ERAS-007 + gilteritinib

ERAS-007 + gilteritinib is an investigational combination therapy comprised of two small molecule inhibitors, ERAS-007 and gilteritinib, being studied primarily for the treatment of relapsed or refractory hematologic malignancies, including acute myeloid leukemia (AML)[1][5]. ERAS-007 is a potent, selective, oral ATP-competitive inhibitor of ERK1/2, targeting the RAS/MAPK pathway, which is a frequent driver of resistance in various cancers such as those with RAS/MAPK pathway alterations[5]. Gilteritinib is an orally available, small molecule inhibitor indicated for use in AML with FLT3 mutations, functioning by inhibiting multiple receptor tyrosine kinases, including FMS-like tyrosine kinase 3 (FLT3), AXL, and ALK, thereby blocking cancer cell growth and survival through inhibition of downstream effectors such as STAT5, ERK, and AKT[2][4][5]. The combination aims to disrupt oncogenic signaling by simultaneously targeting FLT3 mutations and downstream ERK activity, potentially overcoming resistance mechanisms in hematologic cancers[1][5]. ERAS-007 was developed by Erasca, and gilteritinib was developed by Astellas Pharma[2][5].

Other names

ERAS-007 + gilteritinib