Catalog number: 251300-32-0
Category: Main Product
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RARECHEM AL BE 1424; 3-(trifluoromethyl)-2-hydroxybenzoic acid; Trifluoromehtylsalicylicacid
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1.Effect of food on the pharmacokinetics of triflusal and its major active metabolite, 2-hydroxy-4-trifluoromethyl benzoic acid, in healthy subjects.
Ge J, Ding LK, Yang J, Jia YY, Lu CT, Ding Y, Song Y, Song W, Wen AD. Int J Clin Pharmacol Ther. 2015 Mar;53(3):272-6. doi: 10.5414/CP202229.
OBJECTIVE: The objective of this study was to evaluate the pharmacokinetic parameters of triflusal and its major active metabolite, 2-hydroxy-4-trifluoromethyl benzoic acid (HTB), following a single oral dose of 900 mg in healthy subjects under fed and fasting conditions.
2.A phase I study to characterize the multiple-dose pharmacokinetics, pharmacodynamics and safety of new enteric-coated triflusal formulations in healthy male volunteers.
Lee HW1, Lim MS, Seong SJ, Lee J, Park J, Seo JJ, Yun HY, Baek IH, Kwon KI, Yoon YR. Expert Opin Drug Metab Toxicol. 2011 Dec;7(12):1471-9. doi: 10.1517/17425255.2011.630661.
OBJECTIVES: An enteric-coated formulation of triflusal (triflusal EC), an antiplatelet agent, was developed to reduce the high incidence of gastrointestinal adverse events (AEs). The aim of this study is to compare the pharmacokinetics, pharmacodynamics and safety of triflusal EC with triflusal in healthy Korean male subjects to determine bioequivalence and non-inferiority for the purposes of marketing approval.
3.A randomized, double-blind, placebo controlled-trial of triflusal in mild cognitive impairment: the TRIMCI study.
Gómez-Isla T1, Blesa R, Boada M, Clarimón J, Del Ser T, Domenech G, Ferro JM, Gómez-Ansón B, Manubens JM, Martínez-Lage JM, Muñoz D, Peña-Casanova J, Torres F; TRIMCI Study Group. Alzheimer Dis Assoc Disord. 2008 Jan-Mar;22(1):21-9. doi: 10.1097/WAD.0b013e3181611024.
BACKGROUND: Amnestic mild cognitive impairment represents, in many cases, the earliest clinical phases of Alzheimer disease. Anti-inflammatory agents have epidemiologic support as drugs potentially beneficial in Alzheimer disease. In vivo studies have shown that Triflusal and its active metabolite 2-hydroxy-4-trifluoromethyl-benzoic acid have potent anti-inflammatory actions in the central nervous system.
4.Inhibition of cyclooxygenase-2 expression by 4-trifluoromethyl derivatives of salicylate, triflusal, and its deacetylated metabolite, 2-hydroxy-4-trifluoromethylbenzoic acid.
Fernández de Arriba A1, Cavalcanti F, Miralles A, Bayón Y, Alonso A, Merlos M, García-Rafanell J, Forn J. Mol Pharmacol. 1999 Apr;55(4):753-60.
The therapeutic potential of drugs that block the induction of cyclooxygenase-2 has been emphasized. When two 4-trifluoromethyl salicylate derivatives [2-acetoxy-4-trifluoromethyl-benzoic acid (triflusal) and its deacetylated metabolite 2-hydroxy-4-trifluoromethylbenzoic acid (HTB)] were compared with aspirin and sodium salicylate as cyclooxygenase-2 (COX-2) inhibitors, we observed that in bacterial lipopolysaccharide-activated human blood, triflusal, aspirin, and HTB, but not sodium salicylate, inhibited COX-2-mediated prostaglandin E2 (PGE2) production (IC50 = 0.16, 0.18, 0.39, and >10 mM, respectively). However, only triflusal and aspirin inhibited purified COX-2 enzyme. To test this apparent discrepancy, we realized that HTB and triflusal (but neither aspirin nor salicylate) produced a concentration-dependent inhibition of COX-2 protein expression in peripheral human mononuclear cells. This observation was further confirmed in a rat air pouch model in vivo, in which both aspirin and triflusal inhibited PGE2 production (ID50 = 18.
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