|Other names||Velcalcetide, telcalcetide, AMG-416, KAI-4169, ONO-5163|
|Main uses||Secondary hyperparathyroidism in people on hemodialysis|
|Side effects||Low calcium, muscle spasms, diarrhea, nausea|
|Elimination half-life||3–5 days in dialysis patients|
|Excretion||60% in dialysate, 7% in urine and faeces|
|Chemical and physical data|
|Molar mass||1048.26 g·mol−1|
|3D model (JSmol)|
Etelcalcetide, sold under the brand name Parsabiv, is a medication used to treat secondary hyperparathyroidism in people undergoing hemodialysis. It is unclear if it changes outcomes such as life expectancy and heart disease. It is given by injection into a vein at the end of each dialysis session.
Common side effects include low calcium, muscle spasms, diarrhea, and nausea. Other side effects may include allergic reactions, heart failure, upper GI bleeding, and adynamic bone disease. It is a calcimimetic and works by activating calcium-sensing receptors in the parathyroid gland.
Etelcalcetide was approved for medical use in Europe in 2016 and the United States in 2017. In the United Kingdom a dose of 5 mg three times per week costs the NHS about £330 for 4 weeks as of 2021. In the United States this amount costs about 2,100 USD.
Etelcalcetide is used for the treatment of secondary hyperparathyroidism in people with chronic kidney disease (CKD) on hemodialysis. Hyperparathyroidism is the condition of elevated parathyroid hormone (PTH) levels and is often observed in people with CKD.
Mechanism of action
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.
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.
Due to the lower iPTH levels achieved by the use of this drug, it is possible that adynamic bone disease could occur at levels "below 100 pg/mL"
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.
Originally, Etelcalcetide was being developed by KAI Pharmaceuticals. After positive Phase II trials, Amgen acquired KAI for $315 Million.
In 2011, KAI entered into agreement with Ono Pharmaceutical for production of etelcalcetide in Japan, the deal being worth ¥1 Billion.
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.
In February 2017, the FDA approved Parsabiv for the treatment of secondary hyperparathyroidism.
Society and culture
Phase II trials found that Etelcalcetide was able to lower PTH levels in one cohort by -49% vs a 29% increase in the placebo group. In another Phase II study "89% of patients experienced a C30% reduction in PTH and 56% achieved a PTH level of B300 pg/mL."
Phase I Pediatric studies are planned for the USA and UK for etelcalcetide.
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