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    Etelcalcetide

    ACTIVE PHARMA INGREDIENTS

    FINISHED DOSAGE FORMULATIONS

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    2D Structure
    Also known as: Velcalcetide, Parsabiv, 1262780-97-1, Kai-4169, Amg-416, Telcalcetide
    Molecular Formula
    C38H73N21O10S2
    Molecular Weight
    1048.3  g/mol
    InChI Key
    ANIAZGVDEUQPRI-ZJQCGQFWSA-N
    FDA UNII
    60ME133FJB
    Etelcalcetide is a calcimimetic and calcium-sensing receptor (CaSR) agonist composed of a synthetic peptide comprised of seven D-amino acids that can be used to treat secondary hyperparathyroidism (sHPT) in hemodialysis patients with chronic kidney disease (CKD). Upon intravenous administration, etelcalcetide mimics calcium and allosterically binds to and activates the CaSR expressed by the parathyroid gland. This suppresses the synthesis and secretion of parathyroid hormone (PTH), thereby reducing PTH levels and lowering serum calcium and phosphorus levels. Elevated PTH is often observed in patients with CKD and is associated with dysregulated calcium-phosphate homeostasis.
    Etelcalcetide is a Calcium-sensing Receptor Agonist. The mechanism of action of etelcalcetide is as an Increased Calcium-sensing Receptor Sensitivity.
    1 2D Structure

    2D Structure

    2 Identification
    2.1 Computed Descriptors
    2.1.1 IUPAC Name
    (2R)-3-[[(2S)-2-acetamido-3-[[(2R)-1-[[(2R)-1-[[(2R)-1-[[(2R)-1-[[(2R)-1-[[(2R)-1-amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-oxopropyl]disulfanyl]-2-aminopropanoic acid
    2.1.2 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
    2.1.3 InChI Key
    ANIAZGVDEUQPRI-ZJQCGQFWSA-N
    2.1.4 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
    2.1.5 Isomeric SMILES
    C[C@H](C(=O)N[C@H](CCCN=C(N)N)C(=O)N)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](C)NC(=O)[C@@H](CSSC[C@@H](C(=O)O)N)NC(=O)C
    2.2 Other Identifiers
    2.2.1 UNII
    60ME133FJB
    2.3 Synonyms
    2.3.1 MeSH Synonyms

    1. Amg 416

    2. Amg-416

    3. Etelcalcetide Hydrochloride

    4. Kai-4169

    5. Parsabiv

    6. Velcalcetide

    2.3.2 Depositor-Supplied Synonyms

    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

    2.4 Create Date
    2013-06-10
    3 Chemical and Physical Properties
    Molecular Weight 1048.3 g/mol
    Molecular Formula C38H73N21O10S2
    XLogP3-10.7
    Hydrogen Bond Donor Count18
    Hydrogen Bond Acceptor Count17
    Rotatable Bond Count36
    Exact Mass1047.52906996 g/mol
    Monoisotopic Mass1047.52906996 g/mol
    Topological Polar Surface Area618 Ų
    Heavy Atom Count71
    Formal Charge0
    Complexity1910
    Isotope Atom Count0
    Defined Atom Stereocenter Count8
    Undefined Atom Stereocenter Count0
    Defined Bond Stereocenter Count0
    Undefined Bond Stereocenter Count0
    Covalently Bonded Unit Count1
    4 Drug and Medication Information
    4.1 Drug Information
    1 of 1  
    Drug NamePARSABIV
    Active IngredientETELCALCETIDE
    CompanyKAI PHARMS INC (Application Number: N208325. Patents: 8377880, 8999932, 9278995, 9701712, 9820938)

    4.2 Drug Indication

    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.

    5 Pharmacology and Biochemistry
    5.1 Pharmacology

    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.

    5.2 FDA Pharmacological Classification
    5.2.1 Active Moiety
    ETELCALCETIDE
    5.2.2 FDA UNII
    60ME133FJB
    5.2.3 Pharmacological Classes
    Increased Calcium-sensing Receptor Sensitivity [MoA]; Calcium-sensing Receptor Agonist [EPC]
    5.3 ATC Code

    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

    5.4 Absorption, Distribution and Excretion

    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

    5.5 Metabolism/Metabolites

    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.

    5.6 Biological Half-Life

    3 to 4 days

    5.7 Mechanism of Action

    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.