ATH-007

ATH-007 is a potent and highly selective Cyclin E1 (CCNE1) molecular glue degrader being developed by Atheron Therapeutics for the treatment of CCNE1-amplified malignancies. CCNE1 is a critical cell cycle regulator that, when amplified, drives oncogenesis and contributes to resistance against chemotherapy and CDK4/6 inhibitors in various cancers, including breast, high-grade serous ovarian, uterine, and gastro-esophageal cancers. ATH-007 functions by recruiting the Cereblon (CRBN) E3 ubiquitin ligase to induce the proteasomal degradation of CCNE1. Preclinical data presented at AACR 2026 indicates that ATH-007 achieves complete protein degradation (Dmax >95%) with high selectivity over other CRBN substrates such as GSPT1 and IKZF1. Furthermore, the compound demonstrates a favorable safety profile with minimal hematotoxicity and reduced hERG inhibition compared to traditional CDK2 inhibitors, alongside robust dose-dependent anti-tumor activity in vivo.