APG-115 + azacitidine

APG-115 + azacitidine is a combination investigational therapy for hematologic malignancies, notably relapsed/refractory acute myeloid leukemia (AML), chronic myelomonocytic leukemia (CMML), and high-risk myelodysplastic syndrome (MDS). APG-115 is an orally active, small-molecule inhibitor of the mouse double minute 2 homolog (MDM2), which prevents MDM2 from degrading the tumor suppressor protein p53, thereby reactivating p53 function, triggering apoptosis, and cell cycle arrest in p53 wild-type malignant cells. Azacitidine is a hypomethylating chemotherapeutic agent that inhibits DNA methyltransferase, leading to DNA hypomethylation, DNA damage, and reactivation of tumor suppressor genes. The combination is being studied due to evidence of synergistic antileukemic effects by concurrently activating the p53/p21 pathway and promoting apoptosis and cell cycle arrest in malignant hematopoietic cells[1][3][5].

Other names

APG-115 + 5-azacitidine