Impact of Distinct Antiandrogen Exposures on the Plasma Metabolome in Feminizing Gender-affirming Hormone Therapy

J Clin Endocrinol Metab. 2024 Oct 15;109(11):2857-2871. doi: 10.1210/clinem/dgae226.

Abstract

Context: The plasma metabolome is a functional readout of metabolic activity and is associated with phenotypes exhibiting sexual dimorphism, such as cardiovascular disease. Sex hormones are thought to play a key role in driving sexual dimorphism.

Objective: Gender-affirming hormone therapy (GAHT) is a cornerstone of transgender care, but longitudinal changes in the plasma metabolome with feminizing GAHT have not been described.

Methods: Blood samples were collected at baseline and after 3 and 6 months of GAHT from transgender women (n = 53). Participants were randomized to different anti-androgens, cyproterone acetate or spironolactone. Nuclear magnetic resonance-based metabolomics was used to measure 249 metabolic biomarkers in plasma. Additionally, we used metabolic biomarker data from an unrelated cohort of children and their parents (n = 3748) to identify sex- and age-related metabolite patterns.

Results: We identified 43 metabolic biomarkers altered after 6 months in both anti-androgen groups, most belonging to the very low- or low-density lipoprotein subclasses, with all but 1 showing a decrease. We observed a cyproterone acetate-specific decrease in glutamine, glycine, and alanine levels. Notably, of the metabolic biomarkers exhibiting the most abundant "sex- and age-related" pattern (higher in assigned female children and lower in assigned female adults, relative to assigned males), 80% were significantly lowered after GAHT, reflecting a shift toward the adult female profile.

Conclusion: Our results suggest an anti-atherogenic signature in the plasma metabolome after the first 6 months of feminizing GAHT, with cyproterone acetate also reducing specific plasma amino acids. This study provides novel insight into the metabolic changes occurring across feminizing GAHT.

Keywords: GAHT; estradiol; metabolism; metabolome; sex hormones; transgender.

Publication types

  • Randomized Controlled Trial

MeSH terms

  • Adolescent
  • Adult
  • Androgen Antagonists* / therapeutic use
  • Biomarkers* / blood
  • Child
  • Cyproterone Acetate* / therapeutic use
  • Female
  • Hormone Replacement Therapy / methods
  • Humans
  • Male
  • Metabolome* / drug effects
  • Metabolomics / methods
  • Middle Aged
  • Sex Reassignment Procedures / methods
  • Spironolactone / therapeutic use
  • Transgender Persons*
  • Transsexualism / blood
  • Transsexualism / drug therapy
  • Young Adult

Substances

  • Androgen Antagonists
  • Cyproterone Acetate
  • Biomarkers
  • Spironolactone