Information PFK158 PFK158 is a potent and selective inhibitor of PFKFB3 . It has improved PK properties and causes ~80% growth inhibition in several mouse models of human-derived tumors. Targets PFKFB3 In vitro PFK158 results in reduced glucose uptake, ATP production, lactate release as well as induction of apoptosis in gynecologic cancer cells. PFK158 treatment sensitizes chemoresistant cells and induces cell death.