TG-1601 is a novel small molecule that binds with high affinity and selectivity to the epigenetic BET (bromodomain and extra-terminal) family of bromodomain-containing proteins and inhibits their binding to chromatin. BET proteins function as molecular adaptors, or scaffolds, to recruit the machinery necessary for activating gene transcription, e.g. the transcription of two critical oncogenes such as MYC and BCL-2. MYC over-expression appears to be particularly important for the viability of hematologic malignancies. By resetting the genome in tumor cells and reducing MYC levels, TG-1601 can increase the sensitivity of tumors to chemotherapy or specific standard of care, including Immuno-therapies like PD-L1 or CD-20 antibodies.

TG-1601 is currently in pre-clinical development and is being tested in various IND-enabling studies.