生物活性

• 描述Etelcalcetide is a positive allosteric modulator/peptide agonist of the CaR with EC50 value of 25μM for increasing IP1 accumulation in HEK-293 cells expressing the human CaR. It is approved for the treatment of secondary hyperpara-thyroidism in adults with chronic kidney disease on hemodialysis. The efficacy in vivo of Etelcalcetide is usually measured by the magnitude and duration of decreases in plasma plasma parathyroid hormone (PTH) levels. For example, a single dose of etelcalcetide at 0.5mg/kg caused a substantial drop in PTH levels in rats with acute renal dysfunction (1K1C model), and this effect by etelcalcetide remained approximately 50% below their initial level at 24 hrs.
• 作用机制Etelcalcetide forms a covalent disulphide bond with the CaR.
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT03283098	Secondary Hyperparathyroidism	Phase 1	Recruiting	January 23, 2019	China, Beijing ... more >> Research Site Recruiting Beijing, Beijing, China, 100044 China, Jiangsu Research Site Recruiting Nanjing, Jiangsu, China, 210029 China, Shanghai Research Site Recruiting Shanghai, Shanghai, China, 200032 Research Site Recruiting Shanghai, Shanghai, China, 200040 Research Site Recruiting Shanghai, Shanghai, China, 200127 Collapse <<
  NCT03527511	-	-	Recruiting	May 14, 2020	France ... more >> Service de Néphrologie, Rhumatologie et Dermatologie Pédiatriques - Hôpital Femme Mère Enfant - Bron. Recruiting Bron, France, 69677 Contact: Justine BACCHETTA, Pr    04 27 85 61 30 ext +33    justine.bacchetta@chu-lyon.fr    Principal Investigator: Justine BACCHETTA, Pr          Sub-Investigator: Bruno RANCHIN, Dr          Sub-Investigator: Anne-Laure SELIER-LECLERC, Dr          Sub-Investigator: Aurélia BERTHOLET-THOMAS, Dr          Sub-Investigator: Elodie CHEYSSAC, Dr          Sub-Investigator: Corentin TANNE, Dr Collapse <<
  NCT03182699	Secondary Hyperparathyroidism ... more >> Chronic Kidney Disease Requiring Chronic Dialysis Left Ventricular Hypertrophy Collapse <<	Phase 4	Recruiting	December 1, 2020	Austria ... more >> Medical University of Vienna Recruiting Vienna, Austria, 1090 Contact: Rainer Oberbauer, Univ.Prof.    004314040043910    rainer.oberbauer@meduniwien.ac.at    Contact: Katharina Doerr, Dr.    004369911966793    Katharina.doerr@meduniwien.ac.at    Wiener Dialysezentrum Recruiting Vienna, Austria, 1220 Contact: Matthias Lorenz, Priv.Doz.    0043 1 908 13 10    matthias.lorenz@dialysewien.at Collapse <<

• 更多
• 参考文献

• [1] Block GA, Bushinsky DA, et al. Effect of Etelcalcetide vs Cinacalcet on Serum Parathyroid Hormone in Patients Receiving Hemodialysis With Secondary Hyperparathyroidism: A Randomized Clinical Trial. JAMA. 2017 Jan 10;317(2):156-164.

  [2] Subramanian R, Zhu X, et al. Nonclinical Pharmacokinetics, Disposition, and Drug-Drug Interaction Potential of a Novel d-Amino Acid Peptide Agonist of the Calcium-Sensing Receptor AMG 416 (Etelcalcetide). Drug Metab Dispos. 2016 Aug;44(8):1319-31.