Regulation of drug-metabolizing enzymes by sex-related hormones: clinical implications for transgender medicine

Trends Pharmacol Sci. 2022 Jul;43(7):582-592. doi: 10.1016/j.tips.2022.03.006. Epub 2022 Apr 26.

Abstract

Transgender medicine is a diverse and growing clinical field with unmet gaps in pharmacological knowledge. Hormone therapy (testosterone or estrogen treatment), one part of the standard of medical care for transgender adults, aligns secondary sex characteristics with an individual's gender identity and expression. Despite established effects of sex steroids on drug-metabolizing enzyme expression and activity in vitro and in animal models, the effect of long-term, supraphysiological sex hormone treatment on drug metabolism in transgender adults is not yet established. Here, we synthesize available in vitro and animal model data with pharmacological concepts in transgender medicine to predict potential effects of sex steroids on drug-metabolizing enzymes, and their relationship with potential hormone-drug interactions, in transgender medicine.

Keywords: cytochrome P450; drug metabolism; estrogen; hormone therapy; testosterone; transgender people.

Publication types

  • Review

MeSH terms

  • Animals
  • Estrogens / pharmacology
  • Estrogens / therapeutic use
  • Female
  • Gender Identity
  • Gonadal Steroid Hormones
  • Hormones / therapeutic use
  • Humans
  • Male
  • Testosterone / therapeutic use
  • Transgender Persons*

Substances

  • Estrogens
  • Gonadal Steroid Hormones
  • Hormones
  • Testosterone