Trade names Parsabiv Routes ofadministration Intravenous injection | AHFS/Drugs.com UK Drug Information ATC code H05BX04 (WHO) | |
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Biological half-life 3–5 days in dialysis patients Excretion 60% in dialysate, 7% in urine and faeces | ||
Etelcalcetide (formerly velcalcetide, trade name Parsabiv) is a calcimimetic drug for the treatment of secondary hyperparathyroidism in patients undergoing hemodialysis. It is administered intravenously at the end of each dialysis session. Etelcalcetide functions by binding to and activating the calcium-sensing receptor in the parathyroid gland.
Contents
Medical uses
Etelcalcetide is used for the treatment of secondary hyperparathyroidism in patients with chronic kidney disease (CKD) on hemodialysis. Hyperparathyroidism is the condition of elevaded parathyroid hormone (PTH) levels and is often observed in patients with CKD.
Contraindications
The drug is of course contraindicated in people with blood serum calcium levels below the norm.
Side effects
Common side effects (in more than 10% of people) are nausea, vomiting, diarrhoea, muscle spasms, and hypocalcaemia (too low blood calcium levels). In clinical studies, the latter side effect was usually mild to moderate and without symptoms. An increase of the QT interval of more than 60 ms was detected in 1.2% of people receiving etelcalcetide.
Interactions
No interaction studies in humans were conducted. Studies in vitro showed no affinity of etelcalcetide to cytochrome P450 enzymes or common transport proteins. Therefore, no relevant pharmacokinetic interactions are expected.
Mechanism of action
Etelcalcetide functions by binding to and activating the calcium-sensing receptor (CaSR) in the parathyroid gland as an allosteric activator, resulting in PTH reduction and suppression.
Chemistry
The substance is a peptide consisting mostly of D-amino acids instead of the common L-amino acids. More specifically, it is the disulfide of N-acetyl-D-cysteinyl-D-alanyl-D-arginyl-D-arginyl-D-arginyl-D-alanyl-D-argininamide with L-cysteine.
History
On 25 August 2015 Amgen Inc. announced its submission of a new drug application to the Food and Drug Administration for etelcalcetide. The European Medicines Agency approved the drug in November 2016.