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Orserdu Generic Name & Formulations
Legal Class
General Description
Pharmacological Class
How Supplied
Tabs—30
Manufacturer
Generic Availability
NO
Mechanism of Action
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 demonstrated in vitro and in vivo antitumor activity including in ER-positive, HER2-negative breast cancer models resistant to fulvestrant and cyclin-dependent kinase 4/6 inhibitors and those harboring estrogen receptor 1 gene (ESR1) mutations.
Orserdu Indications
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
Adult
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.
Children
Not established.
Orserdu Contraindications
Not Applicable
Orserdu Boxed Warnings
Not Applicable
Orserdu Warnings/Precautions
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
Absorption
The time to achieve peak plasma concentration (tmax) ranges from 1 to 4 hours. The elacestrant oral bioavailability is ~10%.
Distribution
The estimated apparent volume of distribution is 5800L. Plasma protein binding of elacestrant is >99% and independent of concentration.
Elimination
Fecal (82%), renal (7.5%). Half-life: 30 to 50 hours.
Orserdu Interactions
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
Orserdu Note
Not Applicable
Orserdu Patient Counseling
Cost Savings Program
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