Journal of Bone and Mineral Metabolism

, Volume 14, Issue 1, pp 1–9 | Cite as

A pharmacological review of raloxifene

  • Henry U. Bryant
  • Andrew L. Glasebrook
  • Na N. Yang
  • Masahiko Sato
Review Article


In view of its highly tissue-selective pharmacological properties (i.e., relatively pure antagonist in reproductive tissue with minimal agonist effects to nearly full agonist properties in bone and on cholesterol metabolism), terms used to define compounds with slightly related pharmacology (i.e., antiestrogen, partial estrogen agonist) do not adequately describe raloxifene's activity. Thus, raloxifene is distinct from agents such as tamoxifen (which does stimulate the uterus), or frank estrogen (which do not sufficiently antagonize estrogen's agonistic effects in reproductive tissue). In this regard, raloxifene and its pyrrolidine analogue, LY117018, (81) are the first representatives of a novel class of pharmacological agents, which we have termed “selective estrogen receptor modulator” (SERM). While we now have considerable evidence to distinguish estrogen recepto-mediated effects on bone from those on reproductive tissue, the precise mechanism for this tissue-specific mechanism remains an active area of investigation. Clearly, many important issues remain to be explored.

Key words

estrogen raloxifene bone uterus breast cancer cholesterol 


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Copyright information

© Springer-Verlag 1996

Authors and Affiliations

  • Henry U. Bryant
    • 1
  • Andrew L. Glasebrook
    • 1
  • Na N. Yang
    • 1
  • Masahiko Sato
    • 1
  1. 1.Endocrine Research DivisionLilly Corporate Center, Eli Lilly and Co.IndianapolisUSA

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