NCIt definition : The tartrate salt form of lasofoxifene, 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.;
Semantic type(s)