amcenestrant + everolimus

Amcenestrant + everolimus is an investigational oral combination of two antineoplastic agents: amcenestrant, a next-generation selective estrogen receptor degrader (SERD), and everolimus, a small-molecule inhibitor of the mammalian target of rapamycin (mTOR). Amcenestrant antagonizes the estrogen receptor alpha, accelerating its proteasomal degradation, thereby blocking estrogen-driven signaling in breast cancer cells. Everolimus inhibits mTOR, a downstream regulator in the PI3K/AKT pathway, and is approved for several cancers, including hormone receptor-positive breast cancer. The combination aims to provide therapeutic synergy in hormone-dependent and especially estrogen receptor-positive breast cancers by targeting both hormone signaling and resistance pathways. Both agents are administered orally. Preclinical models demonstrate that this combination induces greater anti-tumor efficacy and tumor regression compared to either agent alone.