AG-1-33

AG-1-33 is a genistein-androgen receptor (AR) antagonist conjugate developed by researchers at the Georgia Institute of Technology and Emory University. It is designed to treat both androgen-dependent and castration-resistant prostate cancer (CRPC). The molecule incorporates genistein, a soy isoflavone known to perturb multiple biochemical pathways relevant for cancer survival, into an AR-binding template. AG-1-33 functions as both an AR antagonist and a selective androgen receptor degrader (SARD), aiming to overcome resistance mechanisms such as mutations in the AR ligand-binding domain that can render traditional antagonists like enzalutamide ineffective. In preclinical studies, AG-1-33 has demonstrated potent growth inhibitory activity in LNCaP (AR-dependent) and DU-145 (AR-independent) prostate cancer cell lines.

Other names

genistein-AR antagonist conjugate