etelcalcetide 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2A,ACVR2B,ACVRL1,AKT1,AKT2,AKT3,ALK,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,CHUK,CSF1R,DDR1,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,FGFR1,FLT3,GRK2,GSK3B,IGF1R,IKBKB,ITK,JAK1,JAK2,JAK3,MAP2K1,MAP2K6,MAP3K14,MAP3K21,MAP3K7,MAP4K1,MAPK10,MAPK7,MAPK9,MAPKAPK2,MET,MTOR,NTRK2,PAK4,PDK1,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PLK1,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK,ULK1,ZAP70 66
kinase-selectivity-class GRK2,PDK1 2
pfas-class PFAS structural alert (1 = True, 0 = False) 0

Approvals:

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

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 674.23 41.48 85 1778 474 90626110
Shunt occlusion 393.91 41.48 55 1808 720 90625864
Underdose 317.74 41.48 92 1771 53925 90572659
Blood parathyroid hormone increased 188.83 41.48 36 1827 3401 90623183
Blood calcium decreased 153.25 41.48 46 1817 30136 90596448
Hypocalcaemia 110.53 41.48 39 1824 42329 90584255
Blood parathyroid hormone abnormal 80.92 41.48 12 1851 242 90626342
Peripheral arterial occlusive disease 56.05 41.48 14 1849 4607 90621977
Pemphigoid 55.57 41.48 16 1847 9010 90617574
Nausea 53.37 41.48 87 1776 1110229 89516355
Shunt malfunction 50.92 41.48 7 1856 80 90626504
Shunt infection 48.17 41.48 7 1856 122 90626462
Angina unstable 45.48 41.48 13 1850 7130 90619454
Cardiac failure 45.02 41.48 28 1835 109468 90517116
Calciphylaxis 44.83 41.48 11 1852 3365 90623219

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 831.41 40.82 118 2016 659 42618542
Shunt occlusion 443.60 40.82 71 2063 956 42618245
Blood parathyroid hormone increased 294.82 40.82 55 2079 1872 42617329
Underdose 287.36 40.82 80 2054 16586 42602615
Hypocalcaemia 189.60 40.82 67 2067 30106 42589095
Peripheral arterial occlusive disease 185.19 40.82 47 2087 6791 42612410
Blood calcium decreased 123.41 40.82 38 2096 11070 42608131
Shunt aneurysm 60.40 40.82 8 2126 23 42619178
Angina unstable 58.93 40.82 22 2112 11426 42607775
Blood calcium abnormal 57.34 40.82 12 2122 734 42618467
Shunt infection 56.04 40.82 9 2125 122 42619079
Blood parathyroid hormone abnormal 46.16 40.82 8 2126 176 42619025
Parathyroid gland enlargement 46.11 40.82 8 2126 177 42619024

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 1529.71 39.07 203 3013 1213 110584870
Shunt occlusion 862.10 39.07 126 3090 1611 110584472
Hypocalcaemia 272.00 39.07 93 3123 65273 110520810
Peripheral arterial occlusive disease 270.51 39.07 61 3155 9219 110576864
Underdose 262.77 39.07 90 3126 63464 110522619
Blood parathyroid hormone increased 197.38 39.07 41 3175 4207 110581876
Angina unstable 115.95 39.07 35 3181 16397 110569686
Blood calcium decreased 110.85 39.07 41 3175 35804 110550279
Shunt infection 105.10 39.07 16 3200 269 110585814
Shunt aneurysm 88.92 39.07 11 3205 32 110586051
Cerebral infarction 83.12 39.07 37 3179 51801 110534282
Cardiac failure 71.03 39.07 52 3164 187574 110398509
Myocardial ischaemia 62.68 39.07 25 3191 26659 110559424
Aortic valve stenosis 55.61 39.07 16 3200 6334 110579749
Calciphylaxis 52.58 39.07 14 3202 4173 110581910
Parathyroid gland enlargement 49.07 39.07 8 3208 212 110585871
Fall 44.83 39.07 70 3146 603412 109982671
Sudden death 44.23 39.07 19 3197 24376 110561707
Hypercalcaemia 43.53 39.07 23 3193 46634 110539449
Bile duct stone 42.64 39.07 13 3203 6276 110579807
Large intestine polyp 41.99 39.07 16 3200 15101 110570982

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

Related Drugs by ATC class:

H05BX Other anti-parathyroid agents 5 drugs
calcifediolcinacalcetdoxercalciferolevocalcetparicalcitol

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)
10MG/2ML (5MG/ML) PARSABIV KAI PHARMS INC N208325 Feb. 7, 2017 RX SOLUTION INTRAVENOUS 11959486 June 27, 2034 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 11959486 June 27, 2034 A METHOD OF TREATING SECONDARY HYPERPARATHYROIDISM (SHPT)
5MG/ML (5MG/ML) PARSABIV KAI PHARMS INC N208325 Feb. 7, 2017 RX SOLUTION INTRAVENOUS 11959486 June 27, 2034 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
C583569 MESH_SUPPLEMENTAL_RECORD_UI
8375 IUPHAR_LIGAND_ID
1156090004 SNOMEDCT_US
723539000 SNOMEDCT_US
763584002 SNOMEDCT_US
251837 MMSL
32350 MMSL
33154 MMSL
d08523 MMSL
017097 NDDF
017098 NDDF
1876119 RXNORM
60ME133FJB INXIGHT DRUGS

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