Update on Raloxifene: mechanism of action, clinical efficacy, side effects and contraindications

Raloxifene is the only SERM approved for long-term treatment in the prevention of
osteoporotic fractures and for the reduction of invasive breast cancer risk in
postmenopausal women. The demonstrated beneficial effects on bone and mammalian
tissue led clinical and molecular research to focus mainly on these organs, giving less
attention to all other systemic effects. The aim of this review is to evaluate all described
systemic effects of raloxifene, investigating its molecular and tissutal mechanism of
action.
A literature research was carried out in electronic databases MEDLINE, EMBASE
Sciencedirect and the Cochrane Library in interval time between 2000-2012.
Outcomes were considered in relation to positive/side effects concerning bone
metabolism, lipid metabolism, coagulation pattern, menopausal symptoms, breast cancer onset and endometrial cancer onset. Raloxifene acts as an estrogen agonist or
antagonist depending on the tissue. This feature is related to specific actions on at
least two distinct estrogen receptors, whose proportions vary according to tissue type.
Rraloxifene is an excellent drug for the treatment of osteoporosis and for the
prevention of estrogen receptors positive breast cancer since it guarantees an
excellent safety profile on the endometrium. Raloxifene is furthermore an effective
therapy in women with increased levels of plasma cholesterol.
Raloxifene treatment shifts the coagulation pattern towards pro-thrombosis and the
patients should be exhaustively informed about the risks associated with therapy.
Raloxifene does not show to affect memory and cognition. Finally, it is noteworthy that
quality-of-life studies demonstrated some favourable effects of Raloxifene.