BIIB028

BIIB028 is a small-molecule inhibitor of heat shock protein 90 (Hsp90) developed as an antineoplastic agent. It acts by selectively binding to the ATP/ADP binding pocket of Hsp90, blocking its chaperone function and preventing the proper folding and stabilization of multiple oncogenic client proteins such as HER2/ErbB2, Akt, Raf1, Bcr-Abl, and mutated p53. This leads to proteasomal degradation of these proteins and inhibition of tumor cell proliferation. BIIB028 is a water-soluble phosphate prodrug designed for intravenous administration in patients with advanced solid tumors. In phase I clinical trials, it demonstrated biological activity with some patients achieving prolonged stable disease[1][2][3][4][5][7].