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Identification
NameParicalcitol
Accession NumberDB00910  (APRD01165)
TypeSmall Molecule
GroupsApproved, Investigational
DescriptionParicalcitol is a synthetic vitamin D analog. Paricalcitol has been used to reduce parathyroid hormone levels. Paricalcitol is indicated for the prevention and treatment of secondary hyperparathyroidism associated with chronic renal failure.
Structure
Thumb
Synonyms
19-Nor-1alpha,25-dihydroxyvitamin D2
Paricalcitol
Zemplar
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Paricalcitolinjection, solution2 ug/mLintravenousHospira, Inc.2014-11-01Not applicableUs
Paricalcitolinjection, solution5 ug/mLintravenousAccord Healthcare, Inc.2016-03-01Not applicableUs
Paricalcitolcapsule, liquid filled2 ug/1oralZydus Pharmaceuticals USA Inc2010-06-14Not applicableUs
Paricalcitolinjection5 ug/mLintravenousWest ward Pharmaceutical Corp2014-11-18Not applicableUs
Paricalcitolinjection, solution5 ug/mLintravenousHospira, Inc.2014-11-01Not applicableUs
Paricalcitolinjection5 ug/mLintravenousWest ward Pharmaceutical Corp2014-11-18Not applicableUs
Paricalcitolinjection2 ug/mLintravenousWest ward Pharmaceutical Corp2014-11-18Not applicableUs
Paricalcitolcapsule, liquid filled1 ug/1oralZydus Pharmaceuticals USA Inc2010-06-14Not applicableUs
Paricalcitolinjection, solution2 ug/mLintravenousAccord Healthcare, Inc.2016-03-01Not applicableUs
Zemplarinjection, solution5 ug/mLintravenousAbb Vie Inc.1998-04-17Not applicableUs
Zemplarcapsule, liquid filled2 ug/1oralAbb Vie Inc.2010-06-14Not applicableUs
Zemplarcapsule, liquid filled4 ug/1oralAbb Vie Inc.2010-06-142015-12-29Us
Zemplarcapsule, liquid filled1 ug/1oralCardinal Health2005-05-26Not applicableUs
Zemplarcapsule, liquid filled1 ug/1oralAbb Vie Inc.2010-06-14Not applicableUs
Zemplarsolution5 mcgintravenousAbbvie Corporation2005-12-012012-11-03Canada
Zemplarinjection, solution2 ug/mLintravenousAbb Vie Inc.1998-04-17Not applicableUs
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Paricalcitolcapsule, liquid filled1 ug/1oralAurobindo Pharma Limited2016-01-14Not applicableUs
Paricalcitolcapsule, liquid filled2 ug/1oralDr. Reddy's Laboratories Limited2014-06-25Not applicableUs
Paricalcitolcapsule, liquid filled1 ug/1oralTeva Pharmaceuticals USA Inc2013-09-30Not applicableUs
Paricalcitolcapsule4 ug/1oralAlvogen, Inc.2016-03-012016-03-11Us
Paricalcitolcapsule, gelatin coated4 ug/1oralRising Pharmaceuticals, Inc.2015-11-03Not applicableUs
Paricalcitolcapsule, liquid filled4 ug/1oralGolden State Medical Supply, Inc.2014-03-27Not applicableUs
Paricalcitolcapsule, liquid filled2 ug/1oralGolden State Medical Supply, Inc.2015-12-07Not applicableUs
Paricalcitolcapsule, liquid filled2 ug/1oralBanner Pharmacaps2014-03-27Not applicableUs
Paricalcitolcapsule1 ug/1oralAmneal Pharmaceuticals of New York, LLC2016-01-17Not applicableUs
Paricalcitolcapsule, liquid filled4 ug/1oralDr. Reddy's Laboratories Limited2014-06-25Not applicableUs
Paricalcitolcapsule, liquid filled2 ug/1oralAurobindo Pharma Limited2016-01-14Not applicableUs
Paricalcitolcapsule, liquid filled2 ug/1oralTeva Pharmaceuticals USA Inc2013-09-30Not applicableUs
Paricalcitolcapsule1 mg/1oralBanner Life Sciences Llc.2015-09-02Not applicableUs
Paricalcitolcapsule, liquid filled1 ug/1oralAmerican Health Packaging2015-03-31Not applicableUs
Paricalcitolcapsule, liquid filled4 ug/1oralGolden State Medical Supply, Inc.2015-12-07Not applicableUs
Paricalcitolcapsule, liquid filled4 ug/1oralBanner Pharmacaps2014-03-27Not applicableUs
Paricalcitolcapsule2 ug/1oralAmneal Pharmaceuticals of New York, LLC2016-01-17Not applicableUs
Paricalcitolcapsule, liquid filled1 ug/1oralGolden State Medical Supply, Inc.2014-04-23Not applicableUs
Paricalcitolcapsule, liquid filled4 ug/1oralAurobindo Pharma Limited2016-01-14Not applicableUs
Paricalcitolcapsule, liquid filled4 ug/1oralTeva Pharmaceuticals USA Inc2013-09-30Not applicableUs
Paricalcitolcapsule2 mg/1oralBanner Life Sciences Llc.2015-10-01Not applicableUs
Paricalcitolcapsule, gelatin coated1 ug/1oralRising Pharmaceuticals, Inc.2015-11-03Not applicableUs
Paricalcitolcapsule1 ug/1oralAlvogen, Inc.2016-03-012016-03-11Us
Paricalcitolcapsule, liquid filled1 ug/1oralDr. Reddy's Laboratories Limited2014-06-25Not applicableUs
Paricalcitolcapsule4 ug/1oralAmneal Pharmaceuticals of New York, LLC2016-01-17Not applicableUs
Paricalcitolcapsule, liquid filled2 ug/1oralGolden State Medical Supply, Inc.2014-04-23Not applicableUs
Paricalcitolcapsule, liquid filled1 ug/1oralGolden State Medical Supply, Inc.2015-12-07Not applicableUs
Paricalcitolcapsule, liquid filled1 ug/1oralBanner Pharmacaps2014-03-27Not applicableUs
Paricalcitolcapsule4 mg/1oralBanner Life Sciences Llc.2015-10-01Not applicableUs
Paricalcitolcapsule, gelatin coated2 ug/1oralRising Pharmaceuticals, Inc.2015-11-03Not applicableUs
Paricalcitolcapsule2 ug/1oralAlvogen, Inc.2016-03-012016-03-11Us
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNII6702D36OG5
CAS number131918-61-1
WeightAverage: 416.6365
Monoisotopic: 416.329045274
Chemical FormulaC27H44O3
InChI KeyInChIKey=BPKAHTKRCLCHEA-UBFJEZKGSA-N
InChI
InChI=1S/C27H44O3/c1-18(8-9-19(2)26(3,4)30)24-12-13-25-21(7-6-14-27(24,25)5)11-10-20-15-22(28)17-23(29)16-20/h8-11,18-19,22-25,28-30H,6-7,12-17H2,1-5H3/b9-8+,21-11+/t18-,19+,22-,23-,24-,25+,27-/m1/s1
IUPAC Name
(1R,3R)-5-{2-[(1R,3aS,4E,7aR)-1-[(2R,3E,5S)-6-hydroxy-5,6-dimethylhept-3-en-2-yl]-7a-methyl-octahydro-1H-inden-4-ylidene]ethylidene}cyclohexane-1,3-diol
SMILES
[H]C1CC[C@]2(C)[C@]([H])(CC[C@@]2([H])\C1=C\C=C1C[C@@H](O)C[[email protected]](O)C1)[[email protected]](C)\C=C\[[email protected]](C)C(O)(C)C
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as triterpenoids. These are terpene molecules containing 8 isoprene units.
KingdomOrganic compounds
Super ClassLipids and lipid-like molecules
ClassPrenol lipids
Sub ClassTriterpenoids
Direct ParentTriterpenoids
Alternative Parents
Substituents
  • Polycyclic triterpenoid
  • Triterpenoid
  • Cyclohexanol
  • Tertiary alcohol
  • Cyclic alcohol
  • Secondary alcohol
  • Hydrocarbon derivative
  • Organooxygen compound
  • Alcohol
  • Aliphatic homopolycyclic compound
Molecular FrameworkAliphatic homopolycyclic compounds
External Descriptors
Pharmacology
IndicationFor treatment of secondary hyperparathyroidism associated with chronic kidney disease (CKD) Stage 3 and 4
PharmacodynamicsSecondary hyperparathyroidism is characterized by an elevation in parathyroid hormone (PTH) associated with inadequate levels of active vitamin D hormone. The source of vitamin D in the body is from synthesis in the skin and from dietary intake. Vitamin D requires two sequential hydroxylations in the liver and the kidney to bind to and to activate the vitamin D receptor (VDR). The endogenous VDR activator, calcitriol [1,25(OH)2 D3], is a hormone that binds to VDRs that are present in the parathyroid gland, intestine, kidney, and bone to maintain parathyroid function and calcium and phosphorus homeostasis, and to VDRs found in many other tissues, including prostate, endothelium and immune cells. VDR activation is essential for the proper formation and maintenance of normal bone. In the diseased kidney, the activation of vitamin D is diminished, resulting in a rise of PTH, subsequently leading to secondary hyperparathyroidism and disturbances in the calcium and phosphorus homeostasis.1 Decreased levels of 1,25(OH)2 D3 have been observed in early stages of chronic kidney disease. The decreased levels of 1,25(OH)2 D3 and resultant elevated PTH levels, both of which often precede abnormalities in serum calcium and phosphorus, affect bone turnover rate and may result in renal osteodystrophy. An in vitro study indicates that paricalcitol is not an inhibitor of CYP1A2, CYP2A6, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1 or CYP3A at concentrations up to 50 nM (21 ng/mL).
Mechanism of actionParicalcitol is a synthetic, biologically active vitamin D analog of calcitriol with modifications to the side chain (D2) and the A (19-nor) ring. Preclinical andin vitro studies have demonstrated that paricalcitol's biological actions are mediated through binding of the VDR, which results in the selective activation of vitamin D responsive pathways. Vitamin D and paricalcitol have been shown to reduce parathyroid hormone levels by inhibiting PTH synthesis and secretion.
Related Articles
AbsorptionWell absorbed
Volume of distribution
  • 30.8 ± 7.5 L [CKD Stage 5-HD]
  • 34.9 ± 9.5 L [CKD Stage 5-PD]
  • 23.8 L [healthy subjects]
Protein binding99.8% (bound to plasma proteins)
Metabolism

Metabolized by multiple hepatic and non-hepatic enzymes, including mitochondrial CYP24, as well as CYP3A4 and UGT1A4

Route of eliminationParicalcitol is excreted primarily by hepatobiliary excretion.
Half life4 to 6 hours
Clearance
  • 1.49 +/- 0.60 L/h [chronic kidney disease Stage 5 with hemodialysis]
  • 1.54 +/- 0.95 L/h [chronic kidney disease Stage 5with peritoneal dialysis]
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9971
Blood Brain Barrier+0.795
Caco-2 permeable+0.776
P-glycoprotein substrateSubstrate0.7667
P-glycoprotein inhibitor INon-inhibitor0.7431
P-glycoprotein inhibitor IINon-inhibitor0.8491
Renal organic cation transporterNon-inhibitor0.8292
CYP450 2C9 substrateNon-substrate0.7968
CYP450 2D6 substrateNon-substrate0.8903
CYP450 3A4 substrateSubstrate0.7662
CYP450 1A2 substrateNon-inhibitor0.8127
CYP450 2C9 inhibitorNon-inhibitor0.8277
CYP450 2D6 inhibitorNon-inhibitor0.948
CYP450 2C19 inhibitorNon-inhibitor0.8491
CYP450 3A4 inhibitorNon-inhibitor0.8409
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.6631
Ames testNon AMES toxic0.9116
CarcinogenicityNon-carcinogens0.9111
BiodegradationNot ready biodegradable0.988
Rat acute toxicity4.4277 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9069
hERG inhibition (predictor II)Non-inhibitor0.8015
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Abbott laboratories pharmaceutical products div
  • Abbott laboratories
Packagers
Dosage forms
FormRouteStrength
Capsuleoral1 mg/1
Capsuleoral1 ug/1
Capsuleoral2 ug/1
Capsuleoral2 mg/1
Capsuleoral4 mg/1
Capsuleoral4 ug/1
Capsule, gelatin coatedoral1 ug/1
Capsule, gelatin coatedoral2 ug/1
Capsule, gelatin coatedoral4 ug/1
Capsule, liquid filledoral4 ug/1
Injectionintravenous2 ug/mL
Injectionintravenous5 ug/mL
Capsule, liquid filledoral1 ug/1
Capsule, liquid filledoral2 ug/1
Injection, solutionintravenous2 ug/mL
Injection, solutionintravenous5 ug/mL
Solutionintravenous5 mcg
Prices
Unit descriptionCostUnit
Zemplar 4 mcg capsule37.58USD capsule
Zemplar 5 mcg/ml vial28.03USD ml
Zemplar 2 mcg capsule18.79USD capsule
Zemplar 2 mcg/ml vial11.22USD ml
Zemplar 1 mcg capsule9.39USD capsule
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5246925 No1995-04-172012-04-17Us
US5597815 Yes1996-01-132016-01-13Us
US6136799 Yes1998-10-082018-10-08Us
US6361758 Yes1998-10-082018-10-08Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
logP4.5Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0068 mg/mLALOGPS
logP5.27ALOGPS
logP4.26ChemAxon
logS-4.8ALOGPS
pKa (Strongest Acidic)14.81ChemAxon
pKa (Strongest Basic)-1ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count3ChemAxon
Polar Surface Area60.69 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity127.95 m3·mol-1ChemAxon
Polarizability51.11 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
References
Synthesis Reference

Anchel Schwartz, Alexei Ploutno, Koby Wolfman, “Preparation of paricalcitol.” U.S. Patent US20070149489, issued June 28, 2007.

US20070149489
General ReferencesNot Available
External Links
ATC CodesH05BX02
AHFS Codes
  • 88:16.00
PDB EntriesNot Available
FDA labelDownload (447 KB)
MSDSNot Available
Interactions
Drug Interactions
Drug
AmiodaroneThe serum concentration of Paricalcitol can be increased when it is combined with Amiodarone.
AprepitantThe serum concentration of Paricalcitol can be increased when it is combined with Aprepitant.
AtazanavirThe serum concentration of Paricalcitol can be increased when it is combined with Atazanavir.
AtomoxetineThe metabolism of Paricalcitol can be decreased when combined with Atomoxetine.
BexaroteneThe serum concentration of Paricalcitol can be decreased when it is combined with Bexarotene.
BoceprevirThe serum concentration of Paricalcitol can be increased when it is combined with Boceprevir.
BortezomibThe metabolism of Paricalcitol can be decreased when combined with Bortezomib.
BosentanThe serum concentration of Paricalcitol can be decreased when it is combined with Bosentan.
CarbamazepineThe metabolism of Paricalcitol can be increased when combined with Carbamazepine.
CeritinibThe serum concentration of Paricalcitol can be increased when it is combined with Ceritinib.
ClarithromycinThe serum concentration of Paricalcitol can be increased when it is combined with Clarithromycin.
ClemastineThe metabolism of Paricalcitol can be decreased when combined with Clemastine.
ClotrimazoleThe metabolism of Paricalcitol can be decreased when combined with Clotrimazole.
CobicistatThe serum concentration of Paricalcitol can be increased when it is combined with Cobicistat.
ConivaptanThe serum concentration of Paricalcitol can be increased when it is combined with Conivaptan.
CrizotinibThe metabolism of Paricalcitol can be decreased when combined with Crizotinib.
CyclosporineThe metabolism of Paricalcitol can be decreased when combined with Cyclosporine.
DabrafenibThe serum concentration of Paricalcitol can be decreased when it is combined with Dabrafenib.
DarunavirThe serum concentration of Paricalcitol can be increased when it is combined with Darunavir.
DasatinibThe serum concentration of Paricalcitol can be increased when it is combined with Dasatinib.
DeferasiroxThe serum concentration of Paricalcitol can be decreased when it is combined with Deferasirox.
DelavirdineThe metabolism of Paricalcitol can be decreased when combined with Delavirdine.
DexamethasoneThe serum concentration of Paricalcitol can be decreased when it is combined with Dexamethasone.
DigoxinThe risk or severity of adverse effects can be increased when Paricalcitol is combined with Digoxin.
DihydroergotamineThe metabolism of Paricalcitol can be decreased when combined with Dihydroergotamine.
DiltiazemThe metabolism of Paricalcitol can be decreased when combined with Diltiazem.
DoxycyclineThe metabolism of Paricalcitol can be decreased when combined with Doxycycline.
DronedaroneThe metabolism of Paricalcitol can be decreased when combined with Dronedarone.
EfavirenzThe serum concentration of Paricalcitol can be decreased when it is combined with Efavirenz.
EnzalutamideThe serum concentration of Paricalcitol can be decreased when it is combined with Enzalutamide.
ErythromycinThe metabolism of Paricalcitol can be decreased when combined with Erythromycin.
Eslicarbazepine acetateThe serum concentration of Paricalcitol can be decreased when it is combined with Eslicarbazepine acetate.
EtravirineThe serum concentration of Paricalcitol can be decreased when it is combined with Etravirine.
FluconazoleThe metabolism of Paricalcitol can be decreased when combined with Fluconazole.
FluvoxamineThe metabolism of Paricalcitol can be decreased when combined with Fluvoxamine.
FosamprenavirThe metabolism of Paricalcitol can be decreased when combined with Fosamprenavir.
FosaprepitantThe serum concentration of Paricalcitol can be increased when it is combined with Fosaprepitant.
FosphenytoinThe metabolism of Paricalcitol can be increased when combined with Fosphenytoin.
Fusidic AcidThe serum concentration of Paricalcitol can be increased when it is combined with Fusidic Acid.
IdelalisibThe serum concentration of Paricalcitol can be increased when it is combined with Idelalisib.
ImatinibThe metabolism of Paricalcitol can be decreased when combined with Imatinib.
IndinavirThe serum concentration of Paricalcitol can be increased when it is combined with Indinavir.
IsavuconazoniumThe metabolism of Paricalcitol can be decreased when combined with Isavuconazonium.
IsradipineThe metabolism of Paricalcitol can be decreased when combined with Isradipine.
ItraconazoleThe serum concentration of Paricalcitol can be increased when it is combined with Itraconazole.
IvacaftorThe serum concentration of Paricalcitol can be increased when it is combined with Ivacaftor.
KetoconazoleThe serum concentration of Paricalcitol can be increased when it is combined with Ketoconazole.
LopinavirThe serum concentration of Paricalcitol can be increased when it is combined with Lopinavir.
LovastatinThe metabolism of Paricalcitol can be decreased when combined with Lovastatin.
LuliconazoleThe serum concentration of Paricalcitol can be increased when it is combined with Luliconazole.
MifepristoneThe metabolism of Paricalcitol can be decreased when combined with Mifepristone.
MitotaneThe serum concentration of Paricalcitol can be decreased when it is combined with Mitotane.
ModafinilThe serum concentration of Paricalcitol can be decreased when it is combined with Modafinil.
NafcillinThe serum concentration of Paricalcitol can be decreased when it is combined with Nafcillin.
NefazodoneThe serum concentration of Paricalcitol can be increased when it is combined with Nefazodone.
NelfinavirThe serum concentration of Paricalcitol can be increased when it is combined with Nelfinavir.
NetupitantThe serum concentration of Paricalcitol can be increased when it is combined with Netupitant.
NevirapineThe metabolism of Paricalcitol can be decreased when combined with Nevirapine.
NilotinibThe metabolism of Paricalcitol can be decreased when combined with Nilotinib.
OlaparibThe metabolism of Paricalcitol can be decreased when combined with Olaparib.
OrlistatThe serum concentration of Paricalcitol can be decreased when it is combined with Orlistat.
OsimertinibThe serum concentration of Paricalcitol can be increased when it is combined with Osimertinib.
PalbociclibThe serum concentration of Paricalcitol can be increased when it is combined with Palbociclib.
PentobarbitalThe metabolism of Paricalcitol can be increased when combined with Pentobarbital.
PhenobarbitalThe metabolism of Paricalcitol can be increased when combined with Phenobarbital.
PhenytoinThe metabolism of Paricalcitol can be increased when combined with Phenytoin.
PosaconazoleThe serum concentration of Paricalcitol can be increased when it is combined with Posaconazole.
PrimidoneThe metabolism of Paricalcitol can be increased when combined with Primidone.
RanolazineThe metabolism of Paricalcitol can be decreased when combined with Ranolazine.
RifabutinThe metabolism of Paricalcitol can be increased when combined with Rifabutin.
RifampicinThe metabolism of Paricalcitol can be increased when combined with Rifampicin.
RifapentineThe metabolism of Paricalcitol can be increased when combined with Rifapentine.
RitonavirThe serum concentration of Paricalcitol can be increased when it is combined with Ritonavir.
SaquinavirThe serum concentration of Paricalcitol can be increased when it is combined with Saquinavir.
SildenafilThe metabolism of Paricalcitol can be decreased when combined with Sildenafil.
SiltuximabThe serum concentration of Paricalcitol can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Paricalcitol can be increased when it is combined with Simeprevir.
St. John's WortThe serum concentration of Paricalcitol can be decreased when it is combined with St. John's Wort.
StiripentolThe serum concentration of Paricalcitol can be increased when it is combined with Stiripentol.
SulfisoxazoleThe metabolism of Paricalcitol can be decreased when combined with Sulfisoxazole.
TelaprevirThe serum concentration of Paricalcitol can be increased when it is combined with Telaprevir.
TelithromycinThe serum concentration of Paricalcitol can be increased when it is combined with Telithromycin.
TiclopidineThe metabolism of Paricalcitol can be decreased when combined with Ticlopidine.
TocilizumabThe serum concentration of Paricalcitol can be decreased when it is combined with Tocilizumab.
VenlafaxineThe metabolism of Paricalcitol can be decreased when combined with Venlafaxine.
VerapamilThe metabolism of Paricalcitol can be decreased when combined with Verapamil.
VoriconazoleThe serum concentration of Paricalcitol can be increased when it is combined with Voriconazole.
ZiprasidoneThe metabolism of Paricalcitol can be decreased when combined with Ziprasidone.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
Zinc ion binding
Specific Function:
Nuclear hormone receptor. Transcription factor that mediates the action of vitamin D3 by controlling the expression of hormone sensitive genes. Recruited to promoters via its interaction with BAZ1B/WSTF which mediates the interaction with acetylated histones, an essential step for VDR-promoter association. Plays a central role in calcium homeostasis.
Gene Name:
VDR
Uniprot ID:
P11473
Molecular Weight:
48288.64 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
  3. Andress DL: Vitamin D treatment in chronic kidney disease. Semin Dial. 2005 Jul-Aug;18(4):315-21. [PubMed:16076355 ]
  4. Brancaccio D, Cozzolino M, Pasho S, Fallabrino G, Olivi L, Gallieni M: New acquisitions in therapy of secondary hyperparathyroidism in chronic kidney disease and peritoneal dialysis patients: role of vitamin D receptor activators. Contrib Nephrol. 2009;163:219-26. doi: 10.1159/000223802. Epub 2009 Jun 3. [PubMed:19494617 ]
  5. Wu-Wong JR, Nakane M, Gagne GD, Brooks KA, Noonan WT: Comparison of the pharmacological effects of paricalcitol and doxercalciferol on the factors involved in mineral homeostasis. Int J Endocrinol. 2010;2010:621687. doi: 10.1155/2010/621687. Epub 2010 Mar 2. [PubMed:20204178 ]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxidoreductase activity
Specific Function:
Has a role in maintaining calcium homeostasis. Catalyzes the NADPH-dependent 24-hydroxylation of calcidiol (25-hydroxyvitamin D(3)) and calcitriol (1-alpha,25-dihydroxyvitamin D(3)). The enzyme can perform up to 6 rounds of hydroxylation of calcitriol leading to calcitroic acid. It also shows 23-hydroxylating activity leading to 1-alpha,25-dihydroxyvitamin D(3)-26,23-lactone as end product.
Gene Name:
CYP24A1
Uniprot ID:
Q07973
Molecular Weight:
58874.695 Da
References
  1. Robinson DM, Scott LJ: Paricalcitol: a review of its use in the management of secondary hyperparathyroidism. Drugs. 2005;65(4):559-76. [PubMed:15733015 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Protein homodimerization activity
Specific Function:
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform glucuronidates bilirubin IX-alpha to form both the IX-alpha-C8 and IX-alpha-C12 monoconjugates and diconjugate. Isoform 2 lacks transferase activity but acts as a negative regulator of isoform 1 (By similarity).
Gene Name:
UGT1A4
Uniprot ID:
P22310
Molecular Weight:
60024.535 Da
Comments
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Drug created on June 13, 2005 07:24 / Updated on September 28, 2016 03:41