地舒单抗对骨转移有多大的疗效？

How effective is it against bone metastasis? Desosumab has been approved for the treatment of bone metastases from solid tumors: indicated for the prevention of bone-related events in patients with bone metastases from solid tumors. It was launched in my country in May 2019. Let’s look at the experimental data to see how effective denosumab is in bone metastasis.

Desosumab 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.

Desosumab 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. The effect of denosumab on bone reconstruction can be evaluated by measuring some bone renewal markers, such as the bone resorption marker N-telopeptide, the bone formation marker bone-specific alkaline phosphatase, etc.

The results of three published key clinical trials showed that compared with zoledronic acid, denosumab prolonged the time to the first adverse bone event (ARE) in patients by 17%, or significantly delayed the median time to the first SRE by 8.2 months (27.6 months vs. 19.4 months). months), denosumab also prolonged the time from first episode to recurrence of SRE by 18% in the study; in addition, for patients with mild or no pain at study entry, denosumab also significantly prolonged the time to worsening pain compared with zoledronic acid.

It can significantly reduce the probability of bone metastasis, significantly delay the recurrence time, and has a relatively good effect on the treatment of bone metastasis.