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[Third generation selective estrogen receptor modulators benefits beyond bone: effects on breast]

Pluvio J Coronado Martín1, Joaquín Calaf Alsina

  • 1Departamento de Obstetricia y Ginecología, Hospital Clínico San Carlos, Universidad Complutense de Madrid, Madrid, España. pcoronadom@sego.es

Medicina Clinica
|December 19, 2012
PubMed

Insights

Third-generation selective estrogen receptor modulators (SERMs) like bazedoxifene show anti-estrogen effects but lack proven breast cancer prevention in trials. Further research is needed to understand their clinical efficacy.

Area of Science:

  • Pharmacology
  • Oncology
  • Endocrinology

Context:

  • Selective estrogen receptor modulators (SERMs) are critical in hormone-dependent conditions.
  • Tamoxifen and raloxifene (RLX) demonstrated breast cancer preventive effects, driving the search for improved SERMs.
  • Third-generation SERMs, including bazedoxifene (BZA), ospemifene, arzoxifene, and lasofoxifene, were developed.

Purpose:

  • To evaluate the clinical efficacy of third-generation SERMs, particularly bazedoxifene (BZA), in breast cancer prevention.
  • To compare the preventive effects of BZA with raloxifene (RLX) and placebo in clinical trials.

Summary:

  • Bazedoxifene (BZA) exhibits anti-estrogen activity in experimental models.
  • Pivotal clinical trials (301 and extensions) did not demonstrate a significant breast cancer preventive effect for BZA.
  • Raloxifene (RLX) also failed to show its expected preventive effect in the same trials.
  • The study suggests that the trial design and population characteristics (low breast cancer incidence) may have influenced the observed outcomes for BZA and RLX.

Impact:

  • The findings question the clinical utility of BZA for breast cancer prevention despite its anti-estrogen properties.
  • The results highlight the complexities in evaluating SERM efficacy, potentially due to study populations and trial designs.
  • Further investigation is warranted to elucidate the precise role and optimal application of third-generation SERMs in breast cancer management.

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