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Etelcalcetide is a calcimimetic agent used for the treatment of secondary hyperparathyroidism in patients chronic kidney disease (CKD) undergoing hemodialysis. It effects via binding to and stimulating the calcium-sensing receptor in the parathyroid gland.

Peptide Inhibitors
Catalog number
CAS number
Molecular Formula
Molecular Weight
(2R)-3-[[(2S)-2-acetamido-3-[[(2R)-1-[[(2R)-1-[[(2R)-1-[[(2R)-1-[[(2R)-1-[[(2R)-1-amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-oxopropyl]disulfanyl]-2-aminopropanoic acid
Velcalcetide; telcalcetide; AMG-416; KAI-4169; ONO-5163; Parsabiv
Related CAS
1334237-71-6 (hydrochloride)
1.58±0.1 g/cm3(Predicted)
Store at -20°C
the treatment of secondary hyperparathyroidism
InChI Key
Canonical SMILES
1.Insulin Degludec/Liraglutide.
Baker DE Hosp Pharm. 2017 May;52(5):374-380. doi: 10.1177/0018578717715383. Epub 2017 May 1.
Each month, subscribers to ;The Formulary Monograph Service; receive 5 to 6 well-documented monographs on drugs that are newly released or are in late phase 3 trials. The monographs are targeted to Pharmacy & Therapeutics Committees. Subscribers also receive monthly 1-page summary monographs on agents that are useful for agendas and pharmacy/nursing in-services. A comprehensive target drug utilization evaluation/medication use evaluation (DUE/MUE) is also provided each month. With a subscription, the monographs are available online to subscribers. Monographs can be customized to meet the needs of a facility. Through the cooperation of ;The Formulary, Hospital Pharmacy; publishes selected reviews in this column. For more information about ;The Formulary Monograph Service;, contact Wolters Kluwer customer service at 866-397-3433. The May 2017 monograph topics are brodalumab, etelcalcetide, guselkumab, ribociclib, and sirukumab. The MUE is on ribociclib.
2.Critical Cysteine Residues in Both the Calcium-Sensing Receptor and the Allosteric Activator AMG 416 Underlie the Mechanism of Action.
Alexander ST;Hunter T;Walter S;Dong J;Maclean D;Baruch A;Subramanian R;Tomlinson JE Mol Pharmacol. 2015 Nov;88(5):853-65. doi: 10.1124/mol.115.098392. Epub 2015 Aug 19.
AMG 416 is a novel D-amino acid-containing peptide agonist of the calcium-sensing receptor (CaSR) that is being evaluated for the treatment of secondary hyperparathyroidism in chronic kidney disease patients receiving hemodialysis. The principal amino acid residues and their location in the CaSR that accommodate AMG 416 binding and mode of action have not previously been reported. Herein we establish the importance of a pair of cysteine residues, one from AMG 416 and the other from the CaSR at position 482 (Cys482), and correlate the degree of disulfide bond formation between these residues with the pharmacological activity of AMG 416. KP-2067, a form of the CaSR agonist peptide, was included to establish the role of cysteine in vivo and in disulfide exchange. Studies conducted with AMG 416 in pigs showed a complete lack of pharmacodynamic effect and provided a foundation for determining the peptide agonist interaction site within the human CaSR. Inactivity of AMG 416 on the pig CaSR resulted from a naturally occurring mutation encoding tyrosine for cysteine (Cys) at position 482 in the pig CaSR. Replacing Cys482 in the human CaSR with serine or tyrosine ablated AMG 416 activity. Decidedly, a single substitution of cysteine for tyrosine at position 482 in the native pig CaSR provided a complete gain of activity by the peptide agonist.
3.Population Pharmacokinetic and Pharmacodynamic Modeling of Etelcalcetide in Patients with Chronic Kidney Disease and Secondary Hyperparathyroidism Receiving Hemodialysis.
Chen P;Narayanan A;Wu B;Gisleskog PO;Gibbs JP;Chow AT;Melhem M Clin Pharmacokinet. 2018 Jan;57(1):71-85. doi: 10.1007/s40262-017-0550-4.
INTRODUCTION: ;Etelcalcetide is a novel calcimimetic that binds and activates calcium-sensing receptors (CaSRs) for the treatment of secondary hyperparathyroidism (SHPT).;METHODS: ;To assess titrated dosing regimens, population pharmacokinetic (PK) and PK/pharmacodynamic (PKPD) modeling of etelcalcetide was performed using NONMEM 7.2. In this analysis, plasma etelcalcetide, serum parathyroid hormone (PTH) and calcium (Ca) concentration-time data were collected from five phase I, II, and III clinical trials following single or multiple intravenous doses of etelcalcetide ranging from 2.5 to 60 mg. A semi-mechanistic model was used to describe the relationship between etelcalcetide, PTH, and Ca. This model included the role of PTH in Ca regulation, the feedback of Ca onto PTH production via the CaSR, and the activity of etelcalcetide plasma levels in increasing the sensitivity of the CaSR to Ca via the cooperative binding model. The impact of relevant covariates was evaluated by stepwise forward/backward selection. Model evaluation was based on standard goodness-of-fit plots and prediction-corrected visual predictive checks (pcVPCs). Simulation was conducted to evaluate titrated dosing regimens.
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