An Expert Report on Parecoxib (DB08439): Pharmacology, Clinical Efficacy, and Regulatory Context

Executive Summary

Parecoxib is a parenterally administered, selective cyclooxygenase-2 (COX-2) inhibitor, classified as a non-steroidal anti-inflammatory drug (NSAID). It functions as a water-soluble prodrug, which is rapidly and completely hydrolyzed in vivo to its pharmacologically active metabolite, valdecoxib.[1] Developed to provide potent analgesia in the perioperative setting where oral administration is not feasible, parecoxib is the first and only injectable coxib available for clinical use.[1] Its primary indication is the short-term management of postoperative pain in adults.[4]

The clinical profile of parecoxib is defined by a rapid onset of analgesia, typically within 7-13 minutes, and a sustained effect that supports a 6- to 12-hour dosing interval, making it a valuable component of multimodal analgesic strategies.[1] Its mechanism of action, through the selective inhibition of the COX-2 enzyme by valdecoxib, effectively reduces the synthesis of pro-inflammatory prostaglandins, thereby alleviating pain and inflammation.[2] This selectivity confers a significant safety advantage over traditional, non-selective NSAIDs by sparing the COX-1 enzyme, which is crucial for maintaining gastric mucosal integrity and platelet function. Consequently, parecoxib is associated with a lower risk of gastrointestinal ulceration and does not interfere with platelet aggregation, a critical consideration in the surgical setting.[8]