AZ6197 / AstraZeneca - LARVOL DELTA

Subversion of ERK-MAPK-mediated mRNA translation elongation as a therapeutic strategy in CLL (IWCLL 2025) - "To determine the effects of targeting ERK-MAPK signalling, we combined AZ6197, a novel ERK1/2 inhibitor, alone and in combination with ibrutinib (ERKi IBR). These analyses also identify ERK-MAPK as a novel target for modulating protein synthesis in CLL. Through in vitro CLL modelling, and in vivo studies, we have demonstrated that targeting both ERK and BTK signalling simultaneously, to therapeutically block protein synthesis via eEF2 signalling, is an attractive clinical strategy."

Chronic Lymphocytic Leukemia • Hematological Malignancies • CD40LG • EEF2 • EEF2K • IL21 • MAPK13

Selumetinib-based therapy in uveal melanoma patient-derived xenografts (AACR 2018) - "Selumetinib was administered alone or combined with chemotherapies (dacarbazine and docetaxel) or targeted therapies: the ERK inhibitor, AZ6197 and the mTORC1/2 inhibitor, vistusertib (AZD2014). Our data suggest that ERK and mTORC1/2 targeting could represent promising therapeutic approaches for the treatment of metastatic UM patients."

Clinical • Ocular Melanoma