Elacestrant Dihydrochloride

• Elacestrant Dihydrochloride is an oral selective estrogen receptor degrader (SERD) used for advanced or metastatic breast cancer.
• It targets hormone receptor-positive (HR+), HER2-negative (HER2-) breast cancer, especially after progression on endocrine therapy.
• The medication works by binding to and degrading estrogen receptors, thereby inhibiting cancer cell growth.
• Common side effects include musculoskeletal pain, nausea, fatigue, and elevated cholesterol levels.
• Its approval provides a new therapeutic option for patients with ESR1 mutations, which are often associated with resistance to standard endocrine treatments.

What is Elacestrant Dihydrochloride?

Elacestrant Dihydrochloride is a non-steroidal oral selective estrogen receptor degrader (SERD) approved for the treatment of postmenopausal women and adult men with advanced or metastatic estrogen receptor-positive (ER+), human epidermal growth factor receptor 2-negative (HER2-) breast cancer. This medication is specifically indicated for patients whose disease has progressed after at least one line of endocrine therapy in the metastatic setting, or prior endocrine therapy followed by at least one line of chemotherapy in the metastatic setting. Its development addresses a critical need for new treatment options in this patient population, particularly those with ESR1 mutations, which can lead to resistance to conventional endocrine therapies.

Breast cancer remains a significant global health challenge. According to the World Health Organization (WHO), breast cancer is the most common cancer among women globally, accounting for 1 in 8 cancer diagnoses. The introduction of novel therapies like Elacestrant Dihydrochloride is crucial for improving patient outcomes, especially in advanced stages where treatment options can be limited.

Elacestrant Dihydrochloride Uses and Mechanism of Action

The primary Elacestrant Dihydrochloride uses are in the treatment of advanced or metastatic ER-positive, HER2-negative breast cancer. It is particularly relevant for patients who have developed resistance to existing endocrine therapies, often due to mutations in the estrogen receptor 1 (ESR1) gene. These mutations are common in metastatic breast cancer and can render traditional endocrine treatments less effective. Elacestrant Dihydrochloride offers a targeted approach to overcome this resistance.

The Elacestrant Dihydrochloride mechanism of action involves its role as a selective estrogen receptor degrader. Upon oral administration, Elacestrant Dihydrochloride binds to the estrogen receptor (ER) with high affinity. This binding leads to a conformational change in the receptor, which subsequently triggers its degradation via the ubiquitin-proteasome pathway. By effectively reducing the levels of functional estrogen receptors within cancer cells, Elacestrant Dihydrochloride inhibits the estrogen-dependent signaling pathways that drive tumor growth. This mechanism is distinct from traditional selective estrogen receptor modulators (SERMs) and provides a potent way to counteract ER-driven proliferation, even in the presence of ESR1 mutations.

Elacestrant Dihydrochloride Side Effects

Like all medications, Elacestrant Dihydrochloride can cause side effects. Patients should discuss potential adverse reactions with their healthcare provider and report any concerning symptoms promptly. The most common Elacestrant Dihydrochloride side effects observed in clinical trials include:

• Musculoskeletal pain
• Nausea
• Fatigue
• Vomiting
• Decreased appetite
• Diarrhea
• Constipation
• Abdominal pain
• Headache
• Hot flashes
• Elevated cholesterol levels (hypercholesterolemia)
• Elevated triglycerides (hypertriglyceridemia)

More serious, though less common, side effects can include severe nausea, vomiting, or fatigue that may require dose modification or supportive care. It is crucial for patients to adhere to their prescribed dosage and schedule and to communicate openly with their oncology team regarding any adverse events experienced during treatment. Regular monitoring of blood counts and liver function may also be part of the treatment regimen to manage potential side effects effectively.