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Antiandrogens-Differences and Sequencing

Panelists: Philippa J. Cheetham, MD, Stonybrook University;Raoul S. Concepcion, MD, Urology Associates, PC; Kenneth M. Kernen, MD, Michigan Urology;
Published: Tuesday, Oct 07, 2014

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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.

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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.
View Conference Coverage
Online CME Activities
TitleExpiration DateCME Credits
Clinical Vignette Series: 34th Annual Chemotherapy Foundation Symposium: Innovative Cancer Therapy for Tomorrow®Feb 28, 20182.0
Community Practice Connections™: Personalized Sequencing in Castration-Resistant Prostate Cancer: Bridging the Latest Evidence to the Bedside in Clinical ManagementAug 25, 20181.5
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