GH501

GH501 is a flurbiprofen-modified small-molecule compound developed for the treatment of lethal forms of prostate cancer, specifically castration-resistant prostate cancer (CRPC) and bone metastatic disease. It functions as an inhibitor of the androgen receptor (AR) signaling axis, targeting both the full-length AR and constitutively active AR variants, such as AR-V7, which are often implicated in resistance to standard therapies like enzalutamide. Preclinical studies have demonstrated that GH501 possesses nanomolar potency, effectively inducing cell cycle arrest and apoptosis in CRPC cells. Furthermore, it has shown significant efficacy in inhibiting skeletal tumor growth in xenograft models without observable in vivo toxicities, suggesting its potential as a therapeutic candidate for advanced prostate cancer.