Etelcalcetide is a peptide agonist of the calcium-sensing receptor (CaSR).1 It is selective for CaSR over a panel of 33 receptors and ion channels, as well as the norepinephrine transporter at 10 ?M. Etelcalcetide increases intracellular calcium levels in HEK293T cells expressing the human CaSR receptor with an EC50 value of 0.53 ?M. It also inhibits parathyroid secretion from primary rat parathyroid cells (EC50 = 0.36 ?M in the presence of calcium). Etelcalcetide (0.3, 1, and 3 mg/kg) decreases parathyroid hormone and calcium levels in plasma and serum, respectively, in a model of chronic renal insufficiency with secondary hyperthyroidism in nephrectomized rats fed a high-phosphorus diet. Formulations containing etelcalcetide have been used in the treatment of secondary hyperparathyroidism in adult patients with chronic kidney disease undergoing hemodialysis.
1.Harada, K., Fujioka, A., Konno, M., et al.Pharmacology of Parsabiv? (etelcalcetide, ONO-5163/AMG 416), a novel allosteric modulator of the calcium-sensing receptor, for secondary hyperparathyroidism in hemodialysis patientsEur. J. Pharmacol.842139-145(2019)