Elacestrant is a non-steroidal estrogen receptor antagonist and selective estrogen receptor degrader (SERD). It acts on estrogen receptor alpha (ERα) and promotes receptor degradation, thereby reducing estrogen-receptor-mediated signaling. Elacestrant is an orally bioavailable small-molecule therapeutic used in the treatment of specific hormone receptor-positive breast cancer.
Elacestrant is associated with the development code RAD1901 and has the chemical formula C30H38N2O2, with a molecular weight of approximately 458.6 g/mol. The CAS Registry Number for elacestrant free base is 722533-56-4.
The pharmaceutical product Orserdu (elacestrant) contains the active ingredient in its dihydrochloride salt form. Elacestrant dihydrochloride has the CAS number 1349723-93-8, molecular formula C30H40Cl2N2O2, and molecular weight approximately 531.6 g/mol.
Elacestrant is particularly relevant to pharmaceutical development and oncology research because it provides an orally administered SERD approach for estrogen receptor-positive breast cancer. The FDA approved elacestrant in January 2023 for postmenopausal women or adult men with ER-positive, HER2-negative, ESR1-mutated advanced or metastatic breast cancer following progression after at least one line of endocrine therapy.
For pharmaceutical and research applications, Elacestrant API should be manufactured, tested, handled, packaged, and stored according to applicable quality standards and the approved product specification. Identity, purity, assay, related substances, residual solvents, water content, elemental impurities, and other applicable quality attributes should be controlled according to the relevant specification.
Elacestrant is primarily associated with oncology applications, particularly research and pharmaceutical development involving estrogen receptor-positive breast cancer. Its mechanism involves binding to estrogen receptor alpha and promoting degradation of the receptor, thereby reducing ER-mediated signaling.
| Parameter | Specification |
|---|---|
| Appearance | White to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |
| Loss on Drying | NMT 1.0% |
| Residue on Ignition | NMT 0.5% |
| Heavy Metals | NMT 20 ppm |
| pH (1% Solution) | 2.0 – 4.0 |
| Individual Impurity | NMT 0.5% |
| Total Impurities | NMT 1.0% |
| Water Content | NMT 1.0% |
| Melting Point | 168°C – 172°C |