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Related Concept Videos

Bone Remodeling01:40

Bone Remodeling

Bone remodeling is a continuous and balanced process of bone resorption by osteoclasts and bone formation by osteoblasts. In adults, it helps maintain bone mass and calcium homeostasis. While mechanical stress can stimulate turnover as part of the normal maintenance and reparative process, several hormones also regulate bone remodeling.
Transducer Mechanism: Nuclear Receptors01:31

Transducer Mechanism: Nuclear Receptors

Nuclear receptors, or NRs, are unique transcription factors that regulate gene transcription and affect the cellular pathways involved in reproduction, development, or metabolism. Their ability to be stimulated by small lipophilic ligands and control vital cellular processes makes them ideal drug targets. Nearly 10-15% of currently prescribed drugs target these receptors.
About 48 different soluble family members of nuclear receptors are identified that can be divided into two main classes:
Hormones and Bone Tissue01:17

Hormones and Bone Tissue

The endocrine system produces and secretes hormones, which interact with the skeletal system. These hormones control bone growth, maintain bone once it is formed, and remodel it.
Hormones That Influence Osteoblasts and/or Maintain the Matrix
Several hormones are necessary for controlling bone growth and maintaining the bone matrix. The pituitary gland secretes growth hormone (GH), which, as its name implies, controls bone growth. This happens in several ways: first, it triggers chondrocyte...
Adrenergic Antagonists: ɑ and β-Receptor Blockers01:31

Adrenergic Antagonists: ɑ and β-Receptor Blockers

Third-generation β-blockers, such as labetalol and carvedilol, represent a significant advancement in managing cardiovascular conditions. Unlike conventional β-blockers, which can induce peripheral vasoconstriction, third-generation drugs block α1 adrenoceptors. This promotes vasodilation through several mechanisms, such as increased nitric oxide production, inhibition of calcium ion entry, opening of potassium ion channels, and antioxidant action. Labetalol, for instance, is clinically...

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Related Experiment Video

Updated: May 15, 2026

An In Vivo Estrogen Deficiency Mouse Model for Screening Exogenous Estrogen Treatments of Cardiovascular Dysfunction After Menopause
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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
Summary

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.

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Last Updated: May 15, 2026

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Systems Biology of Metabolic Regulation by Estrogen Receptor Signaling in Breast Cancer
10:36

Systems Biology of Metabolic Regulation by Estrogen Receptor Signaling in Breast Cancer

Published on: March 17, 2016

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.