Cyproterone acetate vs leuprolide acetate in combination with transdermal oestradiol in transwomen: a comparison of safety and effectiveness

Clin Endocrinol (Oxf). 2016 Aug;85(2):239-46. doi: 10.1111/cen.13050. Epub 2016 Mar 21.

Abstract

Objective: To retrospectively compare the effectiveness and safety of 1-year administration of transdermal oestradiol (TE) with cyproterone acetate (CPA) or leuprolide acetate (Leu) in transwomen.

Design, patients and measurements: Forty transwomen received 50 mg of CPA daily orally (n = 20; CPA+E group) or Leu at a dose of 3·75 mg i.m. monthly (n = 20; Leu+E group) in combination with TE at a dose of 1 or 2 mg daily for 1 year. Reproductive hormones, biochemical parameters, body composition and bone mineral density were assessed.

Results: LH, FSH and total testosterone levels were significantly decreased by month three of hormone administration in both groups and continued to decrease until month 12; the decrease in LH levels in the first 12 months was significantly faster in the Leu+E group. Prolactin was significantly increased at month 12 in the CPA+E group only. Bone metabolism parameters and bone mineral density as detected at DEXA did not significantly change in either group, apart from a statistically significant increase in parathyroid hormone after 52 weeks of Leu administration. Total cholesterol and HDL-cholesterol were significantly increased in the Leu+E group and reduced in the CPA+E group. No major adverse effects were registered in either group. Psychological well-being parameters did not differ between the two groups.

Conclusions: Preliminary results from this retrospective observational pilot study suggest that CPA and Leu in combination with TE are equally effective in the suppression of gonadotrophins and testosterone levels over 1 year. Whether the different effects on HDL-cholesterol may lead to long-term different cardiovascular safety profiles remains to be defined.

Publication types

  • Comparative Study
  • Observational Study

MeSH terms

  • Androgen Antagonists
  • Cholesterol, HDL / blood
  • Cyproterone Acetate / administration & dosage*
  • Drug Therapy, Combination
  • Estradiol / administration & dosage*
  • Female
  • Fertility Agents, Female
  • Gonadotropins / blood
  • Humans
  • Leuprolide / administration & dosage*
  • Retrospective Studies
  • Testosterone / blood
  • Transgender Persons
  • Treatment Outcome

Substances

  • Androgen Antagonists
  • Cholesterol, HDL
  • Fertility Agents, Female
  • Gonadotropins
  • Testosterone
  • Cyproterone Acetate
  • Estradiol
  • Leuprolide