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CG-3-245
- Development stage
- Preclinical
- Lead developer
- University of Florida
- Modality
- Small Molecules
01
Overview
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
02
Targets
BCL-2 (BCL-2 family)FLT3 (Fms related receptor tyrosine kinase 3)
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