BET bromodomain inhibitors—A novel epigenetic approach in castration-resistant prostate cancer

http://www.tandfonline.com/doi/full/10.4161/15384047.2014.962297?src=recsys

Although a bit dated (2014), this article does help explain a bit of background around how BET inhibitors are addressing this space, in particular JQ1. My thinking is that ZEN3694 is now getting to the stage where we are going to hear a bit more about its efficacy. It would be nice to understand how it compares to results that JQ1 achieved.

When we get to the next stage of this trial (used in combination with enzalutamide and/or abiraterone), I've got a suspicion that it might work as well or better that what we saw in JQ1. If that's the case, this could be huge.

DYODD and get familiar with this area of research. It could be something that is a real turning point in how cancers can be treated. When we see companies such as Gilead and Medivation (now Pfizer) really getting into this space, it is really exciting for me. If Zenith is seen as a player, there could be a lot of interest from other big pharmas to jump into the game at this stage. I can see the likes of Sanofi, AstraZeneca, Lilly and others all sniffing around not wanting to be left out.

There is a conference (ESMO) coming up Oct 7-11 in Copenhagen where Medivation will be presenting updates from their Phase 3 EMBARK study into prostate cancer using enzalutamide. Should be interesting and again focus attention on epigenetic mechanisms. Here's a link to their news release in case you're interested in reading further.

http://investors.medivation.com/releasedetail.cfm?ReleaseID=991187

One thing that I found interesting in the news release was the line "enzalutamide has been shown to competitively inhibit androgen binding to androgen receptors as well as inhibit androgen receptor nuclear translocation and interaction with DNA. The clinical significance of this MOA is unknown." Hmm. does that mean it works but they don't know why? Based on slides we've seen Zenith present in the past, it seems the Zenith folks are getting a lot better understanding of how some of this actually does work - thus the comment the DM often makes about having a significant lead in this arena.

Not sure if Zenith is participating in this conference (haven't seen anything on their site to suggest they are).

masila