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Estrogen Blockers ​

Overview ​

In most trans men, testosterone therapy alone sufficiently suppresses estrogen. However, some individuals have persistently elevated E2 despite adequate T levels. In these cases, an aromatase inhibitor may be used.

When Are Estrogen Blockers Needed? ​

  • E2 > 50–100 pg/mL despite T in target range (300–1,000 ng/dL)
  • Symptoms of high E2 (bloating, mood swings, breast tenderness)
  • Menstruation persists despite adequate T levels

Available Options ​

MedicationDoseNotes
Anastrozole (Arimidex)0.5–1 mg/weekMost common
Letrozole (Femara)2.5 mg/weekAlternative
Exemestane (Aromasin)12.5–25 mg/weekLess common

How They Work ​

Aromatase inhibitors block the aromatase enzyme, which converts testosterone into estradiol. By blocking this conversion, less T is turned into E2.

Side Effects ​

Side EffectNotes
Joint painMost common
FatigueOccasional
HeadachesOccasional
Bone density (long-term)Theoretical risk; monitor if used long-term

References ​

  1. UCSF Transgender Care. Masculinising hormone therapy — adjunctive medications.