Androgen receptor blockade is a cornerstone of treatment for prostate cancer. Despite castrate levels of testosterone, activation of the androgen receptor remains an important mediator of disease progression in the androgen "independentg" state. Thus, maximal blockade of androgen receptor signaling is a continual goal in the management of castration-resistant prostate cancer. In this review we will discuss how various aspects of androgen receptor signaling are being targeted for therapeutic development in castration-resistant prostate cancer. These include direct androgen receptor inhibitors, inhibitors of adrenal androgen synthesis, and a dual 5α-reductase isoenzyme inhibitor.
- Androgen receptor