Imlunestrant is an investigational, oral selective estrogen receptor degrader (SERD) with pure antagonistic properties. The estrogen receptor (ER) is the key therapeutic target for patients with ER+/HER2- breast cancer.
Novel degraders of ER may overcome endocrine therapy resistance while providing consistent oral pharmacology and convenience of administration. Imlunestrant was specifically designed to deliver continuous estrogen receptor target inhibition throughout the dosing period and regardless of ESR1 mutational status.
Imlunestrant is currently being studied in clinical trials. Safety and efficacy have not been established for the uses being studied.
Imlunestrant is currently being evaluated in the following clinical trials:
EMBER: a global, first-in-human, open-label Phase 1a/b trial evaluating LY3484356 alone or in combination with other anticancer therapies in participants with ER+ advanced breast cancer or endometrioid endometrial cancer.
EMBER-2: an open-label Phase 1 trial evaluating LY3484356 in preoperative, postmenopausal women with stage I-III, ER+/HER2- breast cancer.
EMBER-3: a Phase 3, randomized, open-label study of imlunestrant, investigator's choice of endocrine therapy, and imlunestrant plus abemaciclib in patients with estrogen-receptor-positive, HER2-negative locally advanced or metastatic breast cancer previously treated with endocrine therapy
- A Phase 1a/b trial of imlunestrant (LY3484356), an oral selective estrogen receptor degrader (SERD) in ER-positive (ER+) advanced breast cancer (aBC) and endometrial endometrioid cancer (EEC): Monotherapy results from EMBER
- A first-in-human phase 1a/b trial of LY3484356, an oral selective estrogen receptor (ER) degrader (SERD) in ER+ advanced breast cancer (aBC) and endometrial endometrioid cancer (EEC): Results from the EMBER study
- Preclinical characterization of LY3484356, a novel, potent and orally bioavailable selective estrogen receptor degrader (SERD)