Pelubiprofen: A Comprehensive Pharmacological and Clinical Monograph

1.0 Executive Summary

Pelubiprofen is a nonsteroidal anti-inflammatory drug (NSAID) of the propionic acid class, structurally analogous to ibuprofen, developed by the South Korean firm Daewon Pharmaceutical.[1] It is characterized by a dual mechanism of action that distinguishes it from many other agents in its class. The primary mechanism involves the inhibition of cyclooxygenase (COX) enzymes, with a moderate preference for the inducible COX-2 isoform over the constitutive COX-1 isoform.[3] This is complemented by a distinct secondary mechanism: the suppression of the pro-inflammatory TAK1-IKK-NF-κB signaling pathway, which downregulates the expression of multiple inflammatory genes, including COX-2 itself.[3]

Clinically, Pelubiprofen is approved for the symptomatic relief of osteoarthritis, rheumatoid arthritis, and low back pain in several countries, including South Korea and Russia.[1] It has also been investigated in Phase III clinical trials for additional indications such as the management of fever associated with acute upper respiratory tract infections (URTIs) and post-traumatic pain.[6] Pivotal clinical trials have established its efficacy as non-inferior to active comparators, including the highly selective COX-2 inhibitor celecoxib for rheumatoid arthritis, the moderately selective NSAID aceclofenac for osteoarthritis, and loxoprofen for fever.[4]