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1. Amg 416
2. Amg-416
3. Etelcalcetide Hydrochloride
4. Kai-4169
5. Parsabiv
6. Velcalcetide
1. Velcalcetide
2. Parsabiv
3. 1262780-97-1
4. Kai-4169
5. Amg-416
6. Telcalcetide
7. 60me133fjb
8. Ono-5163
9. D-argininamide, N-acetyl-d-cysteinyl-d-alanyl-d-arginyl-d-arginyl-d-arginyl-d-alanyl-, Disulfide With L-cysteine
10. Etelcalcetide [usan:inn]
11. Unii-60me133fjb
12. Kai 4169
13. Amg416
14. Etelcalcetide [mi]
15. Etelcalcetide [inn]
16. Etelcalcetide (usan/inn)
17. Etelcalcetide [usan]
18. Etelcalcetide [who-dd]
19. Gtpl8375
20. Chembl3545184
21. Schembl21982605
22. Dtxsid70155132
23. Chebi:134700
24. Etelcalcetide [orange Book]
25. Hy-p1955
26. Akos037648615
27. Etelcalcetide Hydrochloride(amg-416)
28. Db12865
29. Bs-14875
30. Cs-0030931
31. J3.559.823e
32. D10676
33. D71178
34. Q21098973
35. N-acetyl-d-cysteinyl-d-alanyl-d-arginyl-d-arginyl-d-arginyl-d-alanyl-d-argininamide Disulfide With L-cysteine
36. S-(((s)-2-acetamido-3-(((r)-1-(((r)-1-(((r)-1-(((r)-1-(((r)-1-(((r)-1-amino-5-guanidino-1-oxopentan-2-yl)amino)-1-oxopropan-2-yl)amino)-5-guanidino-1-oxopentan-2-yl)amino)-5-guanidino-1-oxopentan-2-yl)amino)-5-guanidino-1-oxopentan-2-yl)amino)-1-oxopropan-2-yl)amino)-3-oxopropyl)thio)-l-cysteine
Molecular Weight | 1048.3 g/mol |
---|---|
Molecular Formula | C38H73N21O10S2 |
XLogP3 | -10.7 |
Hydrogen Bond Donor Count | 18 |
Hydrogen Bond Acceptor Count | 17 |
Rotatable Bond Count | 36 |
Exact Mass | 1047.52906996 g/mol |
Monoisotopic Mass | 1047.52906996 g/mol |
Topological Polar Surface Area | 618 Ų |
Heavy Atom Count | 71 |
Formal Charge | 0 |
Complexity | 1910 |
Isotope Atom Count | 0 |
Defined Atom Stereocenter Count | 8 |
Undefined Atom Stereocenter Count | 0 |
Defined Bond Stereocenter Count | 0 |
Undefined Bond Stereocenter Count | 0 |
Covalently Bonded Unit Count | 1 |
1 of 1 | |
---|---|
Drug Name | PARSABIV |
Active Ingredient | ETELCALCETIDE |
Company | KAI PHARMS INC (Application Number: N208325. Patents: 8377880, 8999932, 9278995, 9701712, 9820938) |
Etelcalcetide is a calcium-sensing receptor agonist indicated for: Secondary hyperparathyroidism (HPT) in adult patients with chronic kidney disease (CKD) on hemodialysis.
Parsabiv is indicated for the treatment of secondary hyperparathyroidism (SHPT) in adult patients with chronic kidney disease (CKD) on haemodialysis therapy.
Following a single intravenous bolus administration of etelcalcetide, PTH levels decreased within 30 minutes post dose. In the single-dose study, the extent and duration of the reduction in PTH increased with increasing dose. Reduction in PTH levels correlated with plasma etelcalcetide concentrations in hemodialysis patients. The reduction in PTH resulted in reductions in calcium and attenuation of post-dialytic phosphate elevation. The effect of reducing PTH levels was maintained throughout the 6-month dosing period when etelcalcetide was administered by intravenous bolus three times a week.
H05BX04
H05BX04
S76 | LUXPHARMA | Pharmaceuticals Marketed in Luxembourg | Pharmaceuticals marketed in Luxembourg, as published by d'Gesondheetskeess (CNS, la caisse nationale de sante, www.cns.lu), mapped by name to structures using CompTox by R. Singh et al. (in prep.). List downloaded from https://cns.public.lu/en/legislations/textes-coordonnes/liste-med-comm.html. Dataset DOI:10.5281/zenodo.4587355
H - Systemic hormonal preparations, excl. sex hormones and insulins
H05 - Calcium homeostasis
H05B - Anti-parathyroid agents
H05BX - Other anti-parathyroid agents
H05BX04 - Etelcalcetide
Absorption
The pharmacokinetics of etelcalcetide is linear and does not change over time following single (5 to 60 mg) and multiple intravenous doses (2.5 to 20 mg) in chronic kidney disease patients with secondary hyperparathyroidism requiring hemodialysis. Etelcalcetide exhibited tri-exponential decay following intravenous administration. Based on population pharmacokinetic analysis, following three times a week intravenous dosing at the end of each 3- to 6-hour hemodialysis session in chronic kidney disease patients, etelcalcetide plasma levels reached steady state in 7-8 weeks after dosing with a predicted accumulation ratio of 3- to 4-fold
Route of Elimination
Etelcalcetide is cleared by renal excretion
Volume of Distribution
796 L
Clearance
7.66 L/hr
Etelcalcetide is not metabolized by CYP450 enzymes. Etelcalcetide is biotransformed in blood by reversible disulfide exchange with endogenous thiols to predominantly form conjugates with serum albumin. Following a single radiolabeled dose of etelcalcetide in chronic kidney disease patients with secondary hyperparathyroidism requiring hemodialysis, the plasma exposure of biotransformation products is approximately 5-fold higher than that of etelcalcetide and their concentration-time course parallels that of etelcalcetide.
3 to 4 days
Etelcalcetide is a calcimimetic agent that allosterically modulates the calcium-sensing receptor (CaSR). Etelcalcetide binds to the CaSR and enhances activation of the receptor by extracellular calcium. Activation of the CaSR on parathyroid chief cells decreases PTH secretion.