Roidipedia.Compound reference & reporting
05 AUG 2026
CompoundsAncillary Raloxifene
AncillaryAncillarySERM

Raloxifene

Also known as Evista · Raloxifene hydrochloride

Raloxifene is a second-generation SERM approved for osteoporosis and breast cancer risk reduction. In the PED context it is valued specifically for gynaecomastia: clinical data suggest it reduces established pubertal gynaecomastia more effectively than tamoxifen, making it a preferred SERM when glandular tissue has already formed.

01 Overview

Raloxifene antagonises the oestrogen receptor in breast tissue while acting as an agonist in bone, which is why it both protects against osteoporosis and blocks oestrogen-driven breast growth. A comparative study in adolescents with pubertal gynaecomastia found raloxifene produced greater reduction in breast tissue than tamoxifen, which is the basis for its reputation as the stronger SERM for gyno.

Unlike tamoxifen and clomifene it is used less for HPTA restart and more as a targeted anti-gynaecomastia agent. It carries the SERM-class risk of venous thromboembolism and can cause hot flushes and leg cramps.

02 Mechanism

Selective oestrogen receptor modulator: antagonist at breast tissue, agonist in bone; blocks oestrogen-driven glandular breast growth.

03 Dosing

TierDoseRouteNotes
Gynaecomastia60 mg/dayOralCommonly 60 mg/day; some use up to 120 mg/day short-term for established gyno.
Osteoporosis (label)60 mg/dayOralFDA-approved dose in post-menopausal women.

04 Effects

EffectMagnitudeEvidence
Gynaecomastia regressionReduced established breast tissue more than tamoxifen in a comparative adolescent study.greater than tamoxifenClinical
Bone-protectiveAgonist activity in bone increases bone mineral density, unlike aromatase inhibitors.increased BMDClinical

05 Side effects

EffectSeverityFrequencyEvidenceCountermeasures
Venous thromboembolism riskClass SERM risk of deep vein thrombosis and pulmonary embolism.SevereUncommonClinical
Hot flushesVasomotor flushing, the most frequent reported effect.MildCommonClinical
Leg crampsMuscle/leg cramps reported in label trials.MildCommonClinical

07 References

Raloxifene versus tamoxifen for pubertal gynaecomastiaJ Pediatr
Evista (raloxifene) FDA labelUS FDA

08 Discussion0 comments

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This page is reference information, not medical advice. Doses and protocols are documented as they appear in the clinical literature and in practice — describing them is not a recommendation to use them. Countermeasures listed here are not a substitute for a physician. Legal status varies by jurisdiction and changes.