Dr. Taplin on the Mechanism of Action of Enzalutamide

Mary-Ellen Taplin, MD
Published Online: Thursday, Nov 29, 2012

Mary-Ellen Taplin, MD, associate professor of Medicine at Harvard Medical School and the Dana-Farber Cancer Institute, discusses the unique mechanism of action (MOA) for the androgen receptor antagonist enzalutamide (Xtandi; MDV3100), which was recently approved by the FDA for the treatment of patients with metastatic castration-resistant prostate cancer (mCRPC) who have previously received docetaxel.

The mechanism of action for the agent enzalumatide makes it a fantastic antiandrogen and sets it apart from older agents such as bicalutamide and nilutamide, explains Taplin. The agent is able to inhibit androgen receptor nuclear translocation rather than competing with androgen in the cytoplasm. Blocking entry into the nucleus prevents gene transcription and the activation of growth factors. Taplin believes this unique MOA is likely the reason that enzalutamide is efficacious in patients with mCRPC following chemotherapy.

The optimal way to sequence this agents is an important question that still needs answered. As a result, researchers are currently examining the administration of enzalutamide in early-stage prostate cancer and combination strategies.

Mary-Ellen Taplin, MD, associate professor of Medicine at Harvard Medical School and the Dana-Farber Cancer Institute, discusses the unique mechanism of action (MOA) for the androgen receptor antagonist enzalutamide (Xtandi; MDV3100), which was recently approved by the FDA for the treatment of patients with metastatic castration-resistant prostate cancer (mCRPC) who have previously received docetaxel.

The mechanism of action for the agent enzalumatide makes it a fantastic antiandrogen and sets it apart from older agents such as bicalutamide and nilutamide, explains Taplin. The agent is able to inhibit androgen receptor nuclear translocation rather than competing with androgen in the cytoplasm. Blocking entry into the nucleus prevents gene transcription and the activation of growth factors. Taplin believes this unique MOA is likely the reason that enzalutamide is efficacious in patients with mCRPC following chemotherapy.

The optimal way to sequence this agents is an important question that still needs answered. As a result, researchers are currently examining the administration of enzalutamide in early-stage prostate cancer and combination strategies.




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Online CME Activities
TitleExpiration DateCME Credits
Cancer Summaries and Commentaries™: Update from Chicago: Castrate Resistant Prostate Cancer and Advanced MelanomaAug 10, 20162.5
Clinical Vignette Series: 33rd Annual Chemotherapy Foundation Symposium: Innovative Cancer Therapy for Tomorrow®Feb 19, 20173.0