Licofelone

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Licofelone
Licofelone structure.svg
Legal status
Legal status
  • Investigational
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
ECHA InfoCard 100.222.821 Edit this at Wikidata
Chemical and physical data
Formula C23H22ClNO2
Molar mass 379.88 g·mol−1
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Licofelone is a dual COX/LOX inhibitor[1][2] that was studied in clinical trials as a treatment for osteoarthritis[3] and which was 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.

Phase III trials for osteoarthritis were conducted in the early 2000s,[4][5] but results were mixed and the drug has never been submitted for regulatory approval.

References[edit]

  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. ^ "Licofelone – Novel Analgesic and Anti-Inflammatory Agent for Osteoarthritis". Retrieved January 12, 2018. 
  5. ^ Wildi, L. M; Raynauld, J.-P; Martel-Pelletier, J; Abram, F; Dorais, M; Pelletier, J.-P (2010). "Relationship between bone marrow lesions, cartilage loss and pain in knee osteoarthritis: Results from a randomised controlled clinical trial using MRI". Annals of the Rheumatic Diseases. 69 (12): 2118. doi:10.1136/ard.2009.127993. PMID 20610445.