Licofelone

Licofelone
Ball-and-stick model of the licofelone molecule
Names
IUPAC name
[6-(4-chlorophenyl)-2,2-dimethyl-7-phenyl-2,3-dihydro-1H-pyrrolizin-5-yl]acetic acid
Identifiers
156897-06-2 YesY
3D model (Jmol) Interactive image
ChEMBL ChEMBL52854 N
ChemSpider 117391 N
ECHA InfoCard 100.222.821
PubChem 133021
UNII P5T6BYS22Y N
Properties
C23H22ClNO2
Molar mass 379.879 g·mol−1
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
N verify (what is YesYN ?)
Infobox references

Licofelone is a dual COX/LOX inhibitor[1][2] being considered as a treatment for osteoarthritis[3] and which is under development by Merckle GmbH with partners Alfa Wassermann and Lacer.

Licofelone is both an analgesic and an anti-inflammatory. Inhibition of 5-LOX may reduce the gastrointestinal toxicity associated with other non-steroidal anti-inflammatory drugs, which only inhibit COX (cyclooxygenase). Licofelone is the first drug to inhibit both. It has passed the phase III trials.[4]

References

  1. Fischer L, Hornig M, Pergola C, et al. (October 2007). "The molecular mechanism of the inhibition by licofelone of the biosynthesis of 5-lipoxygenase products". British Journal of Pharmacology. 152 (4): 471–80. doi:10.1038/sj.bjp.0707416. PMC 2050828Freely accessible. PMID 17704828.
  2. Vidal C, Gómez-Hernández A, Sánchez-Galán E, et al. (January 2007). "Licofelone, a balanced inhibitor of cyclooxygenase and 5-lipoxygenase, reduces inflammation in a rabbit model of atherosclerosis". The Journal of Pharmacology and Experimental Therapeutics. 320 (1): 108–16. doi:10.1124/jpet.106.110361. PMID 17015640.
  3. Alvaro-Gracia JM (February 2004). "Licofelone--clinical update on a novel LOX/COX inhibitor for the treatment of osteoarthritis". Rheumatology (Oxford, England). 43 Suppl 1 (90001): i21–5. doi:10.1093/rheumatology/keh105. PMID 14752172.
  4. http://www.drugdevelopment-technology.com/projects/licofelone/



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