Abstract
BackgroundCurrent treatments for the prevention of thromboembolism include heparin and low-molecular weight heparins (LMWHs). A number of studies have suggested that long term administration of these drugs may adversely affect osteoblasts and therefore, bone metabolism. Xarelto™ (Rivaroxaban) is a new anti-thrombotic drug for the prevention of venous thromboembolism in adult patients undergoing elective hip and knee replacement surgery. The aim of this in vitro study was to investigate the possible effects of rivaroxaban on osteoblast viability, function and gene expression compared to enoxaparin, a commonly used LMWH.MethodsPrimary human osteoblast cultures were treated with varying concentrations of rivaroxaban (0.013, 0.13, 1.3 and 13 μg/ml) or enoxaparin (1, 10 and 100 μg/ml). The effect of each drug on osteoblast function was evaluated by measuring alkaline phosphatase activity. The MTS assay was used to assess the effect of drug treatments on cell proliferation. Changes in osteocalcin, Runx2 and BMP-2 messenger RNA (mRNA) expression following drug treatments were measured by real-time polymerase chain reaction (PCR).ResultsRivaroxaban and enoxaparin treatment did not adversely affect osteoblast viability. However, both drugs caused a significant reduction in osteoblast function, as measured by alkaline phosphatase activity. This reduction in osteoblast function was associated with a reduction in the mRNA expression of the bone marker, osteocalcin, the transcription factor, Runx2, and the osteogenic factor, BMP-2.ConclusionsThese data show that rivaroxaban treatment may negatively affect bone through a reduction in osteoblast function.
Highlights
Current treatments for the prevention of thromboembolism include heparin and low-molecular weight heparins (LMWHs)
Rivaroxaban treatment did not have an adverse effect on osteoblast viability, cells treated with the lower concentrations of rivaroxaban (0.013 and 0.13 μg/ml) showed a significant increase in viability of 15% and 10%, respectively (Figure 1)
As long term administration of heparin and LMWH has been associated with reduced bone mineral density [8,15] and increased fracture rates in pregnant women [16,17], we investigated the effect of rivaroxaban on human osteoblasts
Summary
Current treatments for the prevention of thromboembolism include heparin and low-molecular weight heparins (LMWHs). XareltoTM (Rivaroxaban) is a new anti-thrombotic drug for the prevention of venous thromboembolism in adult patients undergoing elective hip and knee replacement surgery. The aim of this in vitro study was to investigate the possible effects of rivaroxaban on osteoblast viability, function and gene expression compared to enoxaparin, a commonly used LMWH. Rivaroxaban or XareltoTM (Bayer Schering Pharma AG) is an anti-thrombotic drug that was granted marketing approval by the European Commission (Enterprise & Industry/Pharmaceuticals) in 2008 for the prevention of venous thromboembolism in adult patients undergoing elective hip and knee replacement surgery [9]. The effect of each drug was evaluated in terms of its effect on osteoblast viability, function and gene expression
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