AU-15330 is a protein hydrolysis-targeted chimeric (PROTAC) degrader of the SWI/SNF ATPase subunits SMARCA2 and SMARCA4.AU-15330 potently inhibits tumor growth in a prostate cancer xenograft model and acts synergistically with the AR antagonist enzalutamide.AU-15330 shows partial therapeutic efficacy and non-toxicity with the AR antagonist enzalutamide in a desmoplasia-resistant prostate cancer (CRPC) model. AU-15330 showed partial therapeutic efficacy in a denervation-resistant prostate cancer (CRPC) model and AU-15330 was characterized by non-toxicity.

AU-15330 (10 and 30 mg/kg; i.v.; 5 days per week for 3 weeks) shows no evident toxicity in immuno-competent mice.[1]
AU-15330 (60 mg/kg with or without 10 mg/kg enzalutamide; i.v.; 3 days per week; p.o.; 5 days per week for 5 weeks) leads to potent inhibition of tumor growth, triggering disease regression in more than 20% of animals. The combinatorial regimen induced the most potent anti-tumor effect, with regression in all animals.[1]
AU-15330 (60 mg/kg with or without 10 mg/kg enzalutamide; i.v.; 3 days per week; p.o.; 5 days per week for 5 weeks) strongly inhibits the growth of C4-2B cell line-derived CRPC xenografts in intact mice as a single agent and synergized with enzalutamide.[1]
AU-15330 (60 mg/kg with or without 10 mg/kg enzalutamide; i.v.; 3 days per week; p.o.; 5 days per week for 5 weeks) combines with enzalutamide induces significant tumor growth inhibition, causing regression in more than 30% of animals in the middle of CRPC variant of the MDA-PCa-146-12 PDX by tumor implantation into castrated mice.[1]