WX-671 + capecitabine

WX-671 + capecitabine is a combination of two oral agents: WX-671 (also known as upamostat, Mesupron), an oral prodrug of the serine protease inhibitor WX-UK1 that targets urokinase-type plasminogen activator (uPA), and capecitabine, a cytotoxic chemotherapeutic agent that is a prodrug of 5-fluorouracil (5-FU). WX-671 inhibits uPA catalytic activity, thereby interfering with tumor cell invasion, metastasis, and tumor growth. Capecitabine is converted to 5-FU, which inhibits thymidylate synthase and disrupts DNA synthesis. This combination was developed primarily to enhance antitumor efficacy and target the metastatic spread of cancers, especially in metastatic breast cancer (MBC) and other solid tumors, with the hypothesis that dual inhibition of tumor proliferation and invasion/metastasis would have synergistic effects. Key studies include a Phase II, double-blind, randomized trial in HER2-negative metastatic breast cancer comparing WX-671 plus capecitabine versus capecitabine monotherapy. The combination is administered orally in 3-week cycles until disease progression or unacceptable toxicity. The main clinical endpoints have been progression-free survival, overall survival, and safety/tolerability[1][3][4].

Brand names

MesupronXeloda

Other names

upamostatcapecitabine