Selective Estrogen Receptor Modulators (SERMs) comprise a class of therapeutic agents widely prescribed for
the prevention and treatment of breast cancer, osteoporosis and postmenopausal symptoms. SERMs are exemplified by
Tamoxifen (TAM), a molecule displaying pronounced activity that is mediated through its in vivo active metabolites (Z)-
4-hydroxytamoxifen and endoxifen. The extensive in vivo metabolism of SERMs along with their wide use as medications,
has led to the development of specific methods for the efficient separation and accurate identification of their parent
molecules and metabolites in biological fluids. For this purpose, Liquid Chromatography (LC) is considered the most efficient
separation technique, especially when combined with mass spectrometry in simple (LC-MS) and/or tandem mode
(LC-MS/MS), constituting the cutting edge analytical approach in terms of selectivity and sensitivity. This review intends
to account the major recent advances on the LC-MS determination of SERMs and metabolites in biological fluids, a subject
not reviewed to date with the exception of TAM which was extensively reviewed on 2010, consequencing the inclusion
of only very recent reports on TAM assessments.
Keywords: Bioanalysis, biological fluids, endoxifen, extraction, HPLC, LC-MS, LC-MS/MS, mass spectrometry, metabolites,
MRM transitions, precipitation, raloxifene, SERMs, solid phase, tamoxifen.
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