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FLAV-27
FLAV-27 is a novel epigenetic lead compound designed to treat Alzheimer’s (AD), Huntington disease (HD) and other central nervous system (CNS) disorders. We have developed a new class of G9a inhibitors with high in vitro potency and selectivity while avoiding toxicity issues. Unlike commercially available G9a inhibitors such as UNC0642, which showed neuroprotective effects but failed due to adverse ADMET profiles and poor blood-brain barrier (BBB) permeability, FLAV-27 demonstrates superior pharmacokinetics. PK/TK studies reveal a 3.8-fold higher brain-to-plasma concentration. Additionally, it exhibits neuroprotective effects in both in vitro PD models and in vivo AD/HD mouse models. Toxicology studies confirm its safety and tolerability.
The practical application of the drug would be its use as a therapeutic treatment for Alzheimer’s disease and other central nervous system disorders characterized by G9a overexpression. Inhibition of this enzyme could improve symptoms, slow disease progression, and/or modify the underlying molecular mechanisms.