The Lambert et al article "Targeting Transcription Factors for Cancer Treatment" is a great overview of transcription factor drug targets for cancer, as the title of the article implies. It covers a lot! Bromodomain containing BET proteins are mentioned a few times but are not thoroughly discussed. Since this article is actually more relevant to Zenith, I will post this reply and link to article over on the Zenith board. Thanks to rndtbl over on Investor Village for originally posting.

https://www.ncbi.nlm.nih.gov/pubmed/29921764

The article mentions a few pan-BET inhibitors that I am familiar with: JQ1, OTX-015 (MK-8628), IBET-762 (GSK525762), CPI-0610. I had to look up GW841819X, which is an early generation pan-BET inhibitor based on a triazolodiazepine scaffold including similar to IBET-762 and JQ1. The article also mentions a couple of BET inhibitors (MS436 and the iridium based inhibitor 1a) that are in the "development stages" that I have never heard of.

Exemplifying the lack of BET inhibitor focus in the article, I don't see any mention of many clinical stage pan-BET inhibitors including ZEN-3694 (Zenith), ABBV-075 (Abbvie), GS-5829 (Gilead), INCB054329 and INCB057643 (Incyte), R06870810/TEN-010 (Hoffman LaRoche), FT-1101 (Forma Therapeutics), PLX51107 (Plexxicon), BMS-986158 (BMS), and a few others.

Although the article mentions RVX-208, which is a bromodomain-2 selective BET inhibitor, this compound has never been presented as or disclosed as a cancer therapeutic. The only bromodomain-2 selective BET inhibitor being tested for oncology is Abbvie's ABBV-744, which just recently started Phase 1 for prostate cancer.

BearDownAZ