Ligand id: 6886

Name: denosumab

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Summary of Clinical Use
Prolia® (FDA approval 2010) is used to treat bone loss in postmenopausal osteoporosis, men receiving androgen deprivation therapy for non-metastatic prostate cancer and women receiving adjuvant aromatase inhibitor therapy for breast cancer. In May 2018 the FDA approval for Prolia® was expanded to include treatment of glucocorticoid-induced osteoporosis in males and females who are at high risk of fracture.
Xgeva® (FDA approval 2011) is used for the prevention of skeletal-related events in patients with bone metastases from solid tumors. In December 2014 Xgeva® approval was expanded to include treatment of hypercalcemia of malignancy (HCM) whch is refractory to traditional bisphosphonate therapy. HCM can develop in cancer patients, with symptoms arising from cancer-driven increases in bone resorption. Untreated HCM can lead to renal failure, progressive mental impairment, coma and death [2,4].
Mechanism Of Action and Pharmacodynamic Effects
Denosumab is a high-affinity, selective inhibitor of receptor activator of nuclear factor-kappaB ligand (RANKL). Inhibition of RANKL-mediated RANK activation on pre-osteoclasts reduces their maturation to osteoclasts, thus protecting bone from degradation [3] and shifting the equilibrium of bone re-modelling towards bone formation.
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