NCIt definition : A non-steroidal, naphthalene-derived, third-generation selective estrogen receptor
modulator (SERM) with potential antineoplastic and anti-osteoporotic activities. Upon
oral administration, lasofoxifene selectively binds to both estrogen receptor alpha
(ERalpha; ESR1) and estrogen receptor beta (ERbeta; ESR2) with high affinity and mimics
the effects of endogenous estradiol with varying agonist and antagonist effects in
ER-expressing tissues. Blockade of ERalpha by lasofoxifene may potentially inhibit
estrogen-dependent cancer cell proliferation in ER-expressing cancers. Lasofoxifene
may also bind to the certain mutant forms of ERalpha, including the Y537S ESR1 mutant,
making it potentially useful in the treatment of tumors that have acquired resistance
to other ER-targeting agents.;
UNII : 337G83N988;
InChIKey : GXESHMAMLJKROZ-IAPPQJPRSA-N;
CAS number : 180916-16-9; a href https://gsrs.ncats.nih.gov/ginas/app/beta/browse-substance?search 180916-16-9
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