Polmacoxib, also known as
(CG-100649), is a first-in-class NSAID which is a dual inhibitor
of COX-2 and carbonic anhydrase (CA). The drug, which
was approved in South Korea for the treatment of colorectal
cancer (CRC) in 2015 and whose discovery has been described
by workers at AmorePacific R&D, interacts with CA in red
blood cells, providing a novel “tissue-specific” transport
mechanism that is designed to deliver sustained levels of drug
to inflamed tissues while maintaining low systemic exposure.
Although the unique dual COX-2/CA inhibition is designed to
provide potentially superior safety to cardiovascular, renal, and
gastrointestinal tissues compared to traditional NSAIDs or
COX-2 inhibitor drugs, the long-term safety profile of the drug,
particularly cardiovascular risks notoriously associated with
inhibition of COX-2, has yet to be determined, and the drug
is currently not approved for use in any other country outside
of South Korea.
