Products Description
English name：Denosumab monoclonal antibody
CAS number：615258-40-7
Molecular formula: C6404H9912N1724O2004S50
Related category: mAb; chemical reagent
Denosumab monoclonal antibody properties
Morphological ：liquid
Color：Colourless to light yellow
Use and synthesis methods
Brief introduction
Dinosumab (Denosumab, denosumab) is a RANK ligand (RANKL) inhibitor, approved by the Food and Drug Administration FDA Denosumab (XgevaChemicalbook, denosumab) for the prevention and treatment of bone related symptoms and inoperable or surgical resection and severe complications.
Target spot
RANK Ligand
Pharmacological action and the mechanism of action
Denosumab is the first approved monoclonal antibody specifically targeting the RANK ligand. RANK ligands are a transmembrane or soluble protein necessary for osteoclasts to maintain their structure, function, and survival. The mRNA of human RANKL is mainly found in bone, bone marrow and lymphoid tissue. Its main role in bone 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 the presence of low levels of macrophage colony-stimulated Chemicalbook factor and RANKL during differentiation into mature osteoclasts. Denosumab has a high affinity with RANKL, preventing RANK ligand activates RANK on the surface of osteoclasts, suppresses the activation and development of osteoclasts, reduces bone resorption, increases the bone mineral density and strength of both cortical bone and trabecular bone, promotes bone reconstruction, and reduces the incidence of vertebrae, non-vertebrae and hip fractures in women with postmenopausal osteoporosis. The effect of denoumab on bone reconstruction can be evaluated by measuring some bone renewal markers, such as N-terminal peptide, a marker of bone resorption, bone formation marker, bone-specific alkaline phosphatase, etc.
Untoward effect
The most common adverse effects reported in clinical trials were back pain (34.7% incidence), limb pain (11.7%), musculoskeletal pain (7.6%), hypercholesterolemia (7.2%) and cystitis (5.9%), and the most common adverse effects leading to discontinuation were breast cancer, back pain and constipation. Other common adverse effects include anemia (3.3%), angina (2.6%), atrial fibrillation (2.0%), vertigo (Chemicalbook5.0%), abdominal pain (3.3%), flatulence (2.2%), gastroesophageal reflux disease (2.1%), peripheral edema (4.9%), weakness (2.3%), upper respiratory tract infection (4.9%), pneumonia (3.9%), pharyngitis (2.3%), herpes zoster (2.0%), spinal osteoarthritis (2.1%), sciatica (4.6%), insomnia (3.2%), skin rash (2%). 5%), pruritus (2.2%).
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