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

Stem definitionDrug idCAS RN
Vitamin D analogues/derivatives 2066 131918-61-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • zemplar
  • paricalcitol-d6
  • paricalcitol
suppressed immunoglobulin production & thymic lymphocyte proliferation in vivo
  • Molecular weight: 416.65
  • Formula: C27H44O3
  • CLOGP: 5.69
  • LIPINSKI: 1
  • HAC: 3
  • HDO: 3
  • TPSA: 60.69
  • ALOGS: -4.79
  • ROTB: 5
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
2 mcg O
2 mcg P

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 0 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.00 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 72 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 0.41 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 0.89 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.00 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 5.30 hours Lombardo F, Berellini G, Obach RS

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2B,BRAF,CAMK2D,CDK5,EIF2AK3,ERBB2,GRK2,ITK,MAPK7,NTRK2,PDK1,PDK2,PDK4,PRKDC,TEK 15
kinase-selectivity-class PDK2 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0

Approvals:

DateAgencyCompanyOrphan
April 17, 1998 FDA ABBVIE

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
Death 3386.28 25.31 1262 5826 455289 90166070
Cardiac disorder 500.20 25.31 182 6906 56690 90564669
Infarction 346.33 25.31 73 7015 2940 90618419
Sepsis 261.96 25.31 167 6921 179647 90441712
Myocardial infarction 193.92 25.31 114 6974 105858 90515501
Cardio-respiratory arrest 179.63 25.31 91 6997 63049 90558310
Cardiac failure 172.46 25.31 107 6981 109389 90511970
Calciphylaxis 161.20 25.31 40 7048 3336 90618023
Cardiovascular disorder 159.76 25.31 54 7034 13438 90607921
Respiratory arrest 153.46 25.31 67 7021 33244 90588115
Nephrogenic systemic fibrosis 134.29 25.31 36 7052 4072 90617287
Adverse event 127.37 25.31 91 6997 117327 90504032
Cerebrovascular disorder 93.65 25.31 25 7063 2781 90618578
Blood parathyroid hormone increased 88.63 25.31 25 7063 3412 90617947
Skin induration 85.35 25.31 24 7064 3238 90618121
Acute myocardial infarction 83.98 25.31 45 7043 34845 90586514
Renal transplant 75.57 25.31 19 7069 1669 90619690
Skin hypertrophy 69.81 25.31 21 7067 3589 90617770
Skin tightness 69.42 25.31 22 7066 4466 90616893
Chronic kidney disease 68.81 25.31 45 7043 50146 90571213
Cerebrovascular accident 64.99 25.31 63 7025 123470 90497889
Peritonitis bacterial 58.45 25.31 20 7068 5151 90616208
Cardiac arrest 48.68 25.31 50 7038 104885 90516474
Peritoneal dialysis complication 45.34 25.31 12 7076 1290 90620069
Skin fibrosis 44.79 25.31 11 7077 877 90620482
Hyperphosphataemia 44.48 25.31 15 7073 3696 90617663
Blood parathyroid hormone abnormal 40.01 25.31 8 7080 246 90621113
Device related infection 39.99 25.31 25 7063 25761 90595598
Arteriovenous fistula thrombosis 39.73 25.31 8 7080 255 90621104
Transplant 38.12 25.31 10 7078 1039 90620320
Drug ineffective 37.68 25.31 32 7056 1384266 89237093
Parathyroidectomy 37.50 25.31 8 7080 340 90621019
Haemorrhagic stroke 36.30 25.31 15 7073 6481 90614878
Shunt occlusion 36.07 25.31 9 7079 766 90620593
Off label use 35.85 25.31 21 7067 1102231 89519128
Acute pulmonary oedema 33.75 25.31 16 7072 9564 90611795
Hypercalcaemia 33.56 25.31 25 7063 34215 90587144
Device related sepsis 33.49 25.31 13 7075 4780 90616579
Joint contracture 33.22 25.31 10 7078 1712 90619647
Azotaemia 32.11 25.31 13 7075 5335 90616024
Pemphigoid 31.57 25.31 15 7073 9011 90612348
Fibrosis 30.76 25.31 13 7075 5939 90615420
Osteomalacia 29.98 25.31 8 7080 887 90620472
Sudden death 28.87 25.31 15 7073 10894 90610465
Unevaluable event 28.86 25.31 28 7060 54820 90566539
Arteriovenous fistula operation 28.26 25.31 6 7082 249 90621110
Pulmonary sepsis 26.67 25.31 9 7079 2222 90619137
Sudden cardiac death 26.66 25.31 9 7079 2223 90619136

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
Death 3930.94 27.17 1859 6868 469326 42143282
Cardiac disorder 724.40 27.17 297 8430 48635 42563973
Infarction 497.24 27.17 117 8610 2918 42609690
Myocardial infarction 347.77 27.17 249 8478 123760 42488848
Cardiovascular disorder 227.55 27.17 90 8637 13275 42599333
Adverse event 208.18 27.17 100 8627 23540 42589068
Sepsis 178.13 27.17 211 8516 199123 42413485
Cardiac failure 167.44 27.17 153 8574 106703 42505905
Respiratory arrest 162.69 27.17 90 8637 28334 42584274
Cardio-respiratory arrest 152.94 27.17 113 8614 58523 42554085
Transplant 131.41 27.17 32 8695 922 42611686
Calciphylaxis 129.76 27.17 33 8694 1140 42611468
Renal transplant 118.78 27.17 36 8691 2389 42610219
Cerebrovascular accident 103.67 27.17 113 8614 97047 42515561
Cerebrovascular disorder 97.06 27.17 29 8698 1832 42610776
Nephrogenic systemic fibrosis 79.07 27.17 29 8698 3472 42609136
Infection 74.98 27.17 103 8624 111965 42500643
Shunt thrombosis 74.66 27.17 13 8714 62 42612546
Cardiac arrest 72.41 27.17 100 8627 109220 42503388
Parathyroidectomy 71.19 27.17 13 8714 85 42612523
Off label use 66.69 27.17 24 8703 638311 41974297
Skin induration 62.88 27.17 21 8706 1906 42610702
Unevaluable event 59.26 27.17 52 8675 34236 42578372
Acute myocardial infarction 54.00 27.17 63 8664 58102 42554506
Shunt occlusion 53.54 27.17 16 8711 1011 42611597
Blood parathyroid hormone increased 51.18 27.17 18 8709 1909 42610699
Drug ineffective 47.58 27.17 36 8691 630161 41982447
Skin hypertrophy 41.28 27.17 17 8710 2772 42609836
Chronic kidney disease 38.65 27.17 48 8679 47193 42565415
Skin tightness 37.98 27.17 15 8712 2195 42610413
Peritoneal dialysis complication 32.84 27.17 13 8714 1914 42610694
Peritonitis bacterial 29.20 27.17 18 8709 6897 42605711
Sudden death 28.27 27.17 25 8702 16604 42596004
Haemorrhagic stroke 28.07 27.17 18 8709 7384 42605224
Joint range of motion decreased 27.31 27.17 18 8709 7735 42604873
Angiosclerosis 27.21 27.17 4 8723 4 42612604

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
Myocardial infarction 419.16 22.41 231 8374 191852 110388842
Death 386.14 22.41 363 8242 698506 109882188
Cardio-respiratory arrest 325.13 22.41 165 8440 115671 110465023
Cardiac disorder 268.83 22.41 127 8478 76153 110504541
Calciphylaxis 263.96 22.41 62 8543 4125 110576569
Infarction 215.03 22.41 55 8550 5214 110575480
Sepsis 212.80 22.41 187 8418 327159 110253535
Respiratory arrest 186.86 22.41 91 8514 58208 110522486
Nephrogenic systemic fibrosis 179.26 22.41 48 8557 5435 110575259
Cardiac failure 174.05 22.41 132 8473 187494 110393200
Skin induration 136.73 22.41 37 8568 4358 110576336
Acute myocardial infarction 117.46 22.41 76 8529 83701 110496993
Skin hypertrophy 104.88 22.41 31 8574 5016 110575678
Renal transplant 99.50 22.41 27 8578 3211 110577483
Skin tightness 93.16 22.41 29 8576 5584 110575110
Peritonitis bacterial 86.15 22.41 32 8573 10501 110570193
Blood parathyroid hormone increased 83.51 22.41 25 8580 4223 110576471
Peritoneal dialysis complication 81.85 22.41 22 8583 2524 110578170
Chronic kidney disease 78.02 22.41 57 8548 76234 110504460
Parathyroidectomy 75.92 22.41 14 8591 279 110580415
Cardiac arrest 74.58 22.41 84 8521 196669 110384025
Cerebrovascular disorder 65.07 22.41 20 8585 3691 110577003
Skin fibrosis 63.96 22.41 16 8589 1384 110579310
Shunt thrombosis 56.72 22.41 10 8595 153 110580541
Cardiovascular disorder 56.71 22.41 30 8575 22730 110557964
Shunt occlusion 55.79 22.41 15 8590 1722 110578972
Joint contracture 50.44 22.41 15 8590 2476 110578218
Peritonitis 49.18 22.41 31 8574 32576 110548118
Azotaemia 48.84 22.41 21 8584 10064 110570630
Scar 44.19 22.41 23 8582 16858 110563836
Cerebrovascular accident 44.03 22.41 62 8543 181222 110399472
Arteriovenous fistula thrombosis 43.67 22.41 10 8595 593 110580101
Device related infection 41.45 22.41 30 8575 39489 110541205
Hypercalcaemia 41.32 22.41 32 8573 46625 110534069
Transplant 40.91 22.41 11 8594 1263 110579431
Fibrosis 40.61 22.41 17 8588 7625 110573069
Device related sepsis 37.28 22.41 16 8589 7631 110573063
Blood parathyroid hormone abnormal 36.51 22.41 8 8597 388 110580306
Off label use 34.24 22.41 40 8565 1500145 109080549
Osteomalacia 34.07 22.41 10 8595 1577 110579117
Sudden death 33.83 22.41 22 8583 24373 110556321
Cardiopulmonary failure 33.54 22.41 15 8590 7888 110572806
Parathyroid tumour benign 33.28 22.41 9 8596 1056 110579638
Skin hyperpigmentation 32.17 22.41 15 8590 8681 110572013
Arrhythmia 30.31 22.41 32 8573 69543 110511151
Hypertensive crisis 29.03 22.41 20 8585 24352 110556342
Nephropathy 28.67 22.41 16 8589 13451 110567243
Hypocalcaemia 28.36 22.41 30 8575 65336 110515358
Haemorrhagic stroke 28.32 22.41 16 8589 13773 110566921
Dialysis 27.96 22.41 18 8587 19601 110561093
Coronary artery disease 27.78 22.41 31 8574 71659 110509035
Arteriovenous fistula operation 26.17 22.41 6 8599 358 110580336
Shunt malfunction 26.07 22.41 6 8599 364 110580330
Hyperparathyroidism 25.49 22.41 10 8595 3800 110576894
Extremity contracture 24.68 22.41 8 8597 1753 110578941
Drug ineffective 23.82 22.41 52 8553 1520488 109060206
Hypotonia 23.81 22.41 15 8590 15730 110564964
Urosepsis 22.82 22.41 19 8586 30656 110550038
Acute pulmonary oedema 22.76 22.41 15 8590 16981 110563713
Peripheral arterial occlusive disease 22.46 22.41 12 8593 9268 110571426

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC H05BX02 SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS
CALCIUM HOMEOSTASIS
ANTI-PARATHYROID AGENTS
Other anti-parathyroid agents
FDA CS M0007651 Ergocalciferols
FDA EPC N0000175849 Vitamin D Analog
FDA EPC N0000175907 Vitamin D2 Analog
CHEBI has role CHEBI:35526 hypoglycemic agent
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:50827 antiparathyroid drug
CHEBI has role CHEBI:76595 nephroprotective agent
CHEBI has role CHEBI:231911 renoprotective agent

Related Drugs by ATC class:

H05BX Other anti-parathyroid agents 5 drugs
calcifediolcinacalcetdoxercalciferoletelcalcetideevocalcet

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

DiseaseRelationSNOMED_IDDOID
Hyperparathyroidism Secondary to Chronic Renal Failure indication
Poisoning by digitalis glycoside contraindication 12876009
Hyperphosphatemia contraindication 20165001 DOID:0050459
Hypervitaminosis D contraindication 27712000 DOID:9971
Hypercalcemia contraindication 66931009 DOID:12678




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Vitamin D3 receptor Nuclear hormone receptor AGONIST EC50 8.70 WOMBAT-PK CHEMBL

External reference:

IDSource
4021107 VUID
N0000148562 NUI
D00930 KEGG_DRUG
4021107 VANDF
C0249582 UMLSCUI
CHEBI:7931 CHEBI
CHEMBL1200622 ChEMBL_ID
DB00910 DRUGBANK_ID
C084656 MESH_SUPPLEMENTAL_RECORD_UI
5281104 PUBCHEM_CID
2791 IUPHAR_LIGAND_ID
7688 INN_ID
6702D36OG5 UNII
221005 RXNORM
11702 MMSL
206206 MMSL
5234 MMSL
d04312 MMSL
007498 NDDF
108946001 SNOMEDCT_US
126233000 SNOMEDCT_US
6702D36OG5 INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Zemplar HUMAN PRESCRIPTION DRUG LABEL 1 0074-1658 INJECTION, SOLUTION 5 ug INTRAVENOUS NDA 27 sections
Zemplar HUMAN PRESCRIPTION DRUG LABEL 1 0074-4314 CAPSULE, LIQUID FILLED 2 ug ORAL NDA 28 sections
Zemplar HUMAN PRESCRIPTION DRUG LABEL 1 0074-4317 CAPSULE, LIQUID FILLED 1 ug ORAL NDA 28 sections
Zemplar HUMAN PRESCRIPTION DRUG LABEL 1 0074-4637 INJECTION, SOLUTION 2 ug INTRAVENOUS NDA 27 sections
Zemplar HUMAN PRESCRIPTION DRUG LABEL 1 0074-9036 CAPSULE, LIQUID FILLED 1 ug ORAL NDA 28 sections
Zemplar HUMAN PRESCRIPTION DRUG LABEL 1 0074-9037 CAPSULE, LIQUID FILLED 2 ug ORAL NDA 28 sections
Paricalcitol HUMAN PRESCRIPTION DRUG LABEL 1 0143-9596 INJECTION 5 ug INTRAVENOUS NDA 24 sections
Paricalcitol HUMAN PRESCRIPTION DRUG LABEL 1 0143-9624 INJECTION 5 ug INTRAVENOUS NDA 24 sections
Paricalcitol HUMAN PRESCRIPTION DRUG LABEL 1 0143-9625 INJECTION 2 ug INTRAVENOUS NDA 24 sections
Paricalcitol HUMAN PRESCRIPTION DRUG LABEL 1 10888-5001 CAPSULE, LIQUID FILLED 1 ug ORAL ANDA 26 sections
Paricalcitol HUMAN PRESCRIPTION DRUG LABEL 1 10888-5002 CAPSULE, LIQUID FILLED 2 ug ORAL ANDA 26 sections
Paricalcitol HUMAN PRESCRIPTION DRUG LABEL 1 10888-5003 CAPSULE, LIQUID FILLED 4 ug ORAL ANDA 26 sections
Paricalcitol HUMAN PRESCRIPTION DRUG LABEL 1 16729-310 INJECTION, SOLUTION 2 ug INTRAVENOUS NDA 24 sections
Paricalcitol HUMAN PRESCRIPTION DRUG LABEL 1 16729-311 INJECTION, SOLUTION 5 ug INTRAVENOUS NDA 24 sections
Paricalcitol Human Prescription Drug Label 1 25000-012 CAPSULE, LIQUID FILLED 1 ug ORAL ANDA 24 sections
Paricalcitol Human Prescription Drug Label 1 25000-014 CAPSULE, LIQUID FILLED 2 ug ORAL ANDA 24 sections
Paricalcitol Human Prescription Drug Label 1 25000-017 CAPSULE, LIQUID FILLED 4 ug ORAL ANDA 24 sections
Paricalcitol HUMAN PRESCRIPTION DRUG LABEL 1 49483-687 CAPSULE, LIQUID FILLED 1 ug ORAL ANDA 24 sections
Paricalcitol HUMAN PRESCRIPTION DRUG LABEL 1 49483-688 CAPSULE, LIQUID FILLED 2 ug ORAL ANDA 24 sections
Paricalcitol HUMAN PRESCRIPTION DRUG LABEL 1 49483-689 CAPSULE, LIQUID FILLED 4 ug ORAL ANDA 24 sections
Paricalcitol HUMAN PRESCRIPTION DRUG LABEL 1 55111-663 CAPSULE, LIQUID FILLED 1 ug ORAL ANDA 25 sections
Paricalcitol HUMAN PRESCRIPTION DRUG LABEL 1 55111-664 CAPSULE, LIQUID FILLED 2 ug ORAL ANDA 25 sections
Paricalcitol HUMAN PRESCRIPTION DRUG LABEL 1 55111-665 CAPSULE, LIQUID FILLED 4 ug ORAL ANDA 25 sections
PARICALCITOL Human Prescription Drug Label 1 55150-212 INJECTION 2 ug INTRAVENOUS ANDA 24 sections
PARICALCITOL Human Prescription Drug Label 1 55150-212 INJECTION 2 ug INTRAVENOUS ANDA 24 sections
PARICALCITOL Human Prescription Drug Label 1 55150-213 INJECTION 5 ug INTRAVENOUS ANDA 24 sections
PARICALCITOL Human Prescription Drug Label 1 55150-213 INJECTION 5 ug INTRAVENOUS ANDA 24 sections
PARICALCITOL Human Prescription Drug Label 1 55150-214 INJECTION 10 ug INTRAVENOUS ANDA 24 sections
PARICALCITOL Human Prescription Drug Label 1 55150-214 INJECTION 10 ug INTRAVENOUS ANDA 24 sections
PARICALCITOL Human Prescription Drug Label 1 55150-215 INJECTION 10 ug INTRAVENOUS ANDA 24 sections