Characterization of Eltenac and novel COX-2 selective thiopheneacetic acid analogues in vitro and in vivo

In vitro and ex vivo pharmacodynamics of selected non-steroidal anti-inflammatory drugs in equine whole blood

“…This was demonstrated by the low concentration of drug necessary to inhibit COX-1 (0.10 µM) and the high percentage inhibition of COX-1 (>50%) when COX-2 was inhibited by >80%. Different results were reported in an in vitro human study (Klein et al, 2008), in which eltenac acted as an unselective COX-1 and COX-2 inhibitor (IC50 COX-1 = 0.03 µM; IC50 COX-2 = 0.03 µM). However, the preferential COX-2 inhibition of eltenac was lost in the ex vivo study, where the drug acted as a non-selective NSAID.…”

Lead Optimization on Conventional Non‐Steroidal Anti‐Inflammatory Drugs: An Approach to Reduce Gastrointestinal Toxicity

“…Klein et al . assessed the effect of novel selective thiopheneacetic acids (thiopheneacetic acid Eltenac and derivatives) on COX isoenzymes in vitro and in vivo . In human whole blood experiments, these derivatives were potent inhibitors of COX‐2 with less pronounced effect on COX‐1.…”