Oral SERDs
Oral drugs that destroy the oestrogen receptor rather than just blocking it, working even when the receptor has mutated to escape older hormone therapies.
Overview
Fulvestrant, the first selective oestrogen receptor degrader, needs monthly injections and has poor bioavailability. Oral SERDs (elacestrant, approved in 2023 for ESR1-mutant advanced breast cancer, followed by imlunestrant, camizestrant, giredestrant and the PROTAC degrader vepdegestrant in late trials) degrade the receptor and keep working against ESR1 mutations that arise after aromatase inhibitors. Trials are moving them earlier, guided by circulating tumour DNA detection of ESR1 mutation.
How it works
Ligand-like molecules bind the oestrogen receptor and induce a conformation that is ubiquitinated and degraded, removing the receptor even when mutated.
- Oral
- Active against ESR1-mutant disease
- ctDNA-guided switching strategies
- Benefit concentrated in ESR1-mutant patients
- Nausea and fatigue
- Several candidates failed in unselected populations
Latest papers
topQuery for this technology: (TITLE:"Oral SERDs" OR ABSTRACT:"Oral SERDs") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about Oral SERDs, not a curated reading list.
Similar pages
not linked directly; found by shared links- TermOral SERD
Shares Giredestrant, Imlunestrant, Camizestrant, Elacestrant.
- TermESR1 mutation
Shares Imlunestrant, Vepdegestrant, Camizestrant, Elacestrant.
- IdeaIntercepting late recurrence with ctDNA surveillance and oral SERDs
Shares Giredestrant, Camizestrant, HR-positive / HER2-negative breast cancer.
- PairingOral SERD + CDK4/6 inhibitor after ESR1 emergence
Shares Imlunestrant, Camizestrant, HR-positive / HER2-negative breast cancer.
- TriallidERA
Shares Giredestrant, HR-positive / HER2-negative breast cancer.
- TrialpersevERA
Shares Giredestrant, HR-positive / HER2-negative breast cancer.
- TrialCAMBRIA-1 & CAMBRIA-2
Shares Camizestrant, HR-positive / HER2-negative breast cancer.
- TermHormone therapy
Shares Vepdegestrant, Elacestrant, Endocrine therapy (SERMs, AIs, SERDs), HR-positive / HER2-negative breast cancer.