Detailed Description of Elacestrant

Elacestrant, an estrogen receptor antagonist developed by the Italian company Menarini, was first approved for marketing by the U.S. FDA on January 27, 2023. Subsequently, it has been approved in regions such as the European Union and the United Kingdom. Currently, although the first prescription for this drug has been issued in China, it has not yet been widely adopted nationwide.

Indications for Elacestrant

Breast cancer

It is indicated for the treatment of estrogen receptor (ER)-positive, human epidermal growth factor receptor 2 (HER2)-negative, and estrogen receptor 1 (ESR1)-mutated advanced or metastatic breast cancer in postmenopausal women or adult men with disease progression following at least one line of endocrine therapy.

Dosage and Administration of Elacestrant

Recommended Dosage

Take 345 mg of elacestrant once daily until disease progression or unacceptable toxicity occurs.

Administration Guidelines

Taking elacestrant with food can reduce the incidence of gastrointestinal reactions such as nausea and vomiting. Administer orally at the same time each day, swallowing the tablet whole (do not chew, crush, or split). If a tablet is found to be damaged, cracked, or otherwise physically compromised, avoid taking it.

Missed Dose Management

If a dose is missed by more than 6 hours or if vomiting occurs, skip the missed dose and take the next dose at the regularly scheduled time the following day.

Dose Adjustments for Elacestrant

Recommended Dose Reductions

(1) First dose reduction: Patients should take 258 mg of elacestrant (three 86 mg tablets) orally once daily.

(2) Second dose reduction: Patients should take 172 mg of elacestrant (two 86 mg tablets) orally once daily.

Dose Adjustments for Adverse Reactions

Grade 1: Continue at the current dose level without adjustment.

Grade 2: Consider temporarily interrupting treatment until symptoms improve to Grade 1 or baseline, then resume at the same dose level.

Grade 3: Interrupt treatment until symptoms improve to Grade 1 or baseline, then resume at the next lower dose level. If Grade 3 toxicity recurs, interrupt treatment again until recovery, then reduce by one dose level.

Grade 4: Interrupt treatment until symptoms improve to Grade 1 or baseline, then resume at a reduced dose level. If Grade 4 or intolerable adverse reactions recur, permanently discontinue elacestrant.

Due to space limitations, please refer to the drug's original prescribing information for detailed content. Specific medication instructions should be followed as directed by a physician.

Adverse Reactions to Elacestrant

Adverse reactions (≥10%)

Common adverse reactions to elacestrant 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 dyspepsia.

Due to space limitations, please refer to the drug's original prescribing information for detailed content. Specific medication instructions should be followed as directed by a physician.

Precautions for Elacestrant

Dyslipidemia

Clinical observations indicate that treatment with elacestrant may induce Grade 3-4 hypercholesterolemia and hypertriglyceridemia. Conduct baseline lipid panel testing before initiating treatment and perform regular monitoring during treatment (recommended every 4-6 weeks). If significant dyslipidemia occurs, consider initiating lipid-lowering therapy or adjusting the oncology treatment plan in accordance with NCCN guidelines.

Fetal/Neonatal Morbidity and Mortality

Based on animal study findings and the drug's mechanism of action, elacestrant may cause fetal harm when administered during pregnancy. Verify pregnancy status in females of reproductive potential before initiating treatment. Inform patients of the potential risk to a fetus if elacestrant is used during pregnancy. Elacestrant may impair fertility.