Evocalcet (KHK7580) functions as an orally administered agonist for the calcium-sensing receptor (CaSR), effectively suppressing the secretion of parathyroid hormone (PTH) from parathyroid gland cells. This characteristic makes Evocalcet a valuable agent for hyperparathyroidism research[1].[2].
体内研究
A single oral dose of Evocalcet at either 0.03 or 0.3 mg/kg influences serum levels of PTH and calcium[1].
Continuous oral administration of Evocalcet at 0.3 mg/kg daily for five weeks decreases serum PTH and calcium levels while elevating serum inorganic phosphorus (IP) levels.
体外研究
When administered at varying concentrations (0, 20, and 60 nM), Evocalcet dose-dependently elevates intracellular calcium levels ([Ca2+].i) in hCaR-HEK293 cells, with an EC50 value of 92.7 nM[2].
Evocalcet exhibits no significant suppressive actions on the activities of cytochrome P450 (CYP) isozymes, indicating a low potential for drug-drug interaction through these pathways.
Evocalcet 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Hamster lung fibroblasts (CCL39, CaSR−) expressing the recombinant human CaSR (HCAR, CaSR+)
500 nM
30 min
To evaluate the effect of EvoSiR4 and EvoSiR6 on CaSR activity. Results showed that EvoSiR4 and EvoSiR6 had EC50 values of 38 nM and 42 nM, respectively, which is a 6-fold improvement in potency compared to evocalcet (EC50 = 243 nM).
Evaluate the effect of Evocalcet on calcium and phosphorus metabolism in rats with chronic kidney disease, results showed significant reduction in serum phosphorus levels
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