CG-4-208

CG-4-208 is a dual-targeting small molecule hybrid inhibitor designed for the treatment of acute myeloid leukemia (AML). It is a single-molecule entity created by chemically linking the BCL-2 inhibitor venetoclax and the FLT3 inhibitor gilteritinib through their solvent-exposed domains. By simultaneously inhibiting BCL-2 (an anti-apoptotic protein) and FLT3 (a receptor tyrosine kinase), CG-4-208 aims to overcome resistance mechanisms and enhance therapeutic efficacy in AML cells that rely on both pathways for survival. Although designed to improve upon the polypharmacy approach of combining the two separate drugs, preclinical evaluations have shown that the physical combination of venetoclax and gilteritinib may currently outperform this specific hybrid molecule in terms of antileukemic activity.

Other names

VEN-GIL hybridVenetoclax-Gilteritinib hybrid inhibitor