Elacestrant

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, as detected by an FDA-authorized test, with disease progression following at least one line of endocrine therapy. ORSERDU is an estrogen receptor antagonist indicated for: treatment of postmenopausal women or adult men, with ER-positive, HER2-negative, ESR1 -mutated advanced or metastatic breast cancer, as detected by an FDA-authorized test, 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 (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. Elacestrant demonstrated in vitro and in vivo antitumor activity including in ER+ HER2- breast cancer models resistant to fulvestrant and cyclin-dependent kinase 4/6 inhibitors and those harboring estrogen receptor 1 gene ( ESR1 ) mutations.

Select patients for treatment with ORSERDU based on the presence of ESR1 mutations. The recommended dosage of ORSERDU is one 345 mg tablet taken orally, once daily, with food. Dose interruption, reduction, or permanent discontinuation may be required due to adverse reactions.

None. None

Dyslipidemia: ORSERDU may cause hypercholesterolemia and hypertriglyceridemia. Monitor lipid profile prior to starting treatment and periodically thereafter. Embryo-Fetal Toxicity: ORSERDU can cause fetal harm. Advise of the potential risk to a fetus and to use effective contraception.

The following clinically significant adverse reactions are described elsewhere in the labeling: Dyslipidemia 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.

Strong and Moderate CYP3A4 Inducers: Avoid concomitant use. Strong and Moderate CYP3A4 Inhibitors: Avoid concomitant use. Effect of Other Drugs on ORSERDU Strong and Moderate CYP3A4 Inhibitors Avoid concomitant use of strong or moderate CYP3A inhibitors with ORSERDU. Elacestrant is a CYP3A4 substrate. Concomitant use of a strong or moderate CYP3A4 inhibitor increase elacestrant exposure, which may increase the risk of adverse reactions of ORSERDU. Strong and Moderate CYP3A4 Inducers Avoid concomitant use of strong or moderate CYP3A inducers with ORSERDU. Concomitant use of a strong or moderate CYP3A4 inducer decreases elacestrant exposure, which may decrease effectiveness of ORSERDU.

Store at 20°C to 25°C (68°F to 77°F). Excursions permitted from 15°C to 30°C (59°F to 86°F).