tarenflurbil
Sign in to saveAlso known as MPC-7869, (-)-(2R)-2-(2-fluorobiphenyl-4-yl)propanoic acid, Flurizan, (R)-2-fluoro-alpha-methyl(1,1'-biphenyl)-4-acetic acid, (2R)-2-(2-fluorobiphenyl-4-yl)propanoic acid, (−)-(2R)-2-(2-fluorobiphenyl-4-yl)propanoic acid, (R)-2-fluoro-α-methyl(1,1'-biphenyl)-4-acetic acid
Tarenflurbil, Flurizan or '''R-flurbiprofen''', is a single enantiomer of the racemate NSAID flurbiprofen. For several years, research and trials for the drug were conducted by Myriad Genetics, to investigate its potential as a treatment for Alzheimer's disease; that investigation concluded in June 2008 when the company announced it would discontinue development of the compound.
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Encyclopedic overview
4 sectionsContents
- Mechanism of action
- Clinical trials
- References
- External links
Tarenflurbil, Flurizan or '''R-flurbiprofen''', is a single enantiomer of the racemate NSAID flurbiprofen. For several years, research and trials for the drug were conducted by Myriad Genetics, to investigate its potential as a treatment for Alzheimer's disease; that investigation concluded in June 2008 when the company announced it would discontinue development of the compound.
==Mechanism of action== At proposed therapeutic concentrations, this molecule lacks anti-inflammatory activity, and does not inhibit either cyclooxygenase 1 (COX-1) or cyclooxygenase 2 (COX-2) enzymes. Only the S-enantiomers of arylpropionic acid NSAID can potently inhibit COX, whereas the R-enantiomers exert almost no COX activity. R-Flurbiprofen is inefficiently converted into S-flurbiprofen, with 1.5% of the R-enantiomer undergoing bioinversion to the S-form. Although this compound lacks activity against COX, studies have shown that this drug is a potent reducer of levels of beta amyloid, the main constituent of amyloid plaques in Alzheimer's disease, and therefore there was interest in this drug as a therapeutic agent.
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