entospletinib + azacitidine

**entospletinib + azacitidine** is a combination therapy consisting of entospletinib, a selective oral small molecule inhibitor of spleen tyrosine kinase (SYK), and azacitidine, a hypomethylating agent. Entospletinib inhibits SYK, which is upregulated in certain acute myeloid leukemia (AML) cells and contributes to leukemogenesis via activation of multiple downstream pathways such as FLT3, STAT3, STAT5, mTOR, and integrin signaling. Azacitidine is a pyrimidine nucleoside analog that integrates into RNA and DNA, where it inhibits DNA methyltransferases, inducing DNA hypomethylation and cytotoxicity, particularly in rapidly dividing abnormal hematopoietic cells. This combination targets high-risk AML, especially in older patients or those with *TP53* mutations or complex karyotypes. Clinical trials have shown the regimen to be active and generally tolerated, though overall response and survival rates remain limited, highlighting the need for novel approaches[1][2].

Other names

entospletinibazacitidineVidaza