pharmacopeia
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/api/v1/drug/elacestrant

Mechanism of action

Sourced from openFDA

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

Breast Cancer Resistance ProteinEstrogen ReceptorP-Glycoprotein

Indications

Sourced from openFDA
  • ORSERDU is indicated for the treatment of postmenopausal women or adult men with estrogen receptor (ER)-positive, human epidermal growth factor receptor 2 (HER2)‑negative, ESR1 -mutated advanced or metastatic breast cancer with disease progression following at least one line of endocrine therapy.ICD-10: C50.919

Contraindications

Sourced from openFDA
  • None.contraindicated

Dosage & administration

Sourced from openFDA

Select patients for treatment with ORSERDU based on the presence of ESR1 mutations. ( 2.1 ) The recommended dosage of ORSERDU is one 345 mg tablet taken orally, once daily, with food ( 2.2 ) Dose interruption, reduction, or permanent discontinuation may be required due to adverse reactions. ( 2.3 ) 2.1 Patient Selection Select patients for treatment of ER-positive, HER2-negative advanced or metastatic breast cancer with ORSERDU based on the presence of ESR1 mutation(s) in plasma specimen using an FDA-approved test [see Indications and Usage ( 1 ) and Clinical Studies ( 14 )] . Information on FDA-approved tests for detection of ESR1 mutations in breast cancer is available at: http://www.fda.gov/CompanionDiagnostics. 2.2 Recommended Dosage The recommended dosage of ORSERDU is 345 mg taken orally with food once daily until disease progression or unacceptable toxicity occurs. Take ORSERDU at approximately the same time each day. Take with food to reduce nausea and vomiting [see Adverse Reactions ( 6.1 )] . Swallow ORSERDU tablet(s) whole. Do not chew, crush, or split prior to swallowing. Do not take any ORSERDU tablets that are broken, cracked, or that look damaged. 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.

Warnings & precautions

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Dyslipidemia: ORSERDU may cause hypercholesterolemia and hypertriglyceridemia. Monitor lipid profile prior to starting treatment and periodically thereafter. ( 5.1 ) Embryo-Fetal Toxicity: ORSERDU can cause fetal harm. Advise of the potential risk to a fetus and to use effective contraception. ( 5.2 , 8.1 , 8.3 ) 5.1 Dyslipidemia Hypercholesterolemia and hypertriglyceridemia occurred in patients taking ORSERDU at an incidence of 30% and 27%, respectively. The incidence of Grade 3 and 4 hypercholesterolemia and hypertriglyceridemia were 0.9% and 2.2%, respectively [see Adverse Reactions ( 6.1 )] . Monitor lipid profile prior to starting and periodically while taking ORSERDU. 5.2 Embryo-Fetal Toxicity Based on findings in animals and its mechanism of action, ORSERDU can cause fetal harm when administered to a pregnant woman. Administration of elacestrant to pregnant rats resulted in adverse developmental outcomes, including embryo-fetal mortality and structural abnormalities, at maternal exposures below the recommended dose based on area under the curve (AUC). Advise pregnant women and females of reproductive potential of the potential risk to a fetus. Advise females of reproductive potential to use effective contraception during treatment with ORSERDU and for 1 week after the last dose. Advise male patients with female partners of reproductive potential to use effective contraception during treatment with ORSERDU and for 1 week after the last dose [see Use in Specific Populations ( 8.1 , 8.3 ) and Clinical Pharmacology ( 12.1 )] .

Adverse reactions

Sourced from openFDA

The following clinically significant adverse reactions are described elsewhere in the labeling: Dyslipidemia [see Warnings and Precautions ( 5.1 )] The most common (>10%) adverse reactions, including laboratory abnormalities, of ORSERDU were 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, and dyspepsia. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Stemline Therapeutics, Inc. at 1-877-332-7961 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. The safety of ORSERDU was evaluated in 467 patients with ER+/HER2- advanced breast cancer following CDK4/6 inhibitor therapy in EMERALD, a randomized, open-label, multicenter study [see Clinical Studies ( 14 )] . Patients received ORSERDU 345 mg orally once daily (n=237) or standard of care (SOC) consisting of fulvestrant or an aromatase inhibitor (n=230). Among patients who received ORSERDU, 22% were exposed for 6 months or longer and 9% were exposed for greater than one year. Serious adverse reactions occurred in 12% of patients who received ORSERDU.

Use in specific populations

Sourced from openFDA

Lactation : Advise not to breastfeed. ( 8.2 ) Hepatic impairment : Avoid use in patients with severe hepatic impairment (Child-Pugh C). Reduce the dosage for patients with moderate hepatic impairment (Child-Pugh B). ( 2.5 , 8.6 ) 8.1 Pregnancy Risk Summary Based on findings in animals and its mechanism of action, ORSERDU can cause fetal harm when administered to a pregnant woman [see Clinical Pharmacology ( 12.1 )] . There are no available human data on ORSERDU use in pregnant women to inform the drug-associated risk. In an animal reproduction study, oral administration of elacestrant to pregnant rats during organogenesis caused embryo-fetal mortality and structural abnormalities at maternal exposures below the recommended dose based on AUC (see Data ) . Advise pregnant women and females of reproductive potential of the potential risk to a fetus. The background risk of major birth defects and miscarriage for the indicated population is unknown. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2%-4% and 15%-20%, respectively.

Pharmacokinetics

Sourced from openFDA
Metabolism
The steady-state mean (%CV) maximum concentration (Cmax) of elacestrant is 119 ng/mL (43.6%) and the area under the concentration-time curve (AUC 0-24h ) is 2440 ng*h/mL (44.3%) after administration of the recommended dosage of 345 mg once daily. The C max and AUC of elacestrant increase more than proportionally over a dosage range from 43 mg to 862 mg once daily (0.125 to 2.5 times the approved recommended dosage).

Approval history

Sourced from openFDA
  • Jan 27, 2023NDANDA217639Stemline Therap

FAERS reports

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Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
7,058 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Nausea1,48821%
  2. 2Fatigue1,11016%
  3. 3Disease Progression78011%
  4. 4Vomiting6749.5%
  5. 5Diarrhoea5537.8%
  6. 6Death5147.3%
  7. 7Drug Ineffective4876.9%
  8. 8Constipation4025.7%
  9. 9Product Dose Omission Issue3735.3%
  10. 10Decreased Appetite3695.2%
  11. 11Pain3695.2%
  12. 12Arthralgia3334.7%
  13. 13Asthenia2423.4%
  14. 14Abdominal Discomfort2343.3%
  15. 15Dyspepsia2333.3%

Clinical trials

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The 10 most recently updated of 38 ClinicalTrials.gov registrations naming Elacestrant as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Frequently asked questions

How does Elacestrant work?
Elacestrant is an estrogen receptor antagonist that binds to estrogen receptor-alpha (ERα). In ER-positive (ER+) HER2-negative (HER2-) breast cancer cells, elacestrant inhibited 17β-estradiol mediated cell proliferation at concentrations inducing degradation of ERα protein mediated through proteasomal pathway.
What is Elacestrant used for?
According to FDA labeling, Elacestrant carries indications including: ORSERDU is indicated for the treatment of postmenopausal women or adult men with estrogen receptor (ER)-positive, human epidermal growth factor receptor 2 (HER2)‑negative, ESR1 -mutated advanced or metastatic breast cancer with disease progression following at least one line of endocrine therapy.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Elacestrant?
Elacestrant is classified as Anti-estrogens, Estrogen Receptor Antagonist, Breast Cancer Resistance Protein Inhibitors, Estrogen Receptor Antagonists, P-Glycoprotein Inhibitors, Cellular Proliferation Alteration, Increased Protein Breakdown.
What are the brand names for Elacestrant?
Elacestrant is marketed under brand names including Orserdu.
What are the contraindications for Elacestrant?
Elacestrant labeling lists contraindications including: None.. Always consult the full prescribing information and a clinician.
Note. Data for elacestrant is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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