Further Insights Into the Metabolism of LGD-4033 in Human Urine. Part 2. A New Minor Metabolite With Antagonistic Activity on the Androgen Receptor Can Indicate Recent Substance Intake.

ABSTRACT: Using a targeted metabolic investigation approach, a new, previously undescribed metabolite, which is a pyrrole derivative of LGD-4033, has been detected and coded as M8. This metabolite can be detected in postadministration human urine samples up to 6 days after administration. It has also been detected in post-administration samples, mimicking supplement contamination, after repeated 10 μg doses detectable for ≥ 120 h after administration. Given M8's structural similarity to LGD-4033, its androgen receptor (AR) agonist/antagonist properties were studied using in silico molecular docking and functional in vitro AR transactivation assays in the PC3(AR)₂ cell model, alongside other selected LGD-4033 metabolites. The results indicate that M8 can act as a potent AR antagonist, wher

SUBMITTER: Angelis YS 

PROVIDER: S-EPMC12796561 | biostudies-literature | 2026 Jan

REPOSITORIES: biostudies-literature