Selective androgen receptor modulators as function promoting therapies

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...

Discovery of diarylhydantoins as new selective androgen receptor modulators.

A novel selective androgen receptor modulator scaffold has been discovered through structural modifications of hydantoin antiandrogens. Several 4-(4-hydroxyphenyl)-N-arylhydantoins displayed partial agonism with nanomolar in vitro potency in transactivation experiments using androgen receptor (AR) transfected cells. In a standard castrated male rat model, several compounds showed good anabolic ...

Pharmacodynamics of selective androgen receptor modulators.

The present study aimed to identify selective androgen receptor modulators (SARMs) with in vivo pharmacological activity. We examined the in vitro and in vivo pharmacological activity of four chiral, nonsteroidal SARMs synthesized in our laboratories. In the in vitro assays, these compounds demonstrated moderate to high androgen receptor (AR) binding affinity, with K(i) values ranging from 4 to...

Pharmacodynamics of Selective Androgen Receptor Modulators ( SARMs )

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. ...