Future SERMs

Recently, leaders in the pharmaceutical industry have developed a list of desired properties for a fourth generation of SERMs (Table 2). In general, future SERMs must oppose endogenous hormone action in the breast and reproductive system while displaying full estrogenic effects in the cardiovasculature, bone and central nervous systems. Additional criteria are that fourth generation compounds possess superior bioavailability compared with existing SERMs and have... 

Finally, new hypotheses of treatment were recently published (Minakuchi et al. 1999 De Leo et al. 2001 Palomba et al. 2002b Shozu et al. 2003 Gainer et al. 2005 Spitz 2003). At present, only SERMs, i.e., raloxifene, seem to hold any real promise in terms of future development. 

In addition to the molecules included in Table 1, research in the field of ER modulators has given rise to other novel scaffolds, which may produce additional SERMs to address unmet medical needs in the not-so-distant future.3... 

Pharmacological management of breast cancer continues to make progress with advanced characterization techniques and the use of aromatase inhibitors and SERMs. Future generations of SERMs will need to be completely devoid of estrogenic activity to prevent the development of resistance, as is occurring with tamoxifen. 

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