Minted: - / 5000

2757 Elacestrant
ced882a8ae21b90a8d508f39fcaf8a0c2a6a4ad5f5830a8ab6f28cba37961852

Properties

Background

Yellow
Bottle

Gray
Cap

Light blue
Syringe

Light blue
Bubbles
No
Drops
Yes
Label
-

Chemistry

Formula
C30H38N2O2
Carbon
30
Polarity
Neutral

Elacestrant (INN) (developmental code names RAD-1901, ER-306323) is a nonsteroidal combined selective estrogen receptor modulator (SERM) and selective estrogen receptor degrader (SERD) (described as a "SERM/SERD hybrid (SSH)") that was discovered by Eisai and is under development by Radius Health and Takeda for the treatment estrogen receptor (ER)-positive advanced breast cancer. Elacestrant has dose-dependent, tissue-selective estrogenic and antiestrogenic activities, with biphasic weak partial agonist activity at the ER at low doses and antagonist activity at higher doses. It shows agonistic activity on bone and antagonistic activity on breast and uterine tissues. Unlike the SERD fulvestrant, elacestrant is able to readily cross the blood-brain-barrier into the central nervous system, where it can target breast cancer metastases in the brain, and is orally bioavailable and does not require intramuscular injection.

From Wikipedia, the free encyclopedia. License: CC BY-SA.