Compound · raloxifene
T1serms_ais

Raloxifene (Evista)

Second-generation SERM with pronounced tissue selectivity. Strong estrogen receptor antagonist in breast and uterine tissue. Estrogen agonist in bone, reducing osteoclast-mediated resorption and maintaining bone mineral density. Minimal uterine stimulation compared to tamoxifen. Demonstrated superior efficacy in gynecomastia reversal versus tamoxifen in clinical trials.

Half-life
28 hours
Bioavailability
2% (oral, extensive first-pass glucuronidation)
Route
oral
Evidence tier
T1 — Multiple RCTs
Optimization pillars
recovery
References
4 peer-reviewed
Dose ranges

Three tiers ordered by aggressiveness. Tier chips on every OPTIMIZE intervention let you filter the catalog by your evidence tolerance.

conservative
30 mg/day
Gynecomastia prevention
moderate
60 mg/day
Active gynecomastia reversal
aggressive
120 mg/day
Aggressive gyno reversal (off-label, limited data)
Monitoring
  • estradiol
  • lipid-panel
  • hdl
  • ldl
  • triglycerides
  • alt
  • ast
Contraindications
  • history-of-dvt-pe
  • active-venous-thromboembolism
  • pregnancy
  • premenopausal-women
References
  • PMID:15159289Raloxifene for the prevention of breast cancer in postmenopausal womenN Engl J Med, 2004
  • PMID:14764776Raloxifene for gynecomastiaJ Clin Endocrinol Metab, 2004
  • PMID:22106945Raloxifene versus tamoxifen for gynecomastia in adolescentsJ Pediatr Endocrinol Metab, 2011
  • PMID:25428787Selective estrogen receptor modulators in the treatment of breast cancerFront Oncol, 2014
Notes

Raloxifene is the SERM most people should be using for gynecomastia and are not. Head-to-head data against tamoxifen shows better breast tissue selectivity with less uterine stimulation. The 2% oral bioavailability sounds alarming until you understand that the active glucuronide metabolites do the work. The 28-hour half-life means daily dosing is sufficient. For existing gynecomastia — not prevention, reversal — 60mg daily for 3-6 months is the clinical protocol. Most people default to tamoxifen because they learned about it first, not because the evidence supports it.

This is not medical advice

Discuss with a licensed clinician before starting, stopping, or changing any compound. This page documents what the research literature describes — it is not a prescription.

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