CEP8983

CEP8983 is a small molecule inhibitor of poly(ADP-ribose) polymerase 1 (PARP-1) and PARP-2. Chemically identified as a 4-methoxy-carbazole derivative, it was originally developed by Cephalon (now Teva Pharmaceutical Industries). CEP8983 acts by inhibiting the repair of single-strand DNA breaks, which leads to the accumulation of double-strand breaks and subsequent apoptosis, particularly in cells with high PARP activity or DNA repair deficiencies (such as BRCA mutations). It is the active moiety of the orally bioavailable prodrug CEP-9722. Preclinical studies demonstrated its efficacy in various cancer models, including non-small cell lung cancer (NSCLC), mesothelioma, and ovarian cancer, where it showed chemosensitizing and cell death-inducing effects.

Other names

4-methoxy-carbazole derivative