A CaSR agonist
Evocalcet is an agonist of the calcium-sensing receptor (CaSR).1 It induces intracellular calcium release in HEK293 cells expressing human CaSR (EC50 = 92.7 nM). Evocalcet reduces serum levels of parathyroid hormone (PTH) and calcium when administered at doses of 0.3 and 0.1 mg/kg, respectively, in non-nephrectomized and 5/6 nephrectomized rats. It also reduces serum levels of PTH without inducing emesis in marmosets when administered at doses of 0.3 and 0.5 mg/kg.
1.Kawata, T., Tokunaga, S., Murai, M., et al.A novel calcimimetic agent, evocalcet (MT4580/KHK7580), suppresses the parathyroid cell function with little effect on the gastrointestinal tract or CYP isozymes in vivo and in vitroPLoS One13(4)e0195316(2018)
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