Licofelone
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| Licofelone | ||
|---|---|---|
 | ||
| IUPAC name [6-(4-chlorophenyl)-2,2-dimethyl-7-phenyl-2,3-dihydro-1H-pyrrolizin-5-yl]acetic acid | ||
| Identifiers | ||
| CAS number | 156897-06-2  | |
| PubChem | 133021 | |
| ChEMBL | CHEMBL52854  | |
| Jmol-3D images | Image 1 | |
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| Properties | ||
| Molecular formula | C23H22ClNO2 | |
| Molar mass | 379.879 g·mol−1 | |
| (verify) (what is: /?) Except where noted otherwise, data are given for materials in their standard state (at 25 °C (77 °F), 100 kPa) | ||
| 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
- ↑ 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 2050828. PMID 17704828.
- ↑ 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.
- ↑ 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.
- ↑ http://www.drugdevelopment-technology.com/projects/licofelone/
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