Elacestrant dihydrochloride

Elacestrant dihydrochloride, also known as RAD1901 dihydrochloride, is the salt form of an orally active selective estrogen receptor degrader. It antagonizes estrogen receptor-alpha signaling and promotes proteasomal loss of the receptor, reducing the receptor population available to sustain estrogen-dependent transcription. These complementary actions underpin its use in research on ER-positive breast cancer and endocrine resistance.

The dihydrochloride is the drug-substance form used in oral elacestrant tablets. Its salt identity distinguishes it from the free base when converting material quantities to an elacestrant-equivalent amount. The unformulated drug substance supplies the active component for tablet-development and laboratory studies. Its defined receptor-targeting mechanism also supports comparison with other endocrine agents in cell-based studies.

Typical Applications

• Oral elacestrant tablet development: Used as the active ingredient in formulation work involving excipient compatibility, tablet manufacture, dissolution and stability, with drug content expressed on the appropriate elacestrant-equivalent basis.
• Estrogen-receptor signaling studies: Used in ER-positive breast-cancer models to examine receptor abundance, estrogen-responsive transcription and proliferation following receptor antagonism and degradation.
• Endocrine-resistance research: Used in models with ESR1 mutations or resistance to endocrine agents to investigate sensitivity to receptor degradation and responses to experimental treatment combinations.

Specifications

Specifications describe the standard grade. Tolerance, test method and documentation package are confirmed per order.