EAPB02303

EAPB02303 is a small molecule anti-cancer agent classified as a prodrug, structurally related to imiqualines, with potent cytotoxic activity at nanomolar concentrations. Its mechanism of action is unique in that it requires bioactivation by the enzyme catechol-O-methyltransferase (COMT), which converts EAPB02303 into its active metabolite, EAPB04303. The active form inhibits microtubule polymerization, thereby disrupting microtubule dynamics and arresting cell division. EAPB02303 also potently downregulates the PI3K/AKT/mTOR and RAS/MAPK signaling pathways, key regulators of cell survival and proliferation, and induces degradation of mutant NPM1 (NPM1c), particularly relevant in acute myeloid leukemia (AML). The drug demonstrates strong anti-tumor activity in preclinical models of pancreatic ductal adenocarcinoma (PDAC) and AML, including chemoresistant forms. Notably, EAPB02303 exhibits selectivity for cancer cells and a favorable toxicity profile in mice[1][2][3].