ASP-6537 (ASP6537) is a novel potent, selective, reversible cyclooxygenase-1 (COX-1) inhibitor with IC50 of 4.9 nM; displays 650-fold selectivity over COX-2 (IC50=3.2 uM); dose dependently inhibits carrageenan-induced paw edema (ED30=22 mg/kg) and paw swelling associated with adjuvant arthritis (ED50=17 mg/kg) in rats; also inhibits TXA2 production more selectively than aspirin in in vitro and in vivo, exerts potent antithrombotic effect in rats.
An enantiomer of Ibuprofen that more potently inhibits COX activity, thromboxane formation, and platelet aggregation than the (R)-form; also inhibits activation of NF-κB more effectively than (R)-ibuprofen (IC50=62 and 122 uM, respectively).
A non-steroidal anti-inflammatory drug (NSAID); primarily indicated as a pre-operative anti-miotic as well as orally for arthritis or dental pain; cyclooxygenase (COX) inhibitor.
Phase 2 Discontinued
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