Long-term treatment with raloxifene, but not bisphosphonates, reduces circulating sclerostin levels in postmenopausal women

Osteoporos Int. 2012 Apr;23(4):1235-43. doi: 10.1007/s00198-011-1675-1. Epub 2011 Jun 10.

Abstract

We determined whether suppression of sclerostin levels by estrogen treatment was mediated by anti-resorptive effect. Raloxifene, but not bisphosphonates, suppressed circulating sclerostin concentration, suggesting that sclerostin may mediate the action of estrogen on bone metabolism, independently of their anti-resorptive effects.

Introduction: Circulating sclerostin concentrations are higher in postmenopausal than in premenopausal women, and estrogen treatment suppresses sclerostin levels in both men and women. We determined whether anti-resorptives may suppress the circulating sclerostin levels.

Methods: We conducted a retrospective observational study. Eighty postmenopausal women were treated with raloxifene for 19.4 ± 7.7 months (n = 16), bisphosphonates for 19.2 ± 6.7 months (n = 32), or were untreated (n = 32) for 17.1 ± 4.6 months. Plasma sclerostin concentrations were measured before and after treatment.

Results: Plasma sclerostin levels after treatment were significantly lower in the raloxifene than in the control group (55.8 ± 23.4 pmol/l vs. 92.1 ± 50.4 pmol/l, p = 0.046), but were similar between the bisphosphonate and control groups. Relative to baseline, raloxifene treatment markedly reduced plasma sclerostin concentration (-40.7 ± 22.8%, p < 0.001), with respect to both control (-7.5 ± 29.1%) and bisphosphonate (-3.1 ± 35.2%) groups. Changes in bone-specific alkaline phosphatase and osteocalcin levels showed reverse associations with sclerostin concentration changes in the raloxifene (γ = -0.505, p = 0.017) and control (γ = -0.410, p = 0.020) groups.

Conclusions: Raloxifene, but not bisphosphonates, significantly suppressed circulating sclerostin concentration, suggesting that sclerostin may mediate the action of estrogen on bone metabolism, independently of their anti-resorptive effects.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adaptor Proteins, Signal Transducing
  • Aged
  • Alkaline Phosphatase / blood
  • Biomarkers / blood
  • Bone Density / drug effects
  • Bone Density Conservation Agents / administration & dosage
  • Bone Density Conservation Agents / pharmacology*
  • Bone Density Conservation Agents / therapeutic use
  • Bone Morphogenetic Proteins / blood
  • Bone Morphogenetic Proteins / drug effects*
  • Diphosphonates / administration & dosage
  • Diphosphonates / pharmacology*
  • Diphosphonates / therapeutic use
  • Drug Administration Schedule
  • Female
  • Genetic Markers / drug effects*
  • Humans
  • Middle Aged
  • Osteocalcin / blood
  • Osteoporosis, Postmenopausal / blood*
  • Osteoporosis, Postmenopausal / drug therapy
  • Osteoporosis, Postmenopausal / physiopathology
  • Raloxifene Hydrochloride / administration & dosage
  • Raloxifene Hydrochloride / pharmacology*
  • Raloxifene Hydrochloride / therapeutic use
  • Retrospective Studies
  • Selective Estrogen Receptor Modulators / administration & dosage
  • Selective Estrogen Receptor Modulators / pharmacology
  • Selective Estrogen Receptor Modulators / therapeutic use

Substances

  • Adaptor Proteins, Signal Transducing
  • Biomarkers
  • Bone Density Conservation Agents
  • Bone Morphogenetic Proteins
  • Diphosphonates
  • Genetic Markers
  • SOST protein, human
  • Selective Estrogen Receptor Modulators
  • Osteocalcin
  • Raloxifene Hydrochloride
  • Alkaline Phosphatase