FT-1101

FT-1101 is an orally bioavailable, potent and selective small molecule inhibitor of the Bromodomain and Extra-Terminal (BET) family of proteins. It acts as a pan-inhibitor targeting all four BET family members (Bromodomain-containing protein 2, Bromodomain-containing protein 3, Bromodomain-containing protein 4, and Bromodomain testis-specific protein), which are epigenetic regulators involved in gene expression. By inhibiting these proteins through binding to their acetylated lysine recognition motifs in bromodomain sites, FT-1101 modulates gene transcription with potential antineoplastic activity. The drug has been investigated primarily for the treatment of relapsed or refractory hematologic malignancies such as acute myeloid leukemia (AML), high-risk myelodysplastic syndrome (MDS), and non-Hodgkin lymphoma (NHL). Development was led by FORMA Therapeutics under a collaboration with Celgene[1][2][4][5][8].