Inoue Atsuto, Harada Kazutsune
ONO Pharmaceutical Co., Ltd, Research Headquarter, Research Promotion, Japan.
ONO Pharmaceutical Co., Ltd, Research Headquarter, Discovery Research Laboratory, Japan.
Clin Calcium. 2017;27(4):537-545.
Etelcalcetide hydrochloride is the first intravenous calcimimetics agent for secondary hyperparathyroidism (SHPT). Etelcalcetide hydrochloride is to be administered through dialysis circuit by physician or medical staff upon completion of dialysis and such administration is expected to reduce the burden of medication in patients. From the nonclinical study results, etelcalcetide functions as an allosteric activator of calcium-sensing receptor(CaSR). Etelcalcetide suppressed PTH secretion both in vitro and in vivo. In a rat model of chronic renal insufficiency, etelcalcetide suppressed SHPT disorders, such as parathyroid gland hypertrophy, bone disorder, and ectopic calcification. In conclusion, etelcalcetide hydrochloride is expected to exhibit therapeutic effect against each SHPT condition by decreasing blood PTH concentrations via CaSR-agonist activity in the clinical situation.
盐酸依特卡肽是首个用于继发性甲状旁腺功能亢进症（SHPT）的静脉注射拟钙剂。盐酸依特卡肽由医生或医护人员在透析结束后通过透析回路给药，预计这种给药方式可减轻患者的用药负担。从非临床研究结果来看，依特卡肽作为钙敏感受体（CaSR）的变构激活剂发挥作用。依特卡肽在体外和体内均能抑制甲状旁腺激素（PTH）分泌。在慢性肾功能不全大鼠模型中，依特卡肽可抑制SHPT相关病症，如甲状旁腺肥大、骨病症和异位钙化。总之，在临床情况下，预计盐酸依特卡肽可通过CaSR激动剂活性降低血PTH浓度，从而对各SHPT病症发挥治疗作用。
