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elacestrant (Orserdu)
Indications:
- ER-positive, HER2-negative, ESR1-mutated advanced or metastatic breast cancer with disease progression following at least one line of endocrine therapy [1]
Dosage:
- 345 mg PO QD with food
Tabs: 86 mg, 345 mg.
Adverse effects:
- common (> 10%)
- decreased appetite, dyspepsia, nausea, vomiting, diarrhea, constipation
- abdominal pain, musculoskeletal pain, fatigue, headache, hot flush
- increased serum cholesterol, increased serum triglycerides
- increased serum ALT, increased serum AST, increased serum creatinine
- decreased blood hemoglobin, decreased serum sodium
Drug interactions:
- strong & moderate CYP3A4 inducers
- strong & moderate CYP3A4 inhibitors
Mechanism of action:
- estrogen receptor antagonist
- binds to estrogen receptor-alpha
- antineoplastic activity in ER+ HER2- breast cancer resistant to fulvestrant & cyclin-dependent kinase 4/6 inhibitors & in cancers harboring estrogen receptor 1 gene (ESR1) mutations
General
antineoplastic endocrine agent
estrogen antagonist
Database Correlations
PUBCHEM correlations
References
- US Food & Drug Administration. Jan 27, 2023
FDA approves elacestrant for ER-positive, HER2-negative, ESR1-mutated advanced
or metastatic breast cancer.
https://www.fda.gov/drugs/resources-information-approved-drugs/fda-approves-elacestrant-er-positive-her2-negative-esr1-mutated-advanced-or-metastatic-breast-cancer
- Highlights of Prescribing Information
Orserdu (elacestrant) tablets for oral use
https://drive.google.com/file/d/1aE_1XYQqLKDZZZQIOMqU-a-VhQUGIT8w/view