New generation estrogen receptor-targeted agents in breast cancer: present situation and future prospectives.

Abstract

Endocrine therapy which blocking the signaling of estrogen receptor, has long been effective for decades as a primary treatment choice for breast cancer patients expressing ER. However, the issue of drug resistance poses a significant clinical challenge. It's critically important to create new therapeutic agents that can suppress ERα activity, particularly in cases of ESR1 mutations. This review highlights recent efforts in drug development of next generation ER-targeted agents, including oral selective ER degraders (SERDs), proteolysis targeting chimera (PROTAC) ER degraders, other innovative molecules such as complete estrogen receptor antagonists (CERANs) and selective estrogen receptor covalent antagonists (SERCAs). The drug design, efficacy and clinical trials for each compound were detailed.