Because selective BET inhibitors present better efficacy and safety than pan-BET inhibitors, current research is focused on the development of BD1- or BD2-selective inhibitors.
Auron Therapeutics Inc. has nominated its first development candidate, AUTX-703, which is being developed for the treatment of patients with small-cell lung cancer, neuroendocrine prostate cancer and acute myeloid leukemia.
The bromodomain and extraterminal domain (BET) family of proteins are involved in cell cycle regulation and for this reason are considered therapeutic targets in cancer therapeutics.
Gilead Sciences Inc. has officially discontinued work on anti-CD47 antibody magrolimab in hematologic cancers, nearly four years after shelling out $4.9 billion to acquire its developer, Forty Seven Inc. The company announced in its full-year 2023 earnings Feb. 6 call that the phase III Enhance-3 study testing magrolimab as a first-line treatment in unfit acute myeloid leukemia patients was discontinued following a futility analysis and higher incidence of grade 5 adverse events.
Acute myeloid leukemia (AML) presents high recurrence and low survival rates due to drug resistance and different gene mutations that contribute to the difficulty of being cured. Cyclin-dependent kinase 8 (CDK8) is a key oncogenic driver in AML and thus considered a therapeutic target worth exploring.
One-third of patients with acute myeloid leukemia (AML) present mutations in the FMS-like tyrosine kinase 3 (FLT3) gene. Several first- and next-generation FLT3 inhibitors are currently being used in AML management, but there is a need for new options able to achieve complete and sustained FLT3 signaling suppression.
Simultaneous inhibition of the phosphoinositide 3-kinase (PI3K) signaling pathway and histone deacetylase (HDAC) provides synergistic efficacy in the treatment of hematological malignancies.