Cancer development and tumor progression involve genetic and epigenetic changes in DNA. Histone deacetylases (HDACs) are key regulators of gene expression that act as transcriptional repressors by removing acetyl groups from histones. HDACs are dysregulated in many cancers, making them a therapeutic target for the treatment of cancer. HDAC inhibitors (HDACi), a novel class of small-molecular therapeutics, are now approved by the FDA as anticancer agents.
KYAN-001 targets HDAC4 and HDAC6, the dysregulation of which has been shown by peer-reviewed research to promote cancer cell viability, proliferation and migration, and drug resensitization2
üFirst in class, nucleoshuttling HDACi
üHigh efficacy in vitro and in vivo (tumor growth inhibition at less than 2mM)
üLow toxicity compared to pan-HDACis
üMetabolically stable – avoids clearance of drug to allow for complete and prolonged effectiveness
üMinimal to no CYP enzyme inhibition – low chance of unanticipated adverse effects and therapeutic failure
üAbility to improve other anticancer agents offers prospects for development in combination with other Pharma drugs