地诺单抗的使用说明

What is denosumab and what are the instructions for using denosumab?

[Chinese drug name] Denosumab injection

[English drug name] Xgeva (denosumab)

[Manufacturer] Amgen Inc

[Approval date] November 18, 2010 Obtained FDA approval for marketing

Denosumab is the first approved monoclonal antibody that specifically targets RANK ligand. RANK ligand is a transmembrane or soluble protein that is necessary for osteoclasts to maintain their structure, function, and survival. Human RANKL mRNA is mainly found in bones, bone marrow and lymphoid tissues. Its main function in bones is to stimulate the differentiation and activity of osteoclasts and inhibit the apoptosis of osteoclasts. Osteoclasts are responsible for bone resorption, and osteoclast precursors must have low levels of macrophage colony-stimulating factor and RANKL during their differentiation into mature osteoclasts. Denosumab has a high affinity with RANKL, preventing RANK ligand from activating RANK on the surface of osteoclasts, inhibiting osteoclast activation and development, reducing bone resorption, increasing bone density and bone strength of both cortical bone and trabecular bone, promoting bone reconstruction, and reducing the incidence of vertebral, non-vertebral and hip fractures in postmenopausal osteoporotic women.

Recommended usage and dosage of denosumab:

(1) Xgeva can only be administered by subcutaneous injection, not intravenous infusion, intramuscular infusion or intradermal injection. (2) Solid tumor bone metastasis: 120mg once every 4 weeks, injected subcutaneously in the upper arm, thigh or abdomen. (3) Giant cell tumor of bone: 120 mg once every 4 weeks, subcutaneous injection, and then 120 mg on d8 and d15 in the first month of treatment. (4) Administer calcium and vitamin D appropriately to prevent hypocalcemia. (5) Malignant hypercalcemia: 120 mg once every 4 weeks, subcutaneous injection, and then 120 mg on d8 and d15 in the first month of treatment. The medication is injected under the skin in the upper arm, thigh, or abdomen.