Difference between revisions of "Elacestrant (Orserdu)"
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==Diseases for which it is established== | ==Diseases for which it is established== | ||
| − | + | *[[Breast cancer, ER-positive]] | |
==History of changes in FDA indication== | ==History of changes in FDA indication== | ||
Revision as of 16:28, 28 January 2023
Mechanism of action
From the NCI Drug Dictionary: An orally available, selective estrogen receptor degrader (SERD) and selective estrogen receptor modulator (SERM), with potential antineoplastic and estrogen-like activities. Upon oral administration of higher doses of elacestrant, this agent acts as a SERD, which binds to the estrogen receptor (ER) and induces a conformational change that results in the degradation of the receptor. This may inhibit the growth and survival of ER-expressing cancer cells. At lower doses of this agent, RAD1901 acts as a SERM and has estrogen-like effects in certain tissues, which can both reduce hot flashes and protect against bone loss. In addition, elacestrant is able to cross the blood-brain barrier (BBB).
Diseases for which it is established
History of changes in FDA indication
- 1/27/2023: Approved for postmenopausal women or adult men with ER-positive, HER2-negative, ESR1-mutated advanced or metastatic breast cancer with disease progression following at least one line of endocrine therapy. (Based on EMERALD)
Also known as
- Code name: RAD1901
- Brand name: Orserdu