Galeterone (TOK-001), Our Newest Breakthrough PCa Drug to Prevent Testosterone Synthesis, Antagonizes Testosterone Binding to the AR and Degrades the AR Protein

Hi Guys,

A major breakthrough is about to be released that has received Fast Track designation from the U.S. Food and Drug Administration (FDA) to speed development as a potential treatment of CRPC.

ARMOR (Androgen Receptor Modulation Optimized for Response) is Tokai’s clinical development program for the evaluation of galeterone (TOK-001) in patients with castration-resistant prostate cancer (CRPC).  Galeterone (TOK-001) is a first-in-class, multi-targeted, small molecule, oral drug for the treatment of castration-resistant prostate cancer (CRPC) that disrupts androgen receptor (AR) signaling, the key driver of CRPC, via a novel triple mechanism of action. Preclinical studies have shown that galeterone selectively inhibits CYP17 lyase to prevent testosterone synthesis, antagonizes testosterone binding to the AR and degrades the AR protein. Galeterone is currently being evaluated in a Phase 2 study in patients with CRPC.

Phase 2 clinical trial evaluating the efficacy and safety of a new oral formulation of galeterone in four distinct populations of CRPC patients: 1) metastatic treatment-naïve patients; 2) non-metastatic treatment-naïve patients; 3) patients who have progressed while taking Zytiga® (abiraterone acetate) and 4) patients who have progressed while taking  Xtandi® (enzalutamide). The primary endpoints of the study are reduction in prostate-specific antigen (PSA) levels and safety. The secondary endpoints include tumor responses by RECIST, levels of circulating tumor cells and markers of CYP17 lyase inhibition and AR modulation. Patients who respond to therapy will have the opportunity to continue treatment in an extension arm of the trial. ARMOR2 is being conducted globally at leading prostate cancer treatment centers.

Galeterone was reformulated prior to the initiation of the ARMOR2 clinical trial in order to increase the drug exposure and mitigate the effect of food on oral bioavailability. The new formulation has been shown to be unaffected by diet, and therefore can be taken with or without food.

Full Story: TOK-001, THE “NEW” PROSTATE CANCER INFOLINK

Full Story: (TOK-001) By ARMOR (Androgen Receptor

“Make Every Day Count” !

Craig Becker

The New Denver Men’s Club

Blog: https://newdenvermensclub.wordpress.com/
“Men Fighting Cancer To Win”

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One thought on “Galeterone (TOK-001), Our Newest Breakthrough PCa Drug to Prevent Testosterone Synthesis, Antagonizes Testosterone Binding to the AR and Degrades the AR Protein

  1. good post this drug has been under development for about 4 years. I first saw a poster on its activity in cell lines about that time. Hopefully there will be no glitches, and on paper it might be better than enzalutamide or abiraterone. However, some mutations in the AR can be predicted that would lead to resistance, and there are of course all kinds of pathways that prostate cancer uses that do not involve the AR that are lurking to cause resistance. Mostly, however, one would hope (probably in a futile way) that Tokai would charge <6000/month if the drug achieves approval.

    From: New Denver Men's Club <comment-reply@wordpress.com> Reply-To: New Denver Men’s Club <comment+_jur67cuurt7qw2xxpj_zt@comment.wordpress.com> Date: Thursday, January 2, 2014 at 8:34 AM To: Mike Glode <Mike.Glode@ucdenver.edu> Subject: [New post] Galeterone (TOK-001), Our Newest Breakthrough PCa Drug to Prevent Testosterone Synthesis, Antagonizes Testosterone Binding to the AR and Degrades the AR Protein

    recbeck posted: “Hi Guys, A major breakthrough is about to be released that has received Fast Track designation from the U.S. Food and Drug Administration (FDA) to speed development as a potential treatment of CRPC. ARMOR (Androgen Receptor Modulation Optimized for “

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