Prostate cancer is the most common cancer and one of the leading causes of 
cancer deaths in men. One of the commonly used approaches to treat metastatic 
prostate cancer was via first-generation nonsteroidal anti-androgens (NSAAs), 
namely flutamide, nilutamide, bicalutamide and topilutamide. Most prostate 
cancer patients who are initially responsive develop the most aggressive form of 
disease called castration-resistant prostate cancer. Second-generation NSAA 
receptor antagonists (enzalutamide, apalutamide and darolutamide) are emerging 
as additional new options to treat castration-resistant prostate cancer. The 
objective of this work was to review the literature on the bioanalytical methods 
for the quantification of first- and second-generation NSAA inhibitors in 
clinical (human plasma) and preclinical (mouse plasma, rat plasma, urine and 
tissue homogenates etc.) studies along with relevant case studies for some 
chosen drugs. Based on the review, it was concluded that the published 
methodologies using either HPLC or LC-MS/MS are well suited for the 
quantification of NSAA inhibitors in various biological fluids to delineate 
pharmacokinetic data.