Etelcalcetide

Etelcalcetide

Clinical data
Trade names	Parsabiv
Synonyms	Velcalcetide, telcalcetide, AMG-416, KAI-4169, ONO-5163
AHFS/Drugs.com	UK Drug Information
Routes of administration	Intravenous injection
ATC code	H05BX04 (WHO)
Pharmacokinetic data
Biological half-life	3–5 days in dialysis patients
Excretion	60% in dialysate, 7% in urine and faeces
Identifiers
IUPAC name (6R,9R,12R,15R,18R,21R,24S,29R)-24-Acetamido-1,29-diamino-12,15,18-tris(3-carbamimidamidopropyl)-6-carbamoyl-1-imino-9,21-dimethyl-8,11,14,17,20,23-hexaoxo-26,27-dithia-2,7,10,13,16,19,22-heptaazatria contan-30-oic acid
CAS Number	1262780-97-1
PubChem CID	71511839
ChemSpider	32697932
UNII	60ME133FJB
KEGG	D10676
Chemical and physical data
Formula	C38H73N21O10S2
Molar mass	1,048.26 g·mol−1
3D model (JSmol)	Interactive image
SMILES C[C@H](C(=O)N[C@H](CCCNC(=N)N)C(=O)N)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](C)NC(=O)[C@@H](CSSC[C@@H](C(=O)O)N)NC(=O)C
InChI InChI=1S/C38H73N21O10S2/c1-18(28(62)56-22(27(40)61)8-4-12-49-35(41)42)53-30(64)23(9-5-13-50-36(43)44)58-32(66)25(11-7-15-52-38(47)48)59-31(65)24(10-6-14-51-37(45)46)57-29(63)19(2)54-33(67)26(55-20(3)60)17-71-70-16-21(39)34(68)69/h18-19,21-26H,4-17,39H2,1-3H3,(H2,40,61)(H,53,64)(H,54,67)(H,55,60)(H,56,62)(H,57,63)(H,58,66)(H,59,65)(H,68,69)(H4,41,42,49)(H4,43,44,50)(H4,45,46,51)(H4,47,48,52)/t18-,19-,21+,22-,23-,24-,25-,26-/m1/s1 Key:ANIAZGVDEUQPRI-ZJQCGQFWSA-N

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.

Etelcalcetide is used for the treatment of secondary hyperparathyroidism in patients with chronic kidney disease (CKD) on hemodialysis. Hyperparathyroidism is the condition of elevated parathyroid hormone (PTH) levels and is often observed in patients with CKD.

The drug is of course contraindicated in people with blood serum calcium levels below the norm.

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.

No interaction studies in humans were conducted. Studies in vitro showed no affinity of etelcalcetide to enzymes or common transport proteins. Therefore, no relevant pharmacokinetic interactions are expected.

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.

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.