lgd-3303 and Osteoporosis

Osteoporosis is a common disease in which the risk of fracture increases due to decreased bone mass and qualitative skeletal changes. Selective androgen receptor modulators (SARMs) are agonists with tissue selectivity, which act as partial or weak androgen receptor (AR) agonists in androgenic tissues, but mainly as complete AR agonists in synthetic metabolic tissues. In the recent 20 years, many scaffolds of SARMs have been reported, among which several molecules are promising and are undergoing clinical trial evaluation. However, it is still a challenge to discover SARMs with high activity and reduced side effects. In this review, not only are structure of SARMs reported in the literatures systematically collected and classified but also the structure-activity relationships (SAR) are systematically summarized. Furthermore, the advances in SARMs as potential treatment for osteoporosis are also updated.

Topics: Androgen Antagonists; Androgens; Humans; Osteoporosis; Receptors, Androgen; Structure-Activity Relationship

Androgen, one of the sex steroid hormones shows various biological activities on the corresponding various tissues. Many efforts to produce novel drug materials maintaining a desired biological activity with an adequate tissue selectivity, which is so-called selective androgen receptor modulators (SARMs) , are being performed. As one of such efforts, studies on SARMs against bone tissues which possess a significant potential to stimulate a bone formation with reducing undesirable androgenic virilizing activities are in progress all over the world. This review focuses on the research and development activities of such SARMs and discuses their usefulness for the treatment of osteoporosis.

Topics: Acetamides; Amides; Aminophenols; Androgens; Anilides; Animals; Drug Design; Female; Humans; Male; Osteogenesis; Osteoporosis; Pyrroles; Pyrrolidines; Quinolones; Receptors, Androgen