Denosumab—A powerful RANKL inhibitor to stop lytic metastases and other bone loss actions by osteoclasts

L Kopper - Pathology & Oncology Research, 2012 - Springer
L Kopper
Pathology & Oncology Research, 2012Springer
Denosumab is a perfect example on the targeted anticancer therapy. The inhibition of
RANKL activity suppressed the osteoclasts' resorptive function and so prevented skeletal
related events. This effect is useful not only against bone metastases, but also in the
treatment of other diseases caused by bone loss. In different solid tumors with bone
metastasis the quality of life also improved, although the overall survival usually showed no
change. On the market the main competitors for denosumab are still the bisphosphonates …
Abstract
Denosumab is a perfect example on the targeted anticancer therapy. The inhibition of RANKL activity suppressed the osteoclasts’ resorptive function and so prevented skeletal related events. This effect is useful not only against bone metastases, but also in the treatment of other diseases caused by bone loss. In different solid tumors with bone metastasis the quality of life also improved, although the overall survival usually showed no change. On the market the main competitors for denosumab are still the bisphosphonates (questions of costs and reimbursement are not discussed) and some potential new agents e.g. Src kinases (as dasatinib, saracatinib, bosutinib), cathepsin K inhibitors, (e.g. odanacatib), and new selective estrogen receptor modulators (e.g. bazedoxifene, lasofoxifene). Nevertheless, today denosumab is one of the most powerful agents in bone-saving area.
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