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Elacestrant for ESR1 Mutant ER-Positive Breast Cancer: Oral Selective Estrogen Receptor Degrader

Novel oral SERD targeting estrogen receptor degradation in endocrine therapy-resistant ESR1 mutated metastatic breast cancer

Written by: Saygı Hospital Health Guide Editorial Board
Last updated:

This content has been compiled by the Saygı Hospital Health Guide Editorial Board and is periodically reviewed by a specialist physician.

This content is for informational purposes only and does not constitute medical advice. You can book an appointment at our Onkoloji department. Book Appointment →

What is Elacestrant for ESR1 Mutant ER-Positive Breast Cancer: Oral Selective Estrogen Receptor Degrader?

Elacestrant is oral selective estrogen receptor degrader binding to ER and inducing receptor conformational change leading to degradation.

ESR1 mutations occur in approximately 30-40% of metastatic ER-positive breast cancer progressing on aromatase inhibitors.

Most common ESR1 mutations include Y537S and D538G producing constitutive receptor activation independent of estrogen.

FDA approval is for ESR1-mutated, ER-positive, HER2-negative advanced or metastatic breast cancer after prior endocrine therapy.

Liquid biopsy with circulating tumor DNA testing identifies ESR1 mutations enabling treatment selection without invasive biopsy.

Symptoms

Nausea is most common adverse effect requiring antiemetic prophylaxis with timing of dose administration.
Fatigue, vomiting and decreased appetite affect quality of life requiring supportive care and symptom management.
Vasomotor symptoms including hot flashes reflect estrogen receptor degradation and effective therapy mechanism.
Constipation, abdominal pain and dyspepsia are common gastrointestinal side effects.
Increased liver function tests, dyslipidemia and bone-related effects require monitoring.

Risk Factors

ESR1 mutations as resistance mechanism develop after aromatase inhibitor therapy with monitoring through liquid biopsy.
Concurrent strong CYP3A4 inhibitors require dose adjustments given metabolic interactions.
Hepatic impairment requires dose modification per established criteria.
Pre-existing nausea, gastroesophageal reflux disease may worsen with elacestrant therapy.
Bone health considerations including baseline DEXA and ongoing surveillance recommended.

When to See a Doctor?

If you experience any of the following symptoms, seek medical attention promptly:

  • ER-positive HER2-negative metastatic breast cancer progression on prior endocrine therapy warrants ESR1 mutation testing.
  • Liquid biopsy ESR1 testing through circulating tumor DNA provides convenient identification of actionable mutation.
  • Severe nausea, vomiting, dehydration or weight loss require evaluation and supportive care optimization.
  • Significant transaminase elevation, jaundice or signs of hepatotoxicity require oncology evaluation.
  • Multidisciplinary care including medical oncology, breast surgery and palliative care optimizes outcomes.

Treatment Methods

01
Elacestrant 345 mg orally daily continuous dosing represents standard regimen taken with food.
02
Antiemetic prophylaxis with serotonin antagonists or olanzapine before dosing reduces nausea.
03
Liquid biopsy ESR1 testing at progression on prior endocrine therapy identifies treatment candidates.
04
Bone health management with calcium, vitamin D supplementation, baseline DEXA and bisphosphonate when indicated.
05
Comprehensive supportive care including symptom management, nutrition support, drug interaction review and patient education supports successful long-term therapy as biomarker-driven approach for ESR1-mutated metastatic breast cancer.

Which Department to Visit?

You can visit our Onkoloji department for these complaints. Our specialist physicians will create the most suitable treatment plan for you.

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Health Disclaimer: The information on this page is prepared for general informational purposes only. It does not replace medical diagnosis and treatment. Please consult your physician for your complaints. Saygı Hospital does not accept responsibility for actions taken based on the information on this page.