enzomenib + gilteritinib

**Enzomenib + gilteritinib** is a combination investigational regimen consisting of two small molecule inhibitors. - **Enzomenib** (DSP-5336) is a selective menin inhibitor designed to target leukemogenic gene fusions and mutations, notably KMT2A (MLL) rearrangements and NPM1 mutations in acute myeloid leukemia (AML). Its mechanism blocks menin binding, disrupting oncogenic transcription factors, leading to differentiation and apoptotic effects in leukemic cells. - **Gilteritinib** is an oral, selective FLT3 inhibitor (targeting both FLT3-ITD and FLT3-TKD mutations), approved for relapsed/refractory AML with FLT3 mutations. It inhibits FLT3 signaling required for proliferation and survival of AML blasts. This combination is under clinical investigation for relapsed/refractory AML, particularly in genetically defined subgroups where both FLT3 and MLL/NPM1 mutations co-exist[4][5]. Preclinical data support potential synergy in targeting leukemic stem cell persistence and resistance mechanisms.

Brand names

Xospata (for gilteritinib)

Other names

DSP-5336 + gilteritinib