BACKGROUND: The medication used to treat benign prostate hyperplasia (BPH), a common condition in men over 50 years of age, can alter the levels of biomarkers used in prostate cancer detection. Commonly used medications for BPH include alpha-blockers, 5-alpha reductase inhibitors (5-ARIs), and muscarinic antagonists. We studied the impact of these drugs on total prostate-specific antigen (tPSA), free PSA (fPSA), [-2]proPSA, fPSA/tPSA ratio, and the Prostate Health Index (PHI), as well as novel potential biomarkers in the form of glycan composition of fPSA. PATIENTS AND METHODS: Serum samples were collected from 564 males with BPH, with a mean age of 68.5 years. The samples were used to measure levels of tPSA, fPSA, and [-2]proPSA. The fPSA/tPSA and PHI were then calculated. The glycan composition of fPSA was analyzed using lectin-based glycoprofiling. Pharmacotherapy data was collected from the patients' medical records. RESULTS: Alpha-blocker monotherapy was associated with higher fPSA and fPSA/tPSA ratio, and decreased PHI. Levels of tPSA were not impacted. Alpha-blocker and 5-ARI dual therapy was associated with reduced levels of fPSA, [-2]proPSA, and PHI. Therapy combining alpha-blockers and antimuscarinic agents did not significantly influence biomarker levels apart from an increase in a Maackia amurensis lectin-recognized glycan originating in fPSA. CONCLUSION: BPH pharmacotherapy notably affects prostate cancer biomarkers. Recognizing the impact of pharmacotherapy is crucial for achieving an accurate diagnosis of prostate cancer and for planning treatment.

• Keywords
• 5‐alpha reductase inhibitors, PSA, alpha‐blockers, antimuscarinic agents, benign prostate hyperplasia, prostate cancer,
• MeSH
• Adrenergic alpha-Antagonists therapeutic use   MeSH
• Muscarinic Antagonists * therapeutic use   MeSH
• Glycosylation MeSH
• Prostatic Hyperplasia * blood   drug therapy   MeSH
• 5-alpha Reductase Inhibitors therapeutic use   MeSH
• Middle Aged MeSH
• Humans MeSH
• Prostatic Neoplasms blood   drug therapy   MeSH
• Prostate pathology   metabolism   MeSH
• Prostate-Specific Antigen * blood   MeSH
• Aged, 80 and over MeSH
• Aged MeSH
• Check Tag
• Middle Aged MeSH
• Humans MeSH
• Male MeSH
• Aged, 80 and over MeSH
• Aged MeSH
• Publication type
• Journal Article MeSH
• Names of Substances
• Adrenergic alpha-Antagonists MeSH
• Muscarinic Antagonists * MeSH
• 5-alpha Reductase Inhibitors MeSH
• Prostate-Specific Antigen * MeSH