wx-671

Upamostat is an inhibitor of a serine protease and is a urokinase plasminogen activator (uPA) inhibitor.

Upamostat, also known as Mesupron and WX-671, is an orally bioavailable second-generation serine protease inhibitor prodrug derived from 3-amidinophenylalanine. It targets the human urokinase plasminogen activator (uPA) system and exhibits potential antineoplastic and antimetastatic properties. After oral administration, the serine protease inhibitor WX-671 is converted into its active form, Nα-(2,4,6-triisopropylphenylsulfonyl)-3-amidinophenylalanine-4-ethoxycarbonylpiperazinylamide (WX-UK1), which inhibits multiple serine proteases, especially uPA, potentially hindering tumor growth and metastasis.

(E)-Upamostat ((E)-WX-671) is the E-isomer of Upamostat. Upamostat (WX-671) serves as a prodrug of WX-UK1, functioning as an orally active serine protease inhibitor.