Food effect on abiraterone pharmacokinetics and safety on abiraterone acetate coadministration with low-fat or high-fat meals was examined in healthy subjects and metastatic castration-resistant prostate cancer (mCRPC) patients. Healthy subjects (n = 36) were randomized to abiraterone acetate (single dose, 1000 mg) + low-fat meal, + high-fat meal, and fasted state. mCRPC patients received repeated doses (abiraterone acetate 1000 mg + 5 mg prednisone twice daily; days 1–7) in a modified fasting state followed by abiraterone acetate plus prednisone within 0.5 hours post–low-fat (n = 6) or high-fat meal (n = 18; days 8–14). In healthy subjects, geometric mean (GM) abiraterone area under plasma concentration–time curve (AUC) increased ˜5- and ˜10-fold, respectively, with low-fat and high-fat meals versus fasted state (GM [coefficient of variation], 1942  and 4077  ng · h/mL vs 421  ng · h/mL, respectively). In mCRPC patients, abiraterone AUC was ˜2-fold higher with a high-fat meal and similar with a low-fat meal versus modified fasting state (GM [coefficient of variation]: 1992  vs 973  ng · h/mL and 1264  vs 1185  ng · h/mL, respectively). Adverse events (all grade ≤ 3) were similar, with high-fat/low-fat meals or fasted/modified fasting state. Short-term dosing with food did not alter abiraterone acetate safety.