Selective Estrogen Receptor Modulators (SERMs)

Disclaimer: This resource is for information purposes only. It is not medical advice and does not replace individualized clinical care. Treatment choices should be made in consultation with a qualified medical provider, based on the best available evidence, patient goals, values, and individual circumstances.

Purpose: SERMs act on estrogen receptors in a tissue-specific way: blocking estrogen in some tissues (e.g., breast) while acting estrogenically in others (e.g., bone). They are occasionally considered in gender-affirming care for those seeking some feminizing effects without prominent breast development.

Key Points:

  • Targeted effect: May limit or prevent breast tissue growth while allowing other estrogenic changes.

  • Most discussed agent: Raloxifene.

  • Evidence base: Primarily cisgender data and approved for medical use by the FDA in 1997; very limited research in trans/non-binary populations.

  • Risks: Comparable clotting risks to other estrogen-involving treatments; long-term safety data in gender-diverse users unknown.

  • Clinical framing: Best viewed as emerging / experimental, not standard.

Provider & Community Resource Overview
Source Focus
QueerDoc
Nov 2020
 Overview of SERMs in gender-affirming care; rationale for minimizing breast development
Transfeminine Science – SERMs Overview
Oct 2020
 Mechanism and potential use in trans/non-binary AMAB; tissue-specific estrogen blockade
GenderGP – Raloxifene Guide
Dec 2025
 Raloxifene basics, rationale, exploratory use in GAC
GenderGP – Raloxifene for Breast Reduction
Oct 2025
 Raloxifene presented as non-surgical option to reduce or limit breast tissue
Transfeminine Science – E2 Dosing Equivalents
Apr 2023
 Estradiol comparison by route (contextual information) for if SERMs are used alongside estrogen