lomonitinib

Lomonitinib is a highly potent and selective small molecule inhibitor that targets both FLT3 and IRAK4 pathways. It specifically inhibits FLT3 internal tandem duplications (ITD), tyrosine kinase domain (TKD), and other clinically relevant FLT3 mutations, as well as IRAK4, a critical mediator in resistance mechanisms. FLT3 mutations are the most frequently identified in acute myeloid leukemia (AML), and resistance to FLT3 inhibitors often arises via the FLT3-ITD-F691L "gatekeeper" mutation or activation of the IRAK4 escape pathway. By inhibiting both, lomonitinib is designed to overcome resistance that limits the efficacy of current FLT3 inhibitors. Early-phase clinical studies have demonstrated a strong safety profile, dose-proportional pharmacokinetics, and effective target engagement with no significant adverse events. Lomonitinib is being developed primarily for the treatment of relapsed/refractory AML with FLT3 mutations, with potential for further expansion into other hematologic and solid malignancies related to FLT3 and IRAK4 pathway activation[1][2][3][4][5][6][7][8][10].

Other names

Lomonitinib [inn]