Is Ormeloxifene (selective estrogen receptor modulator) effective in treating gynaecomastia?

Effectiveness of Ormeloxifene in Treating Gynecomastia

Ormeloxifene is not recommended for treating gynecomastia; tamoxifen is the preferred selective estrogen receptor modulator (SERM) with established efficacy for this condition.

Evidence for SERMs in Gynecomastia Treatment

Gynecomastia is a common condition characterized by benign enlargement of male breast tissue, often caused by an imbalance in the estrogen/testosterone ratio. While there is no specific guideline evidence for ormeloxifene in gynecomastia treatment, several studies support the use of other SERMs:

Tamoxifen Efficacy

• Multiple studies demonstrate tamoxifen's effectiveness in treating gynecomastia:
  • Complete resolution in 78.2% of patients with idiopathic gynecomastia using tamoxifen 20 mg/day 1
  • 83.3% overall response rate (complete or partial resolution) with tamoxifen 20 mg once daily for 6-12 weeks 2
  • Significant decrease in breast size in 7 out of 10 patients in a double-blind crossover study using tamoxifen 10 mg twice daily 3

Clinical Factors Affecting Response

• Tamoxifen is more effective for:
  • "Lump" type gynecomastia (100% response) versus "fatty" type (62.5% response) 2
  • Clinical grade 1-2 gynecomastia 4
  • Patients with lower estrogen levels 4

Treatment Algorithm for Gynecomastia

1. First-line medical therapy:

   • Tamoxifen 10-20 mg twice daily for 3-6 months
   • Monitor for response after 1 month and continue until maximum benefit achieved

2. Alternative SERM options:

   • Raloxifene may be more effective than tamoxifen in some cases
     • One study showed 86% of patients had >50% reduction with raloxifene versus 41% with tamoxifen 5

3. Surgical options:

   • Consider for patients with:
     • Clinical grade 3 gynecomastia 4
     • Failed medical therapy
     • Long-standing fibrotic gynecomastia

Important Considerations

Monitoring and Duration

• Treatment typically continues for 3-6 months or until maximum response
• Recurrence may occur after discontinuation in some patients (seen in follow-up studies) 3

Contraindications and Cautions

• Tamoxifen is contraindicated in patients with history of:
  • Thromboembolic disorders
  • Retinopathy
  • Cataracts
  • Stroke

Side Effects

• Tamoxifen is generally well-tolerated with minimal side effects in the treatment of gynecomastia 3, 2
• No significant toxicity was reported in studies specifically examining gynecomastia treatment

Conclusion

While ormeloxifene has been used as a SERM in other conditions, there is no specific evidence supporting its use in gynecomastia. Tamoxifen has established efficacy and safety data for this indication and should be considered the SERM of choice for medical management of gynecomastia, with raloxifene as a potential alternative with possibly superior efficacy in some cases.