Antiandrogens-Differences and Sequencing

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Raoul Concepcion, MD, and Michael Williams, MD, comment that bicalutamide is commonly utilized in the treatment of prostate cancer; however, clinicians may not be aware that although bicalutamide initially antagonizes the androgen receptor, it loses its ligand binding capacity over time, resulting in stimulation of the androgen receptor.

The antiandrogen enzalutamide inhibits androgen binding to androgen receptors and also inhibits androgen receptor nuclear translocation and interaction with DNA. Michael Williams, MD, comments that enzalutamide is a more potent androgen blocker compared with bicalutamide.

There are currently no prospective data to clarify which antiandrogen should be used first, second, and so forth, remarks Oliver Sartor, MD. He notes that bicalutamide and enzalutamide are both excellent agents, and either agent will most likely yield a good response when used as first-line therapy. With the availability of additional therapeutic options, Sartor comments that more data are needed regarding the optimal sequencing of therapies.

Since the filming of this video, enzalutamide gained approval as a treatment for men with metastatic castration-resistant prostate cancer prior to the administration of chemotherapy.