Raloxifene
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
| Tier | Dose | Route | Notes |
|---|---|---|---|
| Gynaecomastia | 60 mg/day | Oral | Commonly 60 mg/day; some use up to 120 mg/day short-term for established gyno. |
| Osteoporosis (label) | 60 mg/day | Oral | FDA-approved dose in post-menopausal women. |
04 Effects
| Effect | Magnitude | Evidence | |
|---|---|---|---|
| Gynaecomastia regressionReduced established breast tissue more than tamoxifen in a comparative adolescent study. | greater than tamoxifen | Clinical | |
| Bone-protectiveAgonist activity in bone increases bone mineral density, unlike aromatase inhibitors. | increased BMD | Clinical |
05 Side effects
| Effect | Severity | Frequency | Evidence | Countermeasures |
|---|---|---|---|---|
| Venous thromboembolism riskClass SERM risk of deep vein thrombosis and pulmonary embolism. | Severe | Uncommon | Clinical | |
| Hot flushesVasomotor flushing, the most frequent reported effect. | Mild | Common | Clinical | |
| Leg crampsMuscle/leg cramps reported in label trials. | Mild | Common | Clinical |