University of Maryland has presented proteolysis targeting chimeras (PROTACs) comprised of E3 ubiquitin ligase cereblon (CRBN)-binding moiety covalently linked to induced myeloid leukemia cell differentiation protein Mcl-1-binding moiety through a linker reported to be useful for the treatment of cancer.
Peptide-drug conjugates are an emerging class of molecules that allow efficient targeted drug delivery into tumors. Researchers from Oncopeptides AB and their collaborators presented data on the novel peptide-drug conjugate OPDC3, which has a novel alkylating payload, in models of diffuse large B-cell lymphoma (DLBCL) and acute myeloid leukemia (AML).
Oncoprotein Myc is known to be dysregulated in about 70% of cancers, and it is highly expressed in leukemias and lymphomas. Targeting Myc has not been successful and is still an unmet clinical need for cancer patients.
Janssen Pharmaceutica NV and Johnson & Johnson (China) Investment Ltd. have identified substituted phenyl-1H-pyrrolo [2, 3-c] pyridine derivatives acting as menin (MEN1)/MLL interaction inhibitors reported to be useful for the treatment of cancer.
Acute myeloid leukemia (AML) is characterized by hematopoietic precursors arrested in early stages of development. Approximately 20,000 diagnoses and 11,000 deaths occur annually in the United States despite treatment advances.
Affimed NV has received clearance of a clinical trial application (CTA) by the French National Agency for the Safety of Medicines and Health Products (ANSM) for a phase I study of AFM-28 (AFM28-101) in CD123-positive relapsed or refractory acute myeloid leukemia (AML).
Magenta Therapeutics Inc., the developer of an antibody-drug conjugate intended to help prep certain relapsed/refractory acute myeloid leukemia and myelodysplastic syndrome patients for stem cell transplant or gene therapy, has stopped dosing the drug in part of an ongoing trial after observing two cases of serious adverse events (SAEs) possibly related to the candidate.
Ordaōs Bio Inc. has entered into a joint development agreement with Yatiri Bio Inc. to create new therapeutics for two novel targets in acute myeloid leukemia (AML).
The histone-lysine N-methyltransferase 2A (KMT2A; also known as mixed-lineage leukemia 1 [MLL1])-fusion proteins require direct interaction with the nuclear scaffolding protein menin in order to form menin-KMT2A complex, which plays a key role in the transcription of multiple leukemogenic target genes. On the basis of this, it is hypothesized that blocking the menin-KMT2A interaction by small-molecule inhibitors could be a promising new strategy for the treatment of KMT2A-altered and NPM1-mutant acute myeloid leukemia (AML).
Rearrangement of the KMT2A gene is a recurrent mutation in acute myeloid leukemia (AML) that leads to poor outcomes in patients due to increased rate of relapsed and refractory disease. The identification of novel targets and potential therapies is crucial for patients with KMT2A-rearranged leukemias.