum. (2001) [Pubmed]
  2. Safety of anti-inflammatory treatment--new ways of thinking. Brune, K. Rheumatology (Oxford, England) (2004) [Pubmed]
  3. Licofelone--clinical update on a novel LOX/COX inhibitor for the treatment of osteoarthritis. Alvaro-Gracia, J.M. Rheumatology (Oxford, England) (2004) [Pubmed]
  4. Licofelone, a novel 5-LOX/COX-inhibitor, attenuates leukocyte rolling and adhesion on endothelium under flow. Ulbrich, H., Soehnlein, O., Xie, X., Eriksson, E.E., Lindbom, L., Albrecht, W., Laufer, S., Dannhardt, G. Biochem. Pharmacol. (2005) [Pubmed]
  5. Licofelone, a balanced inhibitor of cyclooxygenase and 5-lipoxygenase, reduces inflammation in a rabbit model of atherosclerosis. Vidal, C., G??mez-Hern??ndez, A., S??nchez-Gal??n, E., Gonz??lez, A., Ortega, L., G??mez-Gerique, J.A., Tu????n, J., Egido, J. J. Pharmacol. Exp. Ther. (2007) [Pubmed]
  6. Regulation of the expression of 5-lipoxygenase-activating protein/5-lipoxygenase and the synthesis of leukotriene B(4) in osteoarthritic chondrocytes: role of transforming growth factor beta and eicosanoids. Martel-Pelletier, J., Mineau, F., Fahmi, H., Laufer, S., Reboul, P., Boileau, C., Lavigne, M., Pelletier, J.P. Arthritis Rheum. (2004) [Pubmed]
  7. Study of the role of leukotriene B()4 in abnormal function of human subchondral osteoarthritis osteoblasts: effects of cyclooxygenase and/or 5-lipoxygenase inhibition. Paredes, Y., Massicotte, F., Pelletier, J.P., Martel-Pelletier, J., Laufer, S., Lajeunesse, D. Arthritis Rheum. (2002) [Pubmed]
  8. The metabolic effects of inhibitors of 5-lipoxygenase and of cyclooxygenase 1 and 2 are an advancement in the efficacy and safety of anti-inflammatory therapy. Celotti, F., Durand, T. Prostaglandins Other Lipid Mediat. (2003) [Pubmed]
  9. Effect of licofelone against mechanical hyperalgesia and cold allodynia in the rat model of incisional pain. Singh, V.P., Patil, C.S., Kulkarni, S.K. Pharmacological reports : PR. (2005) [Pubmed]
  10. Licofelone (ML-3000), a dual inhibitor of 5-lipoxygenase and cyclooxygenase, reduces the level of cartilage chondrocyte death in vivo in experimental dog osteoarthritis: inhibition of pro-apoptotic factors. Boileau, C., Martel-Pelletier, J., Jouzeau, J.Y., Netter, P., Moldovan, F., Laufer, S., Tries, S., Pelletier, J.P. J. Rheumatol. (2002) [Pubmed]
  11. Licofelone, an inhibitor of cyclooxygenase and 5-lipoxygenase, specifically inhibits cyclooxygenase-1-dependent platelet activation. Rotondo, S., Krauze-Brzósko, K., Manarini, S., Evangelista, V., Cerletti, C. Eur. J. Pharmacol. (2004) [Pubmed]
  12. Effects on primary haemostasis of an anti-inflammatory agent with 5-lipoxygenase and cyclooxygenase inhibitory activity. Hernandez, M.R., Tonda, R., Pedre??o, J., Salas, E., Arderiu, G., Pino, M., Serradell, M., Escolar, G. Journal of cardiovascular medicine (Hagerstown, Md.) (2006) [Pubmed]
  13. General pharmacology of [2,2-dimethyl-6-(4-chlorophenyl)-7-phenyl-2,3- dihydro-1H-pyrrolizine-5-yl]-acetic acid in experimental animals. Algate, D.R., Augustin, J., Atterson, P.R., Beard, D.J., Jobling, C.M., Laufer, S., Munt, P.L., Tries, S. Arzneimittel-Forschung. (1995) [Pubmed]
  14. Inhibition of gastric H,K-ATPase activity and gastric epithelial cell IL-8 secretion by the pyrrolizine derivative ML 3000. Smolka, A.J., Goldenring, J.R., Gupta, S., Hammond, C.E. BMC gastroenterology [electronic resource]. (2004) [Pubmed]
  15. The regulation of human MMP-13 by licofelone, an inhibitor of cyclo-oxygenases and 5-lipoxygenase, in human osteoarthritic chondrocytes is mediated by the inhibition of the p38 MAP kinase signalling pathway. Boileau, C., Pelletier, J.P., Tardif, G., Fahmi, H., Laufer, S., Lavigne, M., Martel-Pelletier, J. Ann. Rheum. Dis. (2005) [Pubmed]
  16. The gastrointestinal tolerability of the LOX/COX inhibitor, licofelone, is similar to placebo and superior to naproxen therapy in healthy volunteers: results from a randomized, controlled trial. Bias, P., Buchner, A., Klesser, B., Laufer, S. Am. J. Gastroenterol. (2004) [Pubmed]
  17. Licofelone, a dual lipoxygenase-cyclooxygenase inhibitor, downregulates polymorphonuclear leukocyte and platelet function. Rotondo, S., Dell'Elba, G., Krauze-Brzósko, K., Manarini, S., Martelli, N., Pecce, R., Evangelista, V., Cerletti, C. Eur. J. Pharmacol. (2002) [Pubmed]
  18. Gastrointestinal tolerance of [2,2-dimethyl-6-(4-chlorophenyl-7-phenyl- 2,3-dihydro-1H-pyrrolizine-5-yl]-acetic acid in the rat. Laufer, S., Tries, S., Augustin, J., Elsässer, R., Algate, D.R., Atterson, P.R., Munt, P.L. Arzneimittel-Forschung. (1994) [Pubmed]
  19. Osteoarthritis therapy--are there still unmet needs? Laufer, S. Rheumatology (Oxford, England) (2004) [Pubmed]
  20. Treatment with licofelone prevents abnormal subchondral bone cell metabolism in experimental dog osteoarthritis. Lajeunesse, D., Martel-Pelletier, J., Fernandes, J.C., Laufer, S., Pelletier, J.P. Ann. Rheum. Dis. (2004) [Pubmed]
  21. The lipoxygenase-cyclooxygenase inhibitor licofelone prevents thromboxane A2-mediated cardiovascular derangement triggered by the inflammatory peptide fMLP in the rabbit. Rotondo, S., Dell'elba, G., Manarini, S., Cerletti, C., Evangelista, V. Eur. J. Pharmacol. (2006) [Pubmed]
  22. COX-LOX inhibition: current evidence for an emerging new therapy. Skelly, M.M., Hawkey, C.J. International journal of clinical practice. (2003) [Pubmed]
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