Pharmacological effect
1. Target: CaSR, a calcium-sensitive receptor of parathyroid host cells, is a polypeptide calciumide. Different from the mechanism of the small molecule cinacarcin: Etecartide forms reversible covalent binding with extracellular cysteine of CaSR through disulfide bonds, reducing the calcium ion threshold required for CaSR activation and allosterically activating CaSR.
2. CaSR activation → inhibition of parathyroid hormone (PTH) synthesis and secretion; After the decline of PTH, calcium mobilization in bones decreases and calcium excretion in the kidneys increases, simultaneously reducing blood calcium and blood phosphorus, and improving the mineral bone metabolism disorder (CKD-MBD) in CKD.
3. Administration method: Intravenous injection at the end of hemodialysis, three times a week; PTH can decrease within 30 minutes after administration and is suitable for dialysis patients