Wednesday 24 January 2018

Increased expression of androgen receptor (AR) in GBM. Enzalutamide (androgen receptor inhibitor)

SNO 2016 abstract: CSIG-13 ANDROGEN RECEPTOR IS INVOLVED IN GLIOBLASTOMA AND PRESENTS A POTENTIAL THERAPEUTIC TARGET

SNO 2017 abstract: CSIG-24. ANDROGEN RECEPTOR IS A POTENTIAL THERAPEUTIC TARGET IN GLIOBLASTOMA

 "Enzalutamide given orally (20 mg/kg three time per week) to nude mice bearing human gliomas (U78MG) resulted in reduction of 72% in tumor volume (p=0.0027) as compared to mice treated with vehicle. We hope that the results of this study together with continued laboratory efforts will lead to a new approach for the treatment of human glioblastoma."

Enzalutamide is an androgen receptor inhibitor approved by the FDA in 2012 for treatment of prostate cancer.
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2 comments:

  1. Semyon25 January 2018 at 03:46

    Is it interesting,
    crosses the Enzalutamide blood-brain barrier?

    ReplyDelete
    Replies
    1. Stephen W25 January 2018 at 16:41

      "Cross blood brain barrier? Yes, both enzalutamide and the active
      metabolite"
      https://www.cancercareontario.ca/sites/ccocancercare/files/enzalutamide.pdf

      "Enzalutamide also has the ability to cross the blood–brain barrier, which although increasing the risk of seizure, makes it a suitable option when epidural or meningeal metastasis is present."
      https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4407758/

      Delete

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