Efficacy and Actions of Elacestrant
Elacestrant is an anti-tumor drug, belonging to the estrogen receptor antagonist class.
Efficacy and Actions of Elacestrant
Elacestrant is a selective estrogen receptor antagonist with significant anti-tumor activity against ER-positive, HER2-negative advanced or metastatic breast cancer harboring an ESR1 mutation, particularly suitable for cases resistant to prior endocrine therapy.
Indications for Elacestrant
Breast Cancer
Elacestrant is used to treat postmenopausal women or adult men with ER-positive, HER2-negative advanced or metastatic breast cancer harboring an estrogen receptor 1 (ESR1) mutation whose disease has progressed after at least one line of endocrine therapy.
Patients suitable for this treatment should be screened by confirming the presence of an ESR1 mutation through plasma sample testing using a test approved by the US FDA.
Elacestrant Dosage and Administration
1. Pre-treatment Screening
Before initiating elacestrant treatment, an estrogen receptor 1 (ESR1) mutation must be confirmed in a plasma sample using an FDA-approved diagnostic test.
Before initiating elacestrant treatment, the pregnancy status of women of childbearing potential must be verified.
Lipid levels should be monitored before initiating elacestrant treatment.
2. Patient Monitoring
Lipid levels should be monitored regularly during elacestrant treatment.
3. Administration
Administer orally once daily at approximately the same time each day. Take with food to reduce nausea and vomiting.
Swallow the tablet whole. Do not chew, crush, or break the tablet before swallowing. Do not take any broken, cracked, or seemingly damaged tablets.
4. Dosage
345 mg once daily.
5. Management of Missed Doses or Vomiting
If a dose is missed by more than 6 hours or vomiting occurs, skip the dose and take the next dose at the scheduled time the following day.
6. Dosage Adjustment for Toxicity
If adverse reactions occur, treatment may need to be temporarily interrupted, the dose reduced, and/or the drug permanently discontinued. Dosage adjustment may be necessary.
If a dose reduction to below 172 mg is subsequently required, irastran should be permanently discontinued.
7. Use in Special Populations
(1) Hepatic Impairment
Mild Hepatic Impairment: No dose adjustment required.
Moderate Hepatic Impairment: Reduce the dose to 258 mg once daily.
Severe Hepatic Impairment: Avoid use.
(2) Renal Impairment
No specific dosage recommendation.
(3) Elderly Patients
No specific dosage recommendation.
Precautions for Elacestrant
1. Dyslipidemia
Hypercholesterolemia and hypertriglyceridemia, including grade 3 and 4 events, have been reported. Lipid levels should be monitored regularly before and during elacestrant treatment.
2. Fetal/Neonatal Morbidity and Mortality
Elacestrant may cause harm to the fetus; animal studies have shown it to cause fetal structural abnormalities and embryo-fetal death.
The pregnancy status of women of childbearing potential should be verified before initiating elacestrant treatment. Patients should be informed of the potential risks to the fetus from elacestrant use during pregnancy.
This drug may impair fertility. Women of childbearing potential, and their partners, are advised to use effective contraception during treatment and for one week after the last dose.
Common adverse reactions of elacestrant
Adverse reactions (incidence ≥10%) include: musculoskeletal pain, nausea, vomiting, elevated cholesterol, elevated AST/ALT, elevated triglycerides, fatigue, decreased hemoglobin, decreased sodium, elevated creatinine, decreased appetite, diarrhea, headache, constipation, abdominal pain, hot flashes, and indigestion.
