BACKGROUND Raloxifene hydrochloride is a synthetic non-steroidal drug used for the prevention and treatment of post-menopausal osteoporosis. Pre-clinical and clinical data have shown that raloxifene may have a beneficial effect on leiomyomas. The aim of this prospective single-blind, randomized, placebo-controlled clinical trial was to evaluate the effectiveness of the addition of raloxifene to...

The endothelium is thought to play an important role in the genesis of atherosclerosis, and several lines of evidence suggest that the effect of an intervention on endothelial function might predict its involvement in coronary disease progression and in the rate of cardiovascular events. Estrogen has direct effects on the blood vessel wall, indicating that vascular endothelium may play a key ro...

Selective estrogen receptor modulators (SERMs) such as raloxifene have already shown beneficial effects on negative, positive and general psychopathology symptoms in postmenopausal women with schizophrenia. The purpose of the present investigation was to assess the efficacy of raloxifene as an adjuvant agent in the treatment of men with chronic schizophrenia in an 8-week double-blind and placeb...

OBJECTIVES To test the hypothesis that both raloxifene and estrogen would improve insulin sensitivity in postmenopausal women and that the magnitude of the effect would be similar for both drugs. DESIGN Placebo-controlled, double-blind, randomized study. SETTING The General Clinical Research Center of the University of Michigan Medical Center, a university hospital. PARTICIPANTS Forty-fou...

Introduction Selective estrogen receptor modulators (SERMs) such as raloxifene have been shown to be a safer and effective alternative to estrogen to preserve bone mass in the lumbar spine (1). The beneficial effects of raloxifene have been demonstrated in animal studies; predominantly in rats where inhibition of bone loss by raloxifene and estradiol-treated animals was similar (2-3) mediated t...

In the past several years, the concept of tissue-selective nuclear receptor ligands has emerged. This concept has come to fruition with estrogens, with the successful marketing of drugs such as raloxifene. The discovery of raloxifene and other selective estrogen receptor modulators (SERMs) has raised the possibility of generating selective compounds for other pathways, including androgens (that...

Caco-2 cell lysate, and intestinal and liver microsomes derived from female humans and rats were used to compare and contrast the metabolism and disposition of raloxifene. In Caco-2 cell lysate, raloxifene 6-beta-glucuronide (M1) was the main metabolite, although raloxifene 4'-beta-glucuronide (M2) was formed in comparable abundance (58% versus 42%). In rat liver and intestinal microsomes, M1 r...

The crystallization of the ligand-binding domain (LBD) of the estrogen receptor (ER) with 17beta-estradiol and raloxifene [A. M. Brzozowski et al., Nature (Lond.), 389: 753-758, 1997] now provides a molecular basis for the biological activity of complexes as either agonists or antagonists. It is well established that the critical structural feature of antiestrogens is a correctly positioned alk...

Selective estrogen receptor modulators (SERMs) are potentially useful in treating various endometrial disorders, including endometrial cancer, as they block some of the detrimental effects of estrogen. It remains unclear whether each SERM regulates a unique subset of genes and, if so, whether the combination of a SERM and 17beta-estradiol has an additive or synergistic effect on gene expression...

Chronic kidney disease (CKD) is associated with many adverse outcomes including mineral and bone disorders. The prevalence of fractures among patients with CKD exceeds that of the general population, due to impairments in bone quantity, bone quality, and abnormalities of neuromuscular function with profound effects on morbidity and mortality (1). Type 2 diabetes mellitus (T2DM), that is a major...