Abiraterone was caged by the [Ru(tpy)(dmbpy)] (dmbpy = 6,6′-dimethylbipyridine) center and its binding affinity for CYP17A1 and cytotoxicity against DU145 prostate cancer cell line were evaluated in the dark and after activation with light (λirr ≥ 395 nm). Here, CYP17A1 is linked to prostate cancer.