Etelcalcetide hydrochloride - CAS 1334237-71-6
Catalog number: B0084-475311
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C38H74ClN21O10S2
Molecular Weight:
1084.72
COA:
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Targets:
CaSR
Description:
Etelcalcetide is a calcium-sensing receptor agonist as a D-amino peptide calcimimetic for the treatment of secondary hyperparathyroidism. It can bind to and activate the CaSR (calcium-sensing receptor) in the parathyroid gland as an allosteric activator, resulting in PTH reduction and suppression. Amgen Inc. announced its submission of a New Drug Application to the FDA for etelcalcetide in Aug 2015.
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-475311 10 mg $198 In stock
B0084-475311 25 mg $398 In stock
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Purity:
>98%
Related CAS:
1262780-97-1
Appearance:
Solid Powder
Synonyms:
AMG-416; AMG 416; AMG416; Etelcalcetide hydrochloride; KAI-4169; KAI-4169-HCl; ONO-5163; Parsabiv; Telcalcetide; Velcalcetide; Velcalcetide hydrochloride;N-Acetyl-D-cysteinyl-D-alanyl-D-arginyl-D-arginyl-D-arginyl-D-alanyl-D-argininamide disulfide with L-cysteine hydrochloride;1262780-97-1 (free)
Solubility:
Soluble in DMSO.
Storage:
Store at -20°C
MSDS:
Inquire
InChIKey:
KHQMSZGKHGQUHG-WZDHWKSBSA-N
InChI:
InChI=1S/C38H73N21O10S2.ClH/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);1H/t18-,19-,21+,22-,23-,24-,25-,26-;/m1./s1
Canonical SMILES:
CC(C(=O)NC(CCCN=C(N)N)C(=O)N)NC(=O)C(CCCN=C(N)N)NC(=O)C(CCCN=C(N)N)NC(=O)C(CCCN=C(N)N)NC(=O)C(C)NC(=O)C(CSSCC(C(=O)O)N)NC(=O)C.Cl
Current Developer:
Amgen; Ono Pharmaceuticals
1.AMG 416 (velcalcetide) is a novel peptide for the treatment of secondary hyperparathyroidism in a single-dose study in hemodialysis patients.
Martin KJ;Pickthorn K;Huang S;Block GA;Vick A;Mount PF;Power DA;Bell G Kidney Int. 2014 Jan;85(1):191-7. doi: 10.1038/ki.2013.289. Epub 2013 Jul 31.
AMG 416 (velcalcetide), a novel peptide agonist of the calcium-sensing receptor, lowers plasma parathyroid hormone in preclinical uremic animal models and in normal healthy individuals. Here, we studied its efficacy in hemodialysis patients suffering from secondary hyperparathyroidism. Major inclusion criteria were hemodialysis for at least 3 months, serum parathyroid hormone over 300 pg/ml, a corrected serum calcium of 9.0 mg/dl or more, and stable doses of vitamin D analogs for at least 3 weeks prior to screening. Twenty-eight patients were enrolled in one of five cohorts (5, 10, 20, 40, 60 mg). Cohorts 1-3 (four patients each) were treated in a two-period crossover design, while cohorts 4 and 5 (eight patients each) were randomized 1:1 to AMG 416 or placebo. Patients were admitted to a clinical research unit following hemodialysis and studied for 3 days prior to discharge for hemodialysis. Single intravenous doses of AMG 416 from 5 to 60 mg were well tolerated, and plasma levels increased in a dose-related manner. AMG 416 treatment was associated with significant, dose-dependent reductions in serum parathyroid hormone and fibroblast growth factor 23. Compared with placebo, all dose groups of 10 mg or more were associated with attenuation in the rise in serum phosphate during the interdialytic period.
2.Etelcalcetide for the treatment of secondary hyperparathyroidism.
Hamano N;Komaba H;Fukagawa M Expert Opin Pharmacother. 2017 Apr;18(5):529-534. doi: 10.1080/14656566.2017.1303482. Epub 2017 Mar 15.
Calcium sensing receptor is an important target for the treatment of secondary hyperparathyroidism (SHPT). Etelcalcetide hydrochloride is a novel peptide calcimimetic agent that has a similar mechanism of action as cinacalcet hydrochloride. Clinical trials of etelcalcetide have been performed in the US, Europe, and Japan, and these trials demonstrated the safety and efficacy of etelcalcetide in dialysis patients. Etelcalcetide has recently been approved in Europe, the US and Japan. Areas covered: We review the development, pharmacokinetics, and clinical efficacy and safety of etelcalcetide for the treatment of SHPT in hemodialysis patients. We also summarize the clinical evidence regarding cinacalcet to forecast the potential clinical benefit of etelcalcetide. Expert opinion: Etelcalcetide is an injectable calcimimetic with a longer elimination half-life than cinacalcet. The injectable formulation improves adherence and reduces pill burden, while the frequency of gastrointestinal adverse events has been comparable between cinacalcet and etelcalcetide. The longer half-life of etelcalcetide reduces the fluctuation of biochemical markers of mineral and bone metabolism, but it remains to be determined whether such a sustained effect results in improved outcomes.
3.Pharmacokinetics, Biotransformation, and Excretion of [
Subramanian R;Zhu X;Hock MB;Sloey BJ;Wu B;Wilson SF;Egbuna O;Slatter JG;Xiao J;Skiles GL Clin Pharmacokinet. 2017 Feb;56(2):179-192. doi: 10.1007/s40262-016-0433-0.
Etelcalcetide (AMG 416) is a novel synthetic peptide calcium-sensing receptor activator in clinical development as an intravenous calcimimetic for the treatment of secondary hyperparathyroidism in patients with chronic kidney disease (CKD) on hemodialysis. Etelcalcetide is composed of seven D-aminoacids with an L-cysteine linked to a D-cysteine by a disulfide bond. A single intravenous dose of [;14;C]etelcalcetide (10 mg; 26.3 kBq; 710 nCi) was administered to patients with CKD on hemodialysis to elucidate the pharmacokinetics, biotransformation, and excretion of etelcalcetide in this setting. Blood, dialysate, urine, and feces were collected to characterize the pharmacokinetics, biotransformation product profiles, mass balance, and formation of anti-etelcalcetide antibodies. Accelerator mass spectrometry was necessary to measure the microtracer quantities of C-14 excreted in the large volumes of dialysate and other biomatrices. An estimated 67 % of the [;14;C]etelcalcetide dose was recovered in dialysate, urine, and feces 176 days after dose administration. Etelcalcetide was primarily cleared by hemodialysis, with approximately 60 % of the administered dose eliminated in dialysate.
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