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Imlunestrant is an investigational **oral, brain-penetrant selective estrogen receptor degrader** designed to act as a pure estrogen receptor antagonist and to provide continuous estrogen receptor inhibition, including in **ESR1-mutant** breast cancer. Developed by **Eli Lilly**, it is being studied primarily for **ER-positive, HER2-negative breast cancer** in both advanced/metastatic and adjuvant early-disease settings. In the EMBER clinical program, imlunestrant established a recommended phase 2/3 dose of **400 mg once daily** based on phase 1 and preoperative pharmacodynamic data, showed manageable mostly low-grade gastrointestinal and fatigue-related toxicities as monotherapy, and demonstrated phase 3 activity in **ESR1-mutated advanced breast cancer** as monotherapy and broader activity in combination with **abemaciclib** as an all-oral endocrine-based regimen.
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