Elacestrant

Elacestrant is a prescription medicine used for the treatment of breast cancer.

• Elacestrant is available under the following different brand names: Orserdu

Common side effects of Elacestrant include:

• flushing,  
• headache,
• dizziness,
• swelling,
• fast heartbeats, and
• upset stomach

Serious side effects of Elacestrant include:

• hives,
• difficulty breathing,
• swelling of the face, lips, tongue, or throat,
• lightheadedness,
• pounding heartbeats,
• fluttering in the chest,
• flushing (warmth, redness, or tingly feeling),
• tiredness,
• swelling,
• rapid weight gain, and
• shortness of breath

Rare side effects of Elacestrant include:

• none

Seek medical care or call 911 at once if you have the following serious side effects:

• Severe headache, confusion, slurred speech, arm or leg weakness, trouble walking, loss of coordination, feeling unsteady, very stiff muscles, high fever, profuse sweating, or tremors;
• Serious eye symptoms such as sudden vision loss, blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights;
• Serious heart symptoms include fast, irregular, or pounding heartbeats; fluttering in the chest; shortness of breath; sudden dizziness, lightheadedness, or passing out. 

This is not a complete list of side effects and other serious side effects or health problems that may occur because of the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may report side effects or health problems to FDA at 1-800-FDA-1088.

Adult and pediatric dosage

Tablet

• 86 mg
• 345 mg

Breast Cancer

Adult dosage

• 345 mg orally every day with food until disease progression or unacceptable toxicity

Dosage Considerations – Should be Given as Follows: 

• See “Dosages”

If your medical doctor is using this medicine to treat your pain, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider, or pharmacist first.

• Elacestrant has severe interactions with no other drugs.
• Elacestrant has serious interactions with at least 111 other drugs
• Elacestrant has moderate interactions with the following drugs:
  • atorvastatin
  • clonidine
  • colchicine
  • digoxin
  • irinotecan
  • methotrexate
  • sirolimus
  • tacrolimus
  • tazemetostat
  • temsirolimus
  • topotecan
  • ubrogepant
• Elacestrant has minor interactions with no other drugs.

This information does not contain all possible interactions or adverse effects. Visit the RxList Drug Interaction Checker for any drug interactions. Therefore, before using this product, tell your doctor or pharmacist about all your products. Keep a list of all your medications with you and share this information with your doctor and pharmacist. Check with your healthcare professional or doctor for additional medical advice, or if you have health questions or concerns.

Contraindications

• None

Effects of drug abuse

• None

Short-Term Effects

• See “What Are Side Effects Associated with Using Elacestrant?”

Long-Term Effects

• See “What Are Side Effects Associated with Using Elacestrant?”

Cautions

• Hypercholesterolemia and hypertriglyceridemia were reported; monitor lipid profile before initiating and periodically during treatment
• Based on findings in animals and its mechanism of action, elacestrant can cause fetal harm when administered to pregnant females
• Drug interaction overview
• Substrate of CYP3A4 (major), CYP2A6 (minor), and CYP2C9 (minor)
• Inhibitor of P-gp and BCRP
• Strong or moderate CYP3A4 inducers
  • Avoid coadministration
    • Strong or moderate CYP3A4 inducers decrease elacestrant systemic exposure, which may decrease the effectiveness
    • Strong or moderate CYP3A4 inhibitors
  • Avoid coadministration
    • Strong or moderate CYP3A4 inhibitors increase elacestrant systemic exposure, which may increase the risk of adverse effects
  • P-gp substrates
    • Modify dose and monitor
    • Reduce the dose of P-gp substrates per their prescribing information when minimal concentration changes may lead to serious or life-threatening adverse reactions
  • BCRP substrates
    • Modify dose and monitor
    • Reduce the dose of BCRP substrates per their prescribing information when minimal concentration changes may lead to serious or life-threatening adverse reactions

Pregnancy and Lactation

• Based on animal studies and its mechanism of action, elacestrant can cause fetal harm when administered to pregnant females
• Verify the pregnancy status of females of reproductive potential before initiating
• Contraception
  • Advise females of reproductive potential (including partners of men being treated with elacestrant) to use effective contraception during treatment and for 1 week after the last dose
• Infertility
  • Based on findings from animal studies, may impair fertility in females and males of reproductive potential
• Lactation
  • Data are unavailable on the presence of drugs in human milk, effects on milk production, or breastfed children
  • Advise lactating females to not breastfeed during treatment and for 1 week after the last dose