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Hormone Therapy in Breast and Prostate Cancer pp 133–159Cite as

Preclinical Studies of Raloxifene and Related Compounds

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Abstract

The development of raloxifene (also know as keoxifene) for clinical use was based on a series of preclinical studies that demonstrated it has a highly desirable tissue-specific activity. Results indicated that the therapeutic effects of raloxifene (LY138481 HCl; LY156758) mimicked some of those of estrogen in ovariectomized animals by reducing bone loss and lowering serum cholesterol levels. Conversely, in mammary and uterine tissue, raloxifene acted as an antiestrogen and inhibited estrogen stimulation without inherent agonist activity (Fig. 1). Raloxifene was originally synthesized by Jones, who was looking for an antiestrogen with strong receptor binding (1). Jones hoped to produce a structure that would combine some features of the estradiol molecule with novel modifications to affect a potent estrogen receptor (ER) antagonist.

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Authors and Affiliations

  1. Department of Carcinogenesis, Science Park Research Division, The University of Texas M.D. Anderson Cancer Center, Smithville, TX

    Robin Fuchs-Young

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  1. Lombardi Comprehensive Cancer Center, Georgetown University, 3970 Reservoir Rd. NW Research Bldg. E501, Washington, DC, 20057, USA

    V. Craig Jordan

  2. AstraZeneca Pharmaceuticals Zeneca Pharmaceutical, Alderly Park, Alderly House, Macclesfield, SK 10 4TF, UK

    Barrington J.A. Furr

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Fuchs-Young, R. (2009). Preclinical Studies of Raloxifene and Related Compounds. In: Jordan, V.C., Furr, B.J. (eds) Hormone Therapy in Breast and Prostate Cancer. Cancer Drug Discovery and Development. Humana Press. https://doi.org/10.1007/978-1-59259-152-7_6

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