ABBV-744 is a selective bromodomain and extra-terminal (BET) inhibitor that preferentially bind to the 2nd bromodomains (BD) than the 1st BD pf BET family proteins (i.e., BRD2. BRD3. BRD4) [1]. This selective targeting of BD2 subsets of the BET bromodomain abolished the broad antiproliferative activities for previous generation pan BET inhibitors, and only display antiproliferative activities in a limited number of cancer cell lines, including acute myeloid leukaemia and prostate cancer that expressed the full-length androgen receptor (AR) [2]. Improved tolerability is expected due to less impact on global transcription [3].

ABBV-744 is a selective bromodomain and extra-terminal (BET) inhibitor that preferentially bind to the 2nd bromodomains (BD) than the 1st BD pf BET family proteins (i.e., BRD2. BRD3. BRD4) [1]. This selective targeting of BD2 subsets of the BET bromodomain abolished the broad antiproliferative activities for previous generation pan BET inhibitors, and only display antiproliferative activities in a limited number of cancer cell lines, including acute myeloid leukaemia and prostate cancer that expressed the full-length androgen receptor (AR) [2]. Improved tolerability is expected due to less impact on global transcription [3].