LBW242

LBW242 is a small-molecule Smac (Second mitochondria-derived activator of caspases) mimetic and an antagonist of Inhibitor of Apoptosis Proteins (IAPs), including XIAP, cIAP1, and cIAP2. Developed by Novartis, LBW242 mimics the N-terminal IAP-binding motif of Smac/DIABLO, allowing it to bind to the BIR (baculoviral IAP repeat) domains of IAPs. This binding prevents IAPs from inhibiting caspases-3, -7, and -9, thereby promoting the induction of apoptosis. LBW242 has demonstrated synergistic antitumor activity in various preclinical models when combined with conventional chemotherapy, radiotherapy, or other targeted agents like TRAIL and PKC412. It has been investigated for the treatment of multiple malignancies, including medulloblastoma, leukemia, multiple myeloma, and solid tumors such as ovarian and breast cancer.

Other names

Smac mimetic LBW242