Elacestrant: Oral SERD for Breast Cancer Treatment
Elacestrant is an oral selective estrogen receptor degrader (SERD) used to treat HR-positive, HER2-negative advanced breast cancer, particularly in patients with ESR1 mutations.
Things worth knowing about "Elacestrant"
Elacestrant is an oral selective estrogen receptor degrader (SERD) used to treat HR-positive, HER2-negative advanced breast cancer, particularly in patients with ESR1 mutations.
What is Elacestrant?
Elacestrant is an oral selective estrogen receptor degrader (SERD) used in the treatment of advanced or metastatic hormone receptor (HR)-positive, HER2-negative breast cancer. It is a targeted therapy specifically developed for patients whose disease has progressed despite prior endocrine therapy – particularly in cases involving an ESR1 mutation (a mutation in the estrogen receptor gene).
Mechanism of Action
Elacestrant works by selectively binding to the estrogen receptor alpha and triggering its degradation (breakdown) within the tumor cell. Unlike other anti-hormonal therapies such as aromatase inhibitors, elacestrant does not merely block the receptor – it actively promotes the destruction of the receptor protein. This effectively interrupts the estrogen signaling that drives tumor growth.
A key advantage of elacestrant is its activity against tumor cells harboring an ESR1 mutation. These mutations frequently develop as a resistance mechanism during prior aromatase inhibitor therapy and result in constitutive (estrogen-independent) activation of the estrogen receptor. Elacestrant is able to bind to and degrade even these mutated receptor forms.
Indication and Use
Elacestrant is approved for the treatment of postmenopausal women and adult men with:
- Hormone receptor (HR)-positive and HER2-negative advanced or metastatic breast cancer
- Disease progression following at least one line of endocrine therapy, including prior CDK4/6 inhibitor-based therapy
- Presence of an ESR1 mutation (particularly effective in this patient population)
Dosage and Administration
Elacestrant is administered as an oral tablet. The recommended dose is 345 mg once daily, preferably taken with food to improve tolerability. Treatment is continued until disease progression or unacceptable toxicity occurs.
Side Effects
As with all oncology medications, elacestrant may cause side effects. The most commonly reported include:
- Nausea and vomiting
- Elevated cholesterol and triglyceride levels (dyslipidemia)
- Fatigue
- Diarrhea
- Abdominal pain
- Decreased appetite
- Elevated liver enzyme levels
Serious side effects are rare but possible. Regular blood tests are recommended to monitor liver function and lipid levels during treatment.
Clinical Evidence
The approval of elacestrant was primarily based on results from the EMERALD trial, a randomized Phase 3 study. In this trial, elacestrant demonstrated a statistically significant improvement in progression-free survival compared to standard endocrine therapy, particularly in patients with ESR1 mutations. These results supported approval by the FDA (United States, 2023) and the EMA (European Union).
References
- Bidard FC et al. - Elacestrant (oral selective estrogen receptor degrader) versus standard endocrine therapy for estrogen receptor-positive, human epidermal growth factor receptor 2-negative advanced breast cancer: EMERALD Phase 3 Trial. Journal of Clinical Oncology, 2022.
- U.S. Food and Drug Administration (FDA) - Prescribing Information for Orserdu (Elacestrant), 2023. Available at: www.fda.gov
- European Medicines Agency (EMA) - Assessment Report: Orserdu (Elacestrant), 2023. Available at: www.ema.europa.eu
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