Etelcalcetide

Structural formula
General
Non-proprietary name	Etelcalcetide
Molecular formula	C 38 H 73 N 21 O 10 S 2
External identifiers / databases
CAS number 1262780-97-1 PubChem 71511839 DrugBank DB12865 Wikidata Q21098973
Drug information
ATC code	H05 BX04
Drug class	Calcium receptor modulators
properties
Molar mass	1048.25 g mol −1
safety instructions
Please note the exemption from the labeling requirement for drugs, medical devices, cosmetics, food and animal feed GHS hazard labeling no classification available
As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions .

Etelcalcetide is a drug used to treat secondary hyperparathyroidism , a disease that occurs mainly in people with chronic kidney disease and leads to elevated levels of parathyroid hormone .

Drug structure and pharmacokinetics

Etelcalcetide consists of a peptide of seven D - amino acids that form the basic structure of the molecule in a linear chain. A D - cysteine is linked to an L - cysteine via a disulfide group:

Ac-DCys-DAla-DArg-DArg-DArg-DAla-DArg-NH2
     |
  H-LCys-OH

The molecular weight of the active ingredient is 1048.3 Da . The drug is metabolized through disulfide exchange with thiol-containing molecules in the body and takes place less through enzymes . Laboratory tests did not show any effect on the important cytochrome P450 metabolism. In human blood, the drug binds covalently to the blood protein albumin via a disulfide bond . The drug is excreted through the kidneys and, in dialysis patients, removed from the blood by hemodialysis.

Drug effect

Etelcalcetide is an allosteric modulator of the calcium- sensitive receptor on the parathyroid gland. Like other drugs in its class of active ingredients, the drug increases the sensitivity of the receptor by binding, which in turn reduces the downstream parathyroid hormone production. The administration of the drug is intravenous. Two randomized and controlled prospective studies were able to demonstrate a comparable effect with the orally administered drug Cinacalcet .

Admission status

• European Union : On November 11, 2016, etelcalcetide was approved for the treatment of secondary hyperparathyroidism in adult patients with chronic kidney disease undergoing hemodialysis therapy.
• USA: The American FDA approved etelcalcetide on February 7, 2017.

Individual evidence

1. ↑ This substance has either not yet been classified with regard to its hazardousness or a reliable and citable source has not yet been found.
2. ^ Raju Subramanian, Xiaochun Zhu, Savannah J. Kerr, Joel D. Esmay, Steven W. Louie: Nonclinical Pharmacokinetics and Disposition of Etelcalcetide. In: Drug Metabolism and Disposition . August 2016, 44 (8), pp. 1319-1331; doi: 10.1124 / dmd.115.068007 .
3. ^ Edson concentration camp, BM Wu, A. Iyer, W. Goodman: Determination of Etelcalcetide Biotransformation and Hemodialysis Kinetics to Guide the Timing of Its Dosing. In: Kidney International Reports. May 2016, 1 (1), pp. 24–33, doi: 10.1016 / j.ekir.2016.04.002 .
4. ↑ Geoffrey A. Block, David A. Bushinsky, John Cunningham, et al .: Effect of Etelcalcetide vs Placebo on Serum Parathyroid Hormone in Patients Receiving Hemodialysis With Secondary Hyperparathyroidism: Two Randomized Clinical Trials. In: JAMA . 2017, 317 (2), pp. 146–155, doi: 10.1001 / jama.2016.19456 .
5. ^ European Medicines Agency - Find medicine - Parsabiv. Retrieved January 12, 2018 . 
6. ↑ Center for Drug Evaluation and Research: Drug Innovation - Novel Drug Approvals for 2017. Accessed January 12, 2018 . 

This article is about a health issue. It is not used for self-diagnosis and does not replace a diagnosis by a doctor. Please note the information on health issues !