CG-3-242

CG-3-242 is an experimental, polypharmacologic small molecule designed as a dual inhibitor of B-cell lymphoma 2 (BCL-2) and FMS-like tyrosine kinase 3 (FLT3). It is a hybrid molecule synthesized by chemically linking the BCL-2 inhibitor venetoclax and the FLT3 inhibitor gilteritinib through their solvent-exposed domains. Developed primarily for the treatment of acute myeloid leukemia (AML), CG-3-242 aims to provide the synergistic benefits of dual pathway inhibition within a single therapeutic agent, potentially simplifying treatment regimens and ensuring concurrent target engagement within the same cell. Preclinical evaluations have compared its efficacy to the co-administration of venetoclax and gilteritinib, exploring its potential to overcome the heterogeneity and adaptive resistance common in AML. However, recent research suggests that the physical combination of the two parent drugs may maintain higher potency than this specific hybrid scaffold in certain AML cell models.

Other names

VEN-GIL hybridVenetoclax-Gilteritinib hybrid