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
3D model (JSmol)
ChemSpider
ECHA InfoCard 100.222.821
UNII
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).
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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-lipoxygenase (5-LOX) may reduce the gastrointestinal toxicity associated with other nonsteroidal anti-inflammatory drugs (NSAID), which only inhibit cyclooxygenase (COX). 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. PMC 2050828Freely accessible. PMID 17704828. doi:10.1038/sj.bjp.0707416.
  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. PMID 17015640. doi:10.1124/jpet.106.110361.
  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. PMID 14752172. doi:10.1093/rheumatology/keh105.
  4. http://www.drugdevelopment-technology.com/projects/licofelone/



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