Elacestrant

Elacestrant is an estrogen receptor antagonist that binds to estrogen receptor-alpha (ERα). In ER-positive breast cancer cells, elacestrant inhibits 17β-estradiol-mediated cell proliferation and induces degradation of ERα protein through the proteasomal pathway. The recommended dose is 345 mg taken orally with food once daily until disease progression or unacceptable toxicity. Common side effects include musculoskeletal pain, nausea, increased cholesterol, fatigue, vomiting, diarrhea, headache and constipation. Contraindicated in pregnancy. Avoid concomitant use with strong/moderate CYP3A4 inhibitors and inducers.

• ER-positive, HER2-negative, ESR1-mutated advanced or metastatic breast cancer with disease progression following at least one line of endocrine therapy

Elacestrant is an estrogen receptor antagonist that binds to estrogen receptor-alpha (ERα). In ER-positive HER2-negative breast cancer cells, elacestrant inhibited 17β-estradiol-mediated cell proliferation at concentrations inducing degradation of ERα protein mediated through proteasomal pathway.

Elacestrant binds to estrogen receptor-alpha (ERα) and induces degradation of ERα protein through the proteasomal pathway, inhibiting estrogen-mediated cell proliferation.

Adult Dose: 345 mg taken orally with food once daily until disease progression or unacceptable toxicity occurs. Take at approximately the same time each day. Take with food to reduce nausea and vomiting. Swallow tablets whole. Do not chew, crush, or split.

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

Oral tablet. Take once daily with food. Swallow whole. Do not chew, crush or split. Do not take damaged tablets.

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

Most Common (>10%) Adverse Reactions:

• Musculoskeletal pain
• Nausea
• Increased cholesterol
• Increased AST
• Increased triglycerides
• Fatigue
• Decreased hemoglobin
• Vomiting
• Increased ALT
• Decreased sodium
• Increased creatinine
• Decreased appetite
• Diarrhea
• Headache
• Constipation
• Abdominal pain
• Hot flush
• Dyspepsia

• Dyslipidemia: Hypercholesterolemia (30%) and hypertriglyceridemia (27%) occurred. Grade 3 and 4: 0.9% and 2.2%.
• Embryo-Fetal Toxicity: Advise pregnant women of potential risk to fetus.
• Females of reproductive potential should use effective contraception during treatment and for 1 week after last dose.
• Male patients with female partners of reproductive potential should use effective contraception during treatment and for 1 week after last dose.

• Pregnancy (can cause fetal harm)

Strong and Moderate CYP3A4 Inhibitors: Avoid concomitant use. Elacestrant is a CYP3A4 substrate. CYP3A4 inhibitors increase elacestrant exposure.

Strong and Moderate CYP3A4 Inducers: Avoid concomitant use. CYP3A4 inducers decrease elacestrant exposure and may reduce effectiveness.

No known food interactions.

Elacestrant can cause fetal harm when administered to a pregnant woman. No human data available on use in pregnancy.

No data on presence of elacestrant in human milk. Because of potential for serious adverse reactions in breastfed child, advise lactating women not to breastfeed during treatment and for 1 week after last dose.

Safety and efficacy in pediatric patients not established.

Limited information available regarding dose adjustment for elderly patients.

Renal impairment: Use with caution in kidney disease.

Hepatic impairment: Use with caution in liver disease.

Overdose may cause depression, nausea, vomiting, diarrhea, fatigue and electrolyte abnormalities. Provide symptomatic treatment.

Store below 30°C, away from light & moisture. Keep out of reach of children.

Elacestrant