Denosumab
- Atc Codes:M05BX04
- CAS Codes:615258-40-7
- PHARMGKB ID:615258-40-7
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Genes that may be involved
- Drug Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Bulgaria: Prolia; Czech Republic: Prolia; Denmark: Prolia; Estonia: Prolia; Finland: Prolia; Greece: Prolia; Hungary: Prolia; Ireland: Prolia; Latvia: Prolia; Lithuania: Prolia; Luxembourg: Prolia; Malta: Prolia; Netherlands: Prolia; Poland: Prolia; Portugal: Prolia; Romania: Prolia; Slovakia: Prolia; Slovenia: Prolia; Sweden: Prolia; UK: Prolia.
North America
Canada: Prolia; USA: Prolia, Xgeva.
Drug combinations
Chemistry
Denosumab: C~6404~H~9908~N~1724~O~2004~S~50~. Mw: 144716.86. (1) Immunoglobulin G~2~, anti-(human osteoclast differentiation factor)(human monoclonal AMG162 heavy chain), disulfide with human monoclonal AMG162 light chain, dimer (2) AMG 162. CAS: 615258-40-7
Pharmacologic Category
Bone Resorption Inhibitors. Monoclonal Antibody. (ATC-Code: M05BX04).
Mechanism of action
A human monoclonal antibody (IgG~2~) that targets and binds with high affinity and specificity to nuclear factor-κB ligand (RANKL), preventing activation of its receptor, RANK, on the surface of osteoclast precursors and osteoclasts. Prevention of the RANKL/RANK interaction inhibits osteoclast formation, function and survival, thereby decreasing bone resorption in cortical and trabecular bone.
Therapeutic use
Treatment of osteoporosis in postmenopausal women at increased risk of fractures (significantly reduces risk of vertebral, non-vertebral and hip fractures). Treatment of bone loss associated with hormone ablation in men with prostate cancer at increased risk of fractures (significantly reduces risk of vertebral fractures).
Pregnancy and lactiation implications
There are no adequate, well-controlled studies in pregnant women. Not recommended for use in pregnant women. It is unknown whether denosumab is excreted in human milk. Use during lactation only if potential benefit to mother outweighs possible risk to fetus.
Unlabeled use
Contraindications
Hypocalcemia. Hypersensitivity to denosumab or any component of the formulation.
Warnings and precautions
Hypocalcemia must be corrected before initiating therapy. Use with caution in severe renal impairment (CrCl <30 mL/minute) or in patients receiving dialysis (greater risk of developing hypocalcemia). May develop skin infections (predominantly cellulitis) leading to hospitalization. Osteonecrosis of the jaw has been reported in patients with concomitant risk factors treated with denosumab or bisphosphonates; while on treatment, these patients should avoid invasive dental procedures if possible. The needle cover on the pre-filled syringe contains a derivative of latex which may cause allergic reactions. Use not recommended in children and adolescents. Not recommended in rare hereditary problems of fructose intolerance.