ATH-002 / Atheron Therapeutics - LARVOL DELTA

Discovery of a highly potent and selective KAT6A degrader ATH-002 that demonstrates robust anti-tumor activity with a low risk of hematotoxicity in preclinical studies (AACR 2026) - "PF-07248144, the first KAT6A/6B dual inhibitor to enter the clinic, demonstrates durable anti-tumor activity in ER+HER2− metastatic breast cancer, especially in combination with fulvestrant. Besides monotherapy, ATH-002 displayed an enhanced anti-proliferation effect in combination with SERDs or CDK4/6 inhibitors without overlapping hematotoxicity, implying a potential application of KAT6A degrader and SOC therapy. Collectively, our findings support ATH-002 as a clinical candidate for the treatment of KAT6A-amplified tumors."

Preclinical • Breast Cancer • Estrogen Receptor Positive Breast Cancer • HER2 Breast Cancer • HER2 Positive Breast Cancer • Oncology • Solid Tumor • ER • HER-2 • KAT6A • KAT6B • KMT2A • PARP1