VRN16

VRN16 is a novel, highly selective small molecule inhibitor of PKMYT1 (Protein Kinase, Membrane Associated Tyrosine/Threonine 1) developed by Voronoi Productions. PKMYT1 is a serine/threonine kinase that regulates the G2/M phase transition by inhibiting CDK1. In cancers driven by CCNE1 (Cyclin E1) amplification, cells become dependent on PKMYT1 to prevent premature entry into mitosis. By inhibiting PKMYT1, VRN16 forces these cancer cells into mitosis without adequate DNA repair, resulting in mitotic catastrophe and cell death. Preclinical data indicates that VRN16 possesses superior selectivity over other kinases like WEE1, PLKs, and BRAF, potentially offering a wider therapeutic window. It is currently being investigated for the treatment of CCNE1-driven solid tumors, including ovarian, uterine, gastric, and breast cancers.