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Dr. Shore on the Enzalutamide Mechanism of Action

Neal D. Shore, MD
Published: Thursday, Jun 28, 2012

Neal D. Shore, MD, Managing Partner, Atlantic Urology Clinics, Director, CPI, Carolina Urologic Research Center, discusses enzalutamide, a well tolerated oral therapy that showed a nearly five month improvement in survival in patients with advanced prostate cancer.

The mechanism of action for enzalutamide is threefold. It is a powerful, competitive binding at the level of the androgen receptor. It also prevents the translocation of the androgen receptor from cytoplasm to nucleus. Additionally, within the nucleus, there is inhibition of binding at the level of DNA, which Shore says presumably prevents further transcription of tumor genes.

Shore adds that he is excited about additional trials more proximal in the disease state continuum to see if they have benefits for patients earlier on as well.

Neal D. Shore, MD, Managing Partner, Atlantic Urology Clinics, Director, CPI, Carolina Urologic Research Center, discusses enzalutamide, a well tolerated oral therapy that showed a nearly five month improvement in survival in patients with advanced prostate cancer.

The mechanism of action for enzalutamide is threefold. It is a powerful, competitive binding at the level of the androgen receptor. It also prevents the translocation of the androgen receptor from cytoplasm to nucleus. Additionally, within the nucleus, there is inhibition of binding at the level of DNA, which Shore says presumably prevents further transcription of tumor genes.

Shore adds that he is excited about additional trials more proximal in the disease state continuum to see if they have benefits for patients earlier on as well.


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