Medical uses and indications
- Used for osteoporosis at high risk for fractures
- Used for bone loss due to certain medications
- Used for those with bone metastases
- Reduces the risk of fractures in those with cancer
- Considered a reasonable treatment for postmenopausal osteoporosis
Adverse effects
- Common side effects include joint and muscle pain in the arms or legs
- Increased risk of infections such as cellulitis
- Increased risk of hypocalcemia (low blood calcium)
- Increased risk of hypersensitivity allergy reactions
- Increased risk of osteonecrosis of the jaw and atypical femur fractures
Contraindications and interactions
- Contraindicated in people with hypocalcemia
- Requires sufficient calcium and vitamin D levels before starting therapy
- Missing data regarding interactions with other drugs
- May increase the risk of osteonecrosis of the jaw following dental procedures
- Invasive dental procedures should be avoided during treatment
Mechanism of action
- Bone remodeling is the process of removing old bone tissue and replacing it with new bone
- Osteoclasts are cells responsible for breaking down bone
- RANKL is a protein that promotes the maturation of osteoclasts
- Denosumab inhibits the maturation of osteoclasts by binding to and inhibiting RANKL
- Denosumab mimics the action of osteoprotegerin, a natural RANKL inhibitor
Regulatory approval
- Approved by the FDA for use in postmenopausal women with risk of osteoporosis
- Approved by the FDA for prevention of skeleton-related events in patients with bone metastases
- First RANKL inhibitor to be approved by the FDA
- Approved by the European Commission for the treatment of postmenopausal osteoporosis
- Approved by the European Commission for the treatment of bone loss in men with hormone ablation therapy for prostate cancer
Denosumab (trade names Prolia and Xgeva) is a human monoclonal antibody for the treatment of osteoporosis, treatment-induced bone loss, metastases to bone, and giant cell tumor of bone.
 Denosumab injection | |
| Monoclonal antibody | |
|---|---|
| Type | Whole antibody |
| Source | Human |
| Target | RANK ligand |
| Clinical data | |
| Trade names | Prolia, Xgeva |
| Other names | AMG-162 |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a610023 |
| License data | |
| Pregnancy category |
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| Routes of administration | Subcutaneous injection |
| ATC code | |
| Legal status | |
| Legal status | |
| Pharmacokinetic data | |
| Bioavailability | N/A |
| Metabolism | proteolysis |
| Identifiers | |
| CAS Number | |
| DrugBank | |
| ChemSpider |
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| UNII | |
| KEGG | |
| ChEMBL | |
| Chemical and physical data | |
| Formula | C6404H9912N1724O2004S50 |
| Molar mass | 144722.80 g·mol−1 |
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Denosumab is contraindicated in people with low blood calcium levels. The most common side effects are joint and muscle pain in the arms or legs.
Denosumab is an inhibitor of RANKL (receptor activator of nuclear factor kappa-Β ligand), which works by decreasing the development of osteoclasts, which are cells that break down bone. It was developed by the biotechnology company Amgen.
