CG-3-245

CG-3-245 is an experimental, polypharmacologic small molecule hybrid designed to simultaneously inhibit B-cell lymphoma 2 (BCL-2) and FMS-like tyrosine kinase 3 (FLT3). Developed at the University of Florida, the molecule was synthesized by chemically tethering the BCL-2 inhibitor venetoclax to the FLT3 inhibitor gilteritinib through their solvent-exposed domains. This hybrid approach aims to treat acute myeloid leukemia (AML) by leveraging the known clinical synergy between BCL-2 and FLT3 inhibition within a single chemical entity. Preclinical studies indicate that while CG-3-245 possesses antileukemic activity in vitro, the physical combination of the two parent drugs (venetoclax and gilteritinib) currently remains more potent than the hybrid molecule itself.

Other names

VEN-GIL hybridVenetoclax-Gilteritinib hybrid