Discovery of diarylhydantoins as new selective androgen receptor modulators.

Therapeutic androgen receptor ligands

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...

Selective androgen receptor modulators--prospects for emerging therapy in osteoporosis?

Significant medical need exists for new therapy that will increase bone strength beyond what is achieved with anticatabolic bone agents such as bisphosphonates. PTH has shown its ability to increase cancellous bone mass and has a positive impact in reducing the incidence of vertebral fractures. However, its high cost and mode of administration marginalize its widespread usage across the world. ...

Discovery and therapeutic promise of selective androgen receptor modulators.

Androgens are essential for male development and the maintenance of male secondary characteristics, such as bone mass, muscle mass, body composition, and spermatogenesis. The main disadvantages of steroidal androgens are their undesirable physicochemical and pharmacokinetic properties. The recent discovery of nonsteroidal selective androgen receptor modulators (SARMs) provides a promising alter...

Selective androgen receptor modulators (SARMs): a novel approach to androgen therapy for the new millennium.

Selective Androgen Receptor Modulators (SARMs) as Function Promoting Therapies

Purpose of review—The last decade has witnessed unprecedented discovery effort to develop selective androgen receptor modulators (SARMs) that improve physical function and bone health without adversely affecting the prostate and cardiovascular outcomes. This review describes the historical evolution, the rationale for SARM development, and the mechanisms of testosterone action and SARM selectiv...