What are the most effective medications for female-to-male (FTM) transgender individuals, specifically hormone replacement therapy (HRT) with medications such as spironolactone (Aldactone) and estrogen (e.g. estradiol) blockers or inhibitors?

Medical Advisory BoardAll articles are reviewed for accuracy by our Medical Advisory Board
Educational purpose only • Exercise caution as content is pending human review
Article Review Status
Submitted
Under Review
Approved

Last updated: May 15, 2025View editorial policy

Personalize

Help us tailor your experience

Which best describes you? Your choice helps us use language that's most understandable for you.

From the Guidelines

For transgender women (male to female), the most effective hormone therapy regimen typically includes estrogen and anti-androgens, with a common regimen consisting of estradiol (2-6 mg daily, oral or transdermal patches of 0.1-0.2 mg/day) combined with an anti-androgen such as spironolactone (100-300 mg daily) or cyproterone acetate (25-50 mg daily, though not available in the US) 1. The goal of hormone therapy for transgender women is to induce feminizing effects, such as breast development, fat redistribution, reduced muscle mass, and decreased body hair, while minimizing potential side effects.

  • Key considerations for hormone therapy in transgender women include:
    • Estrogen dosage and route of administration, with transdermal patches often preferred due to lower risk of blood clots and liver problems
    • Choice of anti-androgen, with spironolactone being a common option due to its efficacy and relatively favorable side effect profile
    • Monitoring of hormone levels, liver function, and cardiovascular health to minimize potential risks and adjust treatment as needed
    • Individualization of treatment based on patient health factors, such as age, medical history, and lifestyle
  • According to the most recent and highest quality study, hormone therapy for transgender women can be safe and effective when supervised by experienced healthcare providers, with regular monitoring and adjustments to minimize potential side effects and optimize outcomes 1.
  • It is essential to prioritize the patient's overall health and well-being, taking into account potential risks and benefits of hormone therapy, and to provide personalized care and support throughout the treatment process.

From the Research

Medications for Transgender Male to Female Transition

The primary medications used for transgender male to female transition are:

  • Estrogens: to induce feminizing changes and suppress previously developed masculinization 2, 3, 4, 5
  • Antiandrogens: used as adjuncts to help suppress masculinizing features 2, 3, 4, 5

Goals of Hormone Therapy

The goals of hormone therapy for transgender females are to:

  • Induce feminizing changes 2, 3, 4, 5
  • Suppress previously developed masculinization 2, 3, 4, 5
  • Improve gender dysphoria and mental health outcomes 3, 6

Risks and Considerations

The risks and considerations of hormone therapy for transgender females include:

  • Thrombosis: a primary short-term risk of estrogens 2, 5
  • Bone and cardiovascular health: important considerations in transgender patients on long-term hormones 3
  • Metabolic indices: should be monitored while patients are on cross-sex hormone therapy 3
  • Depression and osteoporosis: increased risks in transgender women 5
  • Hormone-sensitive cancer: seems to be low in transgender women, with no increased risk of breast cancer compared with women and no increase in prostate cancer when compared with men 5

References

Guideline

Guideline Directed Topic Overview

Dr.Oracle Medical Advisory Board & Editors, 2025

Research

Gender-Affirming Hormone Therapy for Transgender Females.

Clinical obstetrics and gynecology, 2018

Research

Hormone therapy for transgender patients.

Translational andrology and urology, 2016

Research

Oestrogen and anti-androgen therapy for transgender women.

The lancet. Diabetes & endocrinology, 2017

Research

Hormone Therapy for Transgender Adults.

The Urologic clinics of North America, 2019

Professional Medical Disclaimer

This information is intended for healthcare professionals. Any medical decision-making should rely on clinical judgment and independently verified information. The content provided herein does not replace professional discretion and should be considered supplementary to established clinical guidelines. Healthcare providers should verify all information against primary literature and current practice standards before application in patient care. Dr.Oracle assumes no liability for clinical decisions based on this content.

Have a follow-up question?

Our Medical A.I. is used by practicing medical doctors at top research institutions around the world. Ask any follow up question and get world-class guideline-backed answers instantly.