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Drugs that do not just block the oestrogen receptor but mark it for destruction, so the cancer cell loses the receptor altogether. The new oral versions work even when the receptor has mutated (ESR1) to escape older hormone pills.
Fulvestrant (2002) is an injectable SERD limited by incomplete degradation; elacestrant (2023, EMERALD) was the first oral SERD, approved for ESR1-mutant metastatic disease, followed by camizestrant (SERENA-6, switching at ctDNA-detected ESR1 mutation), imlunestrant and vepdegestrant (a PROTAC). Oral SERDs are now in adjuvant trials (CAMBRIA, lidERA) and in combinations with CDK4/6 and PI3K/AKT inhibitors. Tamoxifen is the older selective modulator (SERM) that blocks the receptor in breast but stimulates it in bone and uterus.
In plain words · The hormone switch that drives most breast cancers. Blocking or destroying it is the oldest and most effective targeted therapy.
Showing the target this term concerns: Estrogen receptor (ERα).
The glossary entry explains the word; the readout page carries the scoring rule, the thresholds approvals use, the companion diagnostics and the tests.
Shares EMERALD, Elacestrant, Estrogen receptor (ERα), Fulvestrant.
Shares Hormone receptor status (ER / PR), ER status (oestrogen receptor by IHC), Tamoxifen, Fulvestrant.
Shares EMERALD, ESR1 mutation (ligand-binding domain, usually in ctDNA), SERENA-6, Elacestrant.
Shares Aromatase inhibitor, Hormone receptor status (ER / PR), Estrogen receptor (ERα).
Shares Estrogen receptor (ERα), Fulvestrant, PROTACs & molecular glues (targeted protein degradation), Endocrine therapy (SERMs, AIs, SERDs).
Shares Elacestrant, Estrogen receptor (ERα), Fulvestrant, HR-positive / HER2-negative breast cancer.
Shares EMERALD, Elacestrant, Estrogen receptor (ERα), Endocrine therapy (SERMs, AIs, SERDs).
Shares EMERALD, Elacestrant.