Alendronate-induced atypical bone fracture: evidence that the drug inhibits osteogenesis

J Clin Pharm Ther. 2014 Aug;39(4):349-53. doi: 10.1111/jcpt.12149. Epub 2014 Mar 24.

Abstract

What is known and objective: Alendronate (ALN) is used for the treatment of post-menopausal osteoporosis. By reducing bone turnover, it increases bone mineral density. However, recent reports suggest an increased risk of atypical bone fractures after long-term ALN administration. Despite its well-known anti-osteoclastic activity, it is unclear whether ALN also suppresses human mesenchymal stem cell (hMSC)-mediated osteogenesis, thus possibly resulting in atypical bone fragility. We hypothesized that ALN does this and we look at its in vitro effects on osteogenesis.

Methods: Morphological analysis, reverse transcriptase polymerase chain reaction, cell viability, alkaline phosphatase (ALP) activity and mineralization assays were investigated in hMSCs treated with a wide range of ALN.

Results and discussion: After treatment with high concentrations of ALN for 3 and 7 days, cell viability was significantly reduced and cell morphology was altered. Osteogenic differentiation of hMSCs was also substantially suppressed as demonstrated by decreased ALP activity although ALN did not affect osteogenic-related genes tested. Furthermore, ALN at all concentrations tested drastically inhibited alizarin red S-positive mineralized matrix.

What is new and conclusion: ALN has a strong inhibitory effect on hMSC-mediated osteogenesis by suppressing cell proliferation, osteoblast differentiation and function. The insight gained may help in the development of safer alternatives.

Keywords: alendronate; mesenchymal stem cell; mineralization; osteoblast differentiation; viability.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alendronate / toxicity*
  • Bone Density Conservation Agents / toxicity*
  • Cell Differentiation / drug effects
  • Cell Proliferation / drug effects
  • Fractures, Bone / chemically induced*
  • Humans
  • In Vitro Techniques
  • Mesenchymal Stem Cells / cytology
  • Mesenchymal Stem Cells / drug effects
  • Osteogenesis / drug effects*
  • Reverse Transcriptase Polymerase Chain Reaction
  • Time Factors

Substances

  • Bone Density Conservation Agents
  • Alendronate