ITRI-90

ITRI-90 is an orally bioavailable proteolysis-targeting chimera (PROTAC) developed by the Industrial Technology Research Institute (ITRI) for the treatment of castration-resistant prostate cancer (CRPC). It is designed to overcome resistance to current anti-androgen therapies, such as enzalutamide, by inducing the degradation of both full-length androgen receptor (AR) and its splice variants, including AR-V7, which lacks the ligand-binding domain. ITRI-90 works by recruiting the Von Hippel-Lindau (VHL) E3 ubiquitin ligase to the AR protein, leading to its ubiquitination and subsequent degradation by the 26S proteasome. This approach effectively shuts down AR signaling, a key driver of prostate cancer progression.