Difference between revisions of "Elacestrant (Orserdu)"
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From the [https://www.cancer.gov/publications/dictionaries/cancer-drug/def/elacestrant 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). | From the [https://www.cancer.gov/publications/dictionaries/cancer-drug/def/elacestrant 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== |
− | + | *[[Breast cancer, ER-positive]] | |
− | |||
+ | ==History of changes in FDA indication== | ||
+ | *2023-01-27: 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)'' | ||
+ | ==History of changes in EMA indication== | ||
+ | *2023-09-20: Initial marketing authorization as Orserdu. Orserdu monotherapy is indicated for the treatment of postmenopausal women, and men, with estrogen receptor (ER)‑positive, HER2-negative, locally advanced or metastatic [[breast cancer]] with an activating ESR1 mutation who have disease progression following at least one line of endocrine therapy including a CDK 4/6 inhibitor. | ||
==Also known as== | ==Also known as== | ||
− | *'''Code name:''' | + | *'''Code name:''' RAD-1901 |
+ | *'''Brand name:''' Orserdu | ||
[[Category:Drugs]] | [[Category:Drugs]] | ||
[[Category:Intramuscular medications]] | [[Category:Intramuscular medications]] | ||
+ | [[Category:Mutation-specific medications]] | ||
[[Category:Estrogen receptor inhibitors]] | [[Category:Estrogen receptor inhibitors]] | ||
− | [[Category:Breast cancer medications | + | [[Category:Breast cancer medications]] |
− | [[Category: | + | [[Category:FDA approved in 2023]] |
+ | [[Category:EMA approved in 2023]] |
Latest revision as of 12:24, 1 October 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
- 2023-01-27: 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)
History of changes in EMA indication
- 2023-09-20: Initial marketing authorization as Orserdu. Orserdu monotherapy is indicated for the treatment of postmenopausal women, and men, with estrogen receptor (ER)‑positive, HER2-negative, locally advanced or metastatic breast cancer with an activating ESR1 mutation who have disease progression following at least one line of endocrine therapy including a CDK 4/6 inhibitor.
Also known as
- Code name: RAD-1901
- Brand name: Orserdu