RVX-2135

RVX-2135 is an orally bioavailable small molecule inhibitor of the Bromodomain and Extra-Terminal (BET) family of proteins, specifically targeting BRD2, BRD3, and BRD4. Developed by Resverlogix, it acts as an epigenetic modulator by binding to the acetylated lysine-recognition pockets (bromodomains) of these proteins. This binding prevents BET proteins from associating with chromatin, thereby suppressing the transcription of key growth and survival genes, most notably the oncogenes c-MYC and BCL-2. Preclinical data presented at AACR 2013 demonstrated that RVX-2135 inhibits the proliferation of acute myeloid leukemia (AML) cells, induces apoptosis, and shows synergistic effects when combined with standard chemotherapy agents such as cytarabine and idarubicin.