Imlunestrant is an estrogen receptor antagonist used to treat estrogen receptor (ER)-positive, human epidermal growth factor receptor 2 (HER2)-negative, estrogen receptor-1 (ESR1)-mutated advanced or metastatic breast cancer in adults with previous endocrine therapy. Imlunestrant works by antagonizing ER transcriptional activity and, by forming an unstable drug-receptor complex, promotes ER degradation via the ubiquitin-proteasome pathway.
- Mechanism
- Curator reviewed · 5 references
Estrogen receptor signalling has closely been tied to breast cancer progression and cancer cell proliferation. Estrogen receptor alpha (ERα) has been primarily implicated in breast cancer, and its activation promotes the expression of oncogenic factors that increase cancer cell proliferation, such as MYC, Cyclin D1, FOXM1, GREB1, BCL2 or amphiregulin, IGF-1 and CXCL12. Imlunestrant binds to ERα with high affinity and, in vitro, induces degradation of ERα: This leads to the inhibition of ER-dependent gene transcription and cellular proliferation in ER+ breast cancer cells.
- Primary indication
- Imlunestrant is indicated for the treatment of adults with estrogen receptor (ER)-positive, human epidermal growth factor receptor 2 (HER2)-negative, estrogen receptor-1 (ESR1)-mutated advanced or metastatic breast cancer with disease progression following at least one line...Curator reviewed · 2 structured indications
- Formula / weight
- C29H24F4N2O3 · 524.516 g/mol (avg)
- First approval
- United States, 2025 · European Union, 2026
- Also known as
- (5r)-5-(4-(2-(3-(fluoromethyl)azetidin-1-yl)ethoxy)phenyl)-8-(trifluoromethyl)-5h-(1)benzopyrano(4,3-c)quinolin-2-ol · 5h-(1)benzopyrano(4,3-c)quinolin-2-ol, 5-(4-(2-(3-(fluoromethyl)-1-azetidinyl)ethoxy)phenyl)-8-(trifluoromethyl)-, (5r)-
- Code names
- LY-3484356
- Brand names
Resolves to
UVBQMXOKKDCBJN-MUUNZHRXSA-NSMILES[H][C@@]1(OC2=CC(=CC=C2C2=C1C1=CC=C(O)C=C1N=C2)C(F)(F)F)C1=CC=C(OCCN2CC(CF)C2)C=C1What you can answer from here — as of September 12, 2026
Which drugs share a target with Imlunestrant, and which of those have an active Phase 3 trial?
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