Review of HPLC and LC–MS/MS assays for the determination of various nonsteroidal anti‐androgens used in the treatment of prostate cancer

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EarlyView Article

  • Published: Jul 11, 2017
  • Author: P.S. Suresh, Nuggehally R. Srinivas, Ramesh Mullangi
  • Journal: Biomedical Chromatography


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.

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