Elacestrant

Elacestrant is a first-in-class, orally bioavailable selective estrogen receptor degrader (SERD) approved for the treatment of ER-positive, HER2-negative advanced or metastatic breast cancer. As a small molecule drug, Elacestrant binds to the estrogen receptor and causes its degradation, leading to a decrease in estrogen signaling. Elacestrant induces the degradation of ER, inhibits ER-mediated signaling and growth of ER-positive breast cancer cell lines in vitro and in vivo, and significantly inhibits tumor growth in multiple patient-derived xenograft (PDX) models. For pharmaceutical quality control and analytical development, Elacestrant serves as an essential reference standard for impurity profiling, method validation, and stability studies. Elacestrant is also a critical reference material for ANDA filings, supporting the development of generic versions of this important endocrine therapy.

 

Product Parameters

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Parameter	Specification
Product Name	Elacestrant
CAS Number	722533-56-4
Molecular Formula	C₃₀H₃₈N₂O₂
Molecular Weight	458.63 g/mol
Appearance	White solid
pKa	10.36±0.40
Density	1.111 ± 0.06 g/cm³ (predicted)
Boiling Point	609.5 ± 55.0 °C at 760 mmHg

 

Oral Medication For Breast Cancer

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Orserdu (Elacestrant), an innovative selective estrogen receptor degerator (SERD) drug, was meticulously developed by Stemline Therapeutics in the United States. It is primarily indicated for the treatment of advanced or metastatic breast cancer that is estrogen receptor (ER)-positive, human epidermal growth factor receptor 2 (HER2)-negative, and harbors an estrogen receptor alpha (ESR1) gene mutation. On January 27,2023, Orserdu received formal approval for marketing from the U.S. Food and Drug Administration (FDA). Currently, Orserdu has not yet obtained approval for market authorization in China nor has it been included in the national medical insurance reimbursement list.

 

Mechanism Of Action

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Eirasquone (RAD-1901) is an estrogen receptor antagonist that binds to estrogen receptor α (ERα). In ER-positive (ER+) / HER2-negative (HER2-) breast cancer cells, irasquone exerts its antitumor effects by mediating the degradation of ERα protein via the proteasomal pathway at concentrations that inhibit 17β-estradiol-mediated cell proliferation. The drug demonstrates antitumor activity both in vitro and in vivo, including in ER+/HER2-breast cancer models resistant to fulvestrant and cyclin-dependent kinase 4/6 inhibitors (CDK4/6 inhibitors), as well as in models harboring estrogen receptor 1 (ESR1) mutations.

 

Synthetic Route

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Contact Us

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Interested in Elacestrant for your oncology API manufacturing campaign, impurity profiling program, or endocrine therapy research? Cosperpharm makes it easy. Get in touch with our team for pricing, documentation, or technical support—we're ready to assist.