SBI-46

SBI-46 is a dual-acting small molecule developed by Texas A&M University for the treatment of castration-resistant prostate cancer (CRPC). It functions as an antiandrogen-equipped histone deacetylase (HDAC) inhibitor, targeting both HDAC enzymes and the androgen receptor (AR), including its splice variants (AR-SV) such as AR-V7. The drug works by downregulating the expression of AR and AR-SV, inhibiting AR nuclear localization, and inducing apoptosis in CRPC cells. Preclinical studies have demonstrated that oral administration of SBI-46 inhibits the growth of CRPC xenograft tumors expressing AR or AR-SV in mouse models without evidence of toxicity, selectively targeting AR-positive cells while sparing AR-negative and normal cells.