CK-103

CK-103 is an orally bioavailable, small-molecule inhibitor of the Bromodomain and Extra-Terminal (BET) family of proteins, with specific activity against BRD4. Developed initially by Jubilant Biosys, the compound was licensed to Checkpoint Therapeutics in 2016 to expand its portfolio of targeted oncology agents. Under a subsequent sublicense agreement, TG Therapeutics is responsible for the development and commercialization of CK-103 in hematological malignancies, while Checkpoint Therapeutics retains the rights for solid tumor indications. The drug functions as an epigenetic modulator, inhibiting the binding of BET proteins to acetylated lysine residues on histones, thereby suppressing the expression of oncogenes such as c-Myc and Bcl-2 that drive tumor cell proliferation and survival.