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Oral drugs that destroy the oestrogen receptor rather than just blocking it, working even when the receptor has mutated to escape older hormone therapies.
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.
Ligand-like molecules bind the oestrogen receptor and induce a conformation that is ubiquitinated and degraded, removing the receptor even when mutated.
Query 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.
Shares Imlunestrant, Giredestrant, Camizestrant, Elacestrant.
Shares Elacestrant, Endocrine therapy (SERMs, AIs, SERDs), HR-positive / HER2-negative breast cancer.
Shares Imlunestrant, Endocrine therapy (SERMs, AIs, SERDs), HR-positive / HER2-negative breast cancer.
Shares Giredestrant, Endocrine therapy (SERMs, AIs, SERDs), HR-positive / HER2-negative breast cancer.
Shares Imlunestrant, Camizestrant, Elacestrant, HR-positive / HER2-negative breast cancer.
Shares Imlunestrant, Camizestrant, HR-positive / HER2-negative breast cancer.
Shares Giredestrant, Endocrine therapy (SERMs, AIs, SERDs), HR-positive / HER2-negative breast cancer.
Shares Giredestrant, Endocrine therapy (SERMs, AIs, SERDs), HR-positive / HER2-negative breast cancer.