What is the mechanism of action of denosumab?

Briefly, denosumab is a fully human monoclonal antibody that inhibits RANKL and helps regulate turnover in healthy bone. Denosumab binds with high specificity and affinity to the cytokine RANKL, inhibiting its action; as a result, osteoclast recruitment, maturation and action are inhibited, and bone resorption slows.

Does denosumab stimulate bone formation?

Denosumab also causes an increase in bone mass and bone strength in the spine, ultradistal and diaphysis of the radius, proximal tibia and the hip. Recently long-term treatment with denosumab has been shown to cause a continued almost linear increase in total hip and femoral neck BMD beyond 3 years up to 8 years.

What is the difference between bisphosphonates and denosumab?

The difference between denosumab and bisphosphonates for clinical outcomes were change in the skeletal BMD. Denosumab has a greater antiresorptive effect than bisphosphonates. The effects of bisphosphonates for preventing bone loss mainly need bisphosphonates binding to bone mineral.

What is denosumab used for?

Denosumab is used to treat bone loss (osteoporosis) in people who have a high risk of getting fractures. Osteoporosis causes bones to become thinner and break more easily.

Is denosumab a RANKL inhibitor?

Denosumab is the first and only approved antagonist targeting RANKL, which can effectively block the interaction between RANKL and RANK, thereby inhibiting the formation of osteoclasts and enhancing bone strength. Denosumab could be administered once in 6 months by a subcutaneous injection of 60 mg each time.

What is the target of denosumab?

Denosumab is designed to target RANKL (RANK ligand), a protein that acts as the primary signal to promote bone removal/resorption. In many bone loss conditions, RANKL overwhelms the body’s natural defense against bone destruction.

Can denosumab reverse osteoporosis?

Denosumab (Prolia®, Xgeva®) reversed cortical bone loss and increased bone mineral density, lowering wrist fracture rates in women with osteoporosis, according to new research.

How is Prolia different from bisphosphonates?

Fosamax (alendronate sodium) and Prolia (denosumab) are used to treat and prevent osteoporosis. Fosamax is also used to treat Paget’s disease. Fosamax and Prolia belong to different drug classes. Fosamax is a bisphosphonate and Prolia is a monoclonal antibody.

How does Prolia injection work?

Prolia works by blocking osteoclasts (certain bone cells) from breaking down bone tissue in your body. This is the drug’s mechanism of action. Specifically, Prolia works by blocking a protein called RANK. The drug attaches to the RANK protein and helps prevent osteoclasts from breaking down bone.

What is denosumab made of?

Each 1 mL single-use prefilled syringe of Prolia contains 60 mg denosumab (60 mg/mL solution), 4.7% sorbitol, 17 mM acetate, 0.01% polysorbate 20, Water for Injection (USP), and sodium hydroxide to a pH of 5.2.