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Tarenflurbil
Tarenflurbil,〔(www.myriad.com ) Update on Flurizan.〕 Flurizan or ''R''-flurbiprofen, is the 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.〔(Myriad Genetics Reports Results of U.S. Phase 3 Trial of Flurizan in Alzheimer's Disease ) from the Myriad Genetics website.〕 ==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.
抄文引用元・出典: フリー百科事典『 ウィキペディア(Wikipedia)』 ■ウィキペディアで「Tarenflurbil」の詳細全文を読む
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