Selective estrogen receptor modulators pharmacokinetics

Morello KC, Wurz GT, DeGregono MW. Pharmacokinetics of selective estrogen receptor modulators. Clinical Pharmacokinetics, 2003, 42 361-372. 

Mountfield, R.J., Kiehr, B. and John, B.A. (2000) Metabolism, disposition, excretion, and pharmacokinetics of levormeloxifene, a selective estrogen receptor modulator, in the rat. Drug Metabolism and Disposition, 28,... 

The clinical significance of the selective estrogen receptor modulators (SERMs) is well documented. The intensive research is currently directed at discovery of the ideal SERM , an agent that is antiestrogenic in breast and endometrial tissue, but pro-estrogenic in the vasculature and brain, which would be of use as a preventative in breast and uterine cancer and an alternate attractive HRT. Compound 1-(R) is a backup development candidate of the bisbenzopyran lead compound in our SERM program. This compound has shown promising preclinical profile with excellent pharmacokinetic properties. The identification and profiles of this novel SERM will be discussed. 

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