etelcalcetide 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
peptides and glycopeptides 5181 1262780-97-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • etelcalcetide
  • parsabiv
  • AMG 416
  • KAI-4169
  • etelcalcetide hydrochloride
  • etelcalcetide HCl
  • velcalcetide
  • velcalcetide hydrochloride
Etelcalcetide is a synthetic peptide calcimimetic agent which reduces parathyroid hormone (PTH) secretion through binding and activation of the calcium-sensing receptor. The reduction in PTH is associated with a concomitant decrease in serum calcium and phosphate levels.
  • Molecular weight: 1048.26
  • Formula: C38H73N21O10S2
  • CLOGP: -11.73
  • LIPINSKI: 3
  • HAC: 31
  • HDO: 22
  • TPSA: 557.71
  • ALOGS: -3.90
  • ROTB: 36
  • Status: ONP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
2.10 mg P

ADMET properties:

PropertyValueReference
Vd (Volume of distribution) 1.98 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 1.67 mL/min/kg Lombardo F, Berellini G, Obach RS
t_half (Half-life) 19.05 hours Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System) 3 Bocci G, Oprea TI, Benet LZ

Approvals:

DateAgencyCompanyOrphan
Nov. 11, 2016 EMA Amgen Europe B.V.
Feb. 7, 2017 FDA KAI PHARMS INC

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Shunt stenosis 649.53 40.07 85 1723 455 63486759
Shunt occlusion 384.43 40.07 55 1753 610 63486604
Underdose 349.77 40.07 92 1716 27364 63459850
Blood parathyroid hormone increased 181.56 40.07 36 1772 3002 63484212
Blood calcium decreased 136.25 40.07 44 1764 26407 63460807
Hypocalcaemia 97.92 40.07 36 1772 31677 63455537
Blood parathyroid hormone abnormal 78.10 40.07 12 1796 220 63486994
Peripheral arterial occlusive disease 52.85 40.07 14 1794 4187 63483027
Shunt infection 49.32 40.07 7 1801 72 63487142
Shunt malfunction 48.97 40.07 7 1801 76 63487138
Nausea 46.70 40.07 85 1723 854386 62632828
Pemphigoid 45.12 40.07 14 1794 7330 63479884
Angina unstable 41.38 40.07 13 1795 7082 63480132

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Shunt stenosis 813.64 42.19 118 1907 664 34954242
Shunt occlusion 452.39 42.19 72 1953 798 34954108
Underdose 290.96 42.19 80 1945 13700 34941206
Blood parathyroid hormone increased 287.20 42.19 53 1972 1461 34953445
Peripheral arterial occlusive disease 195.45 42.19 49 1976 5825 34949081
Hypocalcaemia 167.44 42.19 60 1965 24229 34930677
Blood calcium decreased 117.41 42.19 37 1988 10047 34944859
Shunt aneurysm 59.23 42.19 8 2017 23 34954883
Angina unstable 58.95 42.19 23 2002 11630 34943276
Blood calcium abnormal 58.86 42.19 12 2013 556 34954350
Shunt infection 57.07 42.19 9 2016 92 34954814
Blood parathyroid hormone abnormal 46.01 42.19 8 2017 154 34954752
Cerebral infarction 42.85 42.19 24 2001 27431 34927475

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Shunt stenosis 1477.32 40.85 203 2858 1188 79740139
Shunt occlusion 853.14 40.85 127 2934 1377 79739950
Underdose 295.87 40.85 90 2971 33061 79708266
Peripheral arterial occlusive disease 271.36 40.85 63 2998 8195 79733132
Hypocalcaemia 232.78 40.85 83 2978 49841 79691486
Blood parathyroid hormone increased 183.16 40.85 39 3022 3406 79737921
Angina unstable 110.23 40.85 36 3025 16491 79724836
Shunt infection 105.39 40.85 16 3045 196 79741131
Blood calcium decreased 94.07 40.85 38 3023 31781 79709546
Shunt aneurysm 85.87 40.85 11 3050 32 79741295
Cerebral infarction 80.86 40.85 38 3023 45638 79695689
Cardiac failure 67.08 40.85 52 3009 154790 79586537
Myocardial ischaemia 57.06 40.85 25 3036 25494 79715833
Aortic valve stenosis 54.10 40.85 16 3045 5278 79736049
Calciphylaxis 45.65 40.85 13 3048 3757 79737570

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC H05BX04 SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS
CALCIUM HOMEOSTASIS
ANTI-PARATHYROID AGENTS
Other anti-parathyroid agents
FDA MoA N0000020081 Increased Calcium-sensing Receptor Sensitivity
FDA EPC N0000175902 Calcium-sensing Receptor Agonist

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Secondary hyperparathyroidism indication 91478007 DOID:12466




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 1.83 acidic
pKa2 12.62 acidic
pKa3 13.21 acidic
pKa4 13.22 acidic
pKa5 13.76 acidic
pKa6 13.85 acidic
pKa7 11.35 Basic
pKa8 10.93 Basic
pKa9 10.57 Basic
pKa10 10.15 Basic
pKa11 8.46 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
10MG/2ML (5MG/ML) PARSABIV KAI PHARMS INC N208325 Feb. 7, 2017 RX SOLUTION INTRAVENOUS 9701712 July 29, 2030 A METHOD OF TREATING SECONDARY HYPERPARATHYROIDISM (SHPT)
2.5MG/0.5ML (2.5MG/0.5ML) PARSABIV KAI PHARMS INC N208325 Feb. 7, 2017 RX SOLUTION INTRAVENOUS 9701712 July 29, 2030 A METHOD OF TREATING SECONDARY HYPERPARATHYROIDISM (SHPT)
5MG/ML (5MG/ML) PARSABIV KAI PHARMS INC N208325 Feb. 7, 2017 RX SOLUTION INTRAVENOUS 9701712 July 29, 2030 A METHOD OF TREATING SECONDARY HYPERPARATHYROIDISM (SHPT)
10MG/2ML (5MG/ML) PARSABIV KAI PHARMS INC N208325 Feb. 7, 2017 RX SOLUTION INTRAVENOUS 8999932 Feb. 7, 2031 A METHOD OF TREATING SECONDARY HYPERPARATHYROIDISM (SHPT)
2.5MG/0.5ML (2.5MG/0.5ML) PARSABIV KAI PHARMS INC N208325 Feb. 7, 2017 RX SOLUTION INTRAVENOUS 8999932 Feb. 7, 2031 A METHOD OF TREATING SECONDARY HYPERPARATHYROIDISM (SHPT)
5MG/ML (5MG/ML) PARSABIV KAI PHARMS INC N208325 Feb. 7, 2017 RX SOLUTION INTRAVENOUS 8999932 Feb. 7, 2031 A METHOD OF TREATING SECONDARY HYPERPARATHYROIDISM (SHPT)

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Extracellular calcium-sensing receptor GPCR AGONIST EC50 4.60 IUPHAR DRUG LABEL

External reference:

IDSource
60ME133FJB UNII
1334237-71-6 SECONDARY_CAS_RN
4037030 VANDF
C3713906 UMLSCUI
CHEBI:134700 CHEBI
CHEMBL3545184 ChEMBL_ID
D10676 KEGG_DRUG
71511839 PUBCHEM_CID
DB12865 DRUGBANK_ID
CHEMBL3545183 ChEMBL_ID
9809 INN_ID
8375 IUPHAR_LIGAND_ID
1876119 RXNORM
251837 MMSL
32350 MMSL
33154 MMSL
d08523 MMSL
017097 NDDF
017098 NDDF
1156090004 SNOMEDCT_US
723539000 SNOMEDCT_US
763584002 SNOMEDCT_US
C583569 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
PARSABIV HUMAN PRESCRIPTION DRUG LABEL 1 55513-740 INJECTION, SOLUTION 2.50 mg INTRAVENOUS NDA 28 sections
PARSABIV HUMAN PRESCRIPTION DRUG LABEL 1 55513-740 INJECTION, SOLUTION 2.50 mg INTRAVENOUS NDA 28 sections
PARSABIV HUMAN PRESCRIPTION DRUG LABEL 1 55513-741 INJECTION, SOLUTION 5 mg INTRAVENOUS NDA 28 sections
PARSABIV HUMAN PRESCRIPTION DRUG LABEL 1 55513-741 INJECTION, SOLUTION 5 mg INTRAVENOUS NDA 28 sections
PARSABIV HUMAN PRESCRIPTION DRUG LABEL 1 55513-742 INJECTION, SOLUTION 10 mg INTRAVENOUS NDA 28 sections
PARSABIV HUMAN PRESCRIPTION DRUG LABEL 1 55513-742 INJECTION, SOLUTION 10 mg INTRAVENOUS NDA 28 sections