zeprumetostat + HRS-8080 or zeprumetostat + HRS-1358

Zeprumetostat (SHR2554) is an oral, selective small molecule inhibitor of Enhancer of Zeste Homolog 2 (EZH2), a histone methyltransferase that catalyzes the trimethylation of histone H3 lysine 27 (H3K27me3) to promote gene silencing. In the context of advanced breast cancer, zeprumetostat is being investigated in combination with novel endocrine therapies developed by Jiangsu Hengrui Pharmaceutical: HRS-8080, an oral selective estrogen receptor degrader (SERD), and HRS-1358, an estrogen receptor-targeting proteolysis-targeting chimera (PROTAC). These combinations are designed to address endocrine resistance by simultaneously inhibiting the estrogen receptor signaling pathway and EZH2-mediated epigenetic reprogramming. A Phase 2 trial sponsored by Henan Cancer Hospital evaluates the safety and preliminary efficacy of these all-oral regimens in patients with advanced breast cancer.

Other names

SHR2554 + HRS-8080SHR2554 + HRS-1358SHR2554 + Endocrine Therapy