Dual Targeting of BET proteins and DRD2 Halts Cancer Survival and Resistance Pathways
We are seeking a pharma licensee or co-developer for our first-in-class dual inhibitor CG223 selective against both BET proteins and Dopamine Receptor 2 (DRD2).
CG223 is “affinity tunable” with 2 distinct sites for binding of BET bromo-domain proteins and DRD2. This unique dual mechanism of action is first-in-class. The distinct chemical structure of our drug has resulted in a superior pharmacological profile compared to competing drugs that are based on a common benzodiazepine scaffold.
In animal tumor models, treatment with our drug candidate leads to significant depletion of cancer gene products driven by cMYC and also blocks DRD2 signaling leading to striking inhibition of tumor growth.
Suppressing two targets necessary for cell proliferation and survival provides our drug candidates with a clear competitive advantage compared to single action drugs.