• Breast cancer

Orserdu Generic Name & Formulations

General Description

Elacestrant 86mg, 345mg; tabs.

Pharmacological Class

Estrogen receptor antagonist.

How Supplied


Generic Availability


Orserdu Indications


In postmenopausal women or adult men, with ER-positive, HER2-negative, ESR1-mutated advanced or metastatic breast cancer with disease progression following at least 1 line of endocrine therapy.

Orserdu Dosage and Administration


Select patients based on the presence of ESR1 mutation(s) in plasma specimen. Swallow whole. Take with food. 345mg once daily, until disease progression or unacceptable toxicity occurs. Moderate hepatic impairment (Child-Pugh B): 258mg once daily. Dose modifications for adverse reactions: see full labeling.


Not established.

Orserdu Contraindications

Not Applicable

Orserdu Boxed Warnings

Not Applicable

Orserdu Warnings/Precautions


Risk for dyslipidemia. Monitor lipid profile prior to initiation and periodically during treatment. Hepatic impairment (severe): avoid; (moderate): reduce dose. Embryo-fetal toxicity. Advise females of reproductive potential and males (w. female partners) to use effective contraception during and for 1 week after the last dose. Pregnancy: exclude status prior to initiation. Nursing mothers: not recommended (during and for 1 week after the last dose).

Orserdu Pharmacokinetics


The time to achieve peak plasma concentration (tmax) ranges from 1 to 4 hours. The elacestrant oral bioavailability is ~10%. 


The estimated apparent volume of distribution is 5800L. Plasma protein binding of elacestrant is >99% and independent of concentration.


Primarily metabolized by CYP3A4 and to a lesser extent by CYP2A6 and CYP2C9.


Fecal (82%), renal (7.5%). Half-life: 30 to 50 hours.

Orserdu Interactions


Potentiated by moderate or strong CYP3A4 inhibitors (eg, fluconazole, itraconazole); avoid. Antagonized by moderate or strong CYP3A4 inducers (eg, efavirenz, rifampin); avoid. Potentiates P-gp or BCRP substrates (eg, digoxin, rosuvastatin); reduce dose of substrates when concomitant Orserdu.

Orserdu Adverse Reactions

Adverse Reactions

Musculoskeletal pain, nausea, fatigue, vomiting, decreased appetite, diarrhea, headache, constipation, abdominal pain, hot flush, dyspepsia, lab abnormalities (increased cholesterol, increased AST/ALT, increased triglycerides, decreased hemoglobin,  decreased sodium, increased creatinine).

Orserdu Clinical Trials

See Literature

Orserdu Note

Not Applicable

Orserdu Patient Counseling

See Literature