Abstract

Raloxifene (Evista®, 4) is a selective estrogen receptor modulator that has estrogenic action on the estrogen receptors in bone and liver and anti-estrogenic effect on uterus and breasts. Raloxifene is used for the treatment and prevention of osteoporosis in postmenopausal women and for reduction in risk of invasive breast cancer. Raloxifene can be abused in sports because it counteracts the adverse effects of extensive use of anabolic androgenic steroids (gynaecomastia). It also increases testosterone concentration by stimulation of testosterone biosynthesis. Raloxifene is included in the list of prohibited substances and methods in sports of the World Anti-Doping Agency (WADA). According to WADA’S international standard for laboratories and the ISO 17025 standard, well-characterized reference compounds should be used for the identification of a prohibited substance, if available. As a part of this ongoing WADA-funded research project we synthesized three hydroxylated phase one raloxifene metabolites for doping analytical purposes. The synthesized metabolites were purified and fully characterized by chromatographic and spectroscopic methods. Einleitung