Olema Oncology presents preclinical data on anti-tumor activity for OP-3136

Olema Pharmaceuticals announced results from three preclinical studies that will be presented during poster sessions at the 36th EORTC-NCI-AACR Symposium on Molecular Targets and Cancer Therapeutics in Barcelona, Spain. Title: “Combining OP-3136, a KAT6 inhibitor, with endocrine therapy and CDK4/6 inhibitor enhances anti-tumor activity in ER+/HER2- breast cancer models”. Key findings include: OP-3136 inhibited cell proliferation and synergized with anti-estrogens and a CDK4/6 inhibitor in a breast cancer cell line. OP-3136 led to either tumor growth inhibition or tumor regression in vivo in xenograft models across all treatment groups. In combination with OP-3136, palazestrant was consistently superior to fulvestrant and led to improved anti-tumor activity and tumor regression. OP-3136 showed robust synergistic anti-tumor activity when combined with fulvestrant or palazestrant as doublet therapy in breast cancer models. Title: “Combining palazestrant, a CERAN, and everolimus, an mTOR inhibitor, enhances tumor suppression in ER+/HER2- breast cancer models”: Key findings include: Palazestrant and everolimus demonstrate synergy in vitro and in vivo and resulted in greater anti-proliferative activity than either agent alone. Combining palazestrant with everolimus causes gene signature transcriptional changes, downregulating cell cycle progression and upregulating apoptosis. These data support clinical investigation of the combination of palazestrant and everolimus. Title: “Combining palazestrant, a CERAN, and capivasertib, a pan-AKT inhibitor, enhances tumor suppression in ER+/HER2- breast cancer models”: Key findings include: Palazestrant and capivasertib work synergistically to inhibit proliferation of multiple ER+ breast cancer models, both in vitro and in vivo. Palazestrant demonstrates superior anti-tumor efficacy over fulvestrant in combination with capivasertib, significantly inhibiting and repressing tumor growth. Combining palazestrant and capivasertib increases downregulation of genes associated with cell cycle progression. These data support clinical investigation of the combination of palazestrant and capivasertib.