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Ligand id: 6886
View more information in the IUPHAR Pharmacology Education Project: denosumab
|No information available.|
|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  and shifting the equilibrium of bone re-modelling towards bone formation.|
For extended ADME data see the following:
Electronic Medicines Compendium (eMC)
European Medicines Agency (EMA)