flopropione

Flopropione is a phloroglucinol-derived small molecule traditionally used in Japan as an antispasmodic agent for the treatment of biliary and urinary tract disorders. It acts as a catechol-O-methyltransferase (COMT) inhibitor and exhibits musculotropic effects that relax smooth muscle, particularly the sphincter of Oddi. More recently, flopropione has been repositioned for the prevention of cisplatin-induced nephrotoxicity. In this context, it functions as an inhibitor of cysteine conjugate beta-lyase (C-S lyase), an enzyme responsible for metabolizing cisplatin-cysteine conjugates into highly reactive and nephrotoxic thiol compounds. By blocking this bioactivation pathway, flopropione aims to mitigate acute kidney injury in cancer patients receiving cisplatin-based chemotherapy.

Brand names

CospanonCompasLabrodaxMirulevPellegalSpasmex

Other names

2,4,6-trihydroxypropiophenonephloropropiophenonephlorpropiophenone