New selective estrogen and androgen receptor modulators

Research output: Contribution to journalReview articlepeer-review

29 Scopus citations


Purpose of review: The present review focuses on the most significant recent findings regarding selective estrogen receptor modulators (SERMs) and selective androgen receptor modulators (SARMs). SERMs, which interact with estrogen receptor-α and estrogen receptor-β in multiple tissues, continue to generate clinical interest in potential applications in as many disorders as the tissues in which the two known receptors are found. SARMs have been demonstrated to have fewer clinical applications to date, but continue to be investigated for use in multiple disorders in which androgen receptor modulation is likely to be important. Both types of compounds hold great promise for therapeutic use in multiple hormonal disorders involving tissue-specific effects mediated by estrogen or androgen receptors. Recent findings: Although SERMs have been available for clinical use for 50 years, recent investigation has focused on large randomized clinical trials for newer indications of older agents or smaller clinical trials of newer agents with improved clinical activity and reduced side effects in specific tissues. In particular, the large, prospective, randomized, controlled, multiyear Study of Tamoxifen and Raloxifene and Raloxifene Use in the Heart clinical trials have recently shown interesting similarities and differences between tamoxifen and raloxifene in estrogen-responsive tissues. Lasofoxifene and arzoxifene are two newer SERMs that have recently been demonstrated to improve bone mineral density and lower serum cholesterol values compared with older SERMs in smaller clinical trials. SARMs are a newer category of drug still being investigated mostly at the basic and preclinical level, with fewer clinical trials available for review. SARMs are currently being investigated mostly for use in prostate cancer at different stages but hold promise for multiple other applications. Summary Recent clinical trials indicate that SERMs are useful in treatment of disorders of bone and mineral metabolism and breast cancer and in reduction of cardiovascular risk factors. SARMs offer important benefits for management of prostate cancer at different stages, as well as other disorders.

Original languageEnglish (US)
Pages (from-to)374-379
Number of pages6
JournalCurrent opinion in rheumatology
Issue number4
StatePublished - Jul 2009


  • Breast cancer
  • Osteoporosis
  • Prostate cancer
  • Selective androgen receptor modulator
  • Selective estrogen receptor modulator

ASJC Scopus subject areas

  • Rheumatology


Dive into the research topics of 'New selective estrogen and androgen receptor modulators'. Together they form a unique fingerprint.

Cite this