Alfacalcidol

Identification

Summary

Alfacalcidol is a vitamin D analogue used for the management of hypocalcemia, secondary hyperparathyroidism, and osteodystrophy in patients with chronic renal failure, as well as some types of rickets and osteomalacia.

Brand Names
One-alpha
Generic Name
Alfacalcidol
DrugBank Accession Number
DB01436
Background

Alfacalcidol, or 1-alpha-hydroxycholecalciferol or 1-alpha-hydroxyvitamin D3, is a non-endogenous analogue of vitamin D.4 It plays an essential function in calcium homeostasis and bone metabolism. Alfacaldisol is activated by the enzyme 25-hydroxylase in the liver to mediate its effects in the body, or most importantly, the kidneys and bones. The pharmacological actions of alfacalcidol are prolonged than vitamin D because a negative feedback mechanism regulates the final activation step of vitamin D in the kidneys.1,2

Alfacalcidol is available in oral and intravenous formulations. In Canada, it is marketed as ONE-ALPHA, which manages hypocalcemia, secondary hyperparathyroidism, and osteodystrophy in adults with chronic renal failure.9 In approving European countries, alfacalcidol is also indicated for managing nutritional and malabsorptive rickets and osteomalacia, vitamin D-dependent rickets and osteomalacia, and hypophosphataemic vitamin D resistant rickets and osteomalacia.11,12

Type
Small Molecule
Groups
Approved, Nutraceutical
Structure
Thumb
Weight
Average: 400.6371
Monoisotopic: 400.334130652
Chemical Formula
C27H44O2
Synonyms
  • (5Z,7E)-9,10-seco-5,7,10(19)-cholestatrien-1α,3β-diol
  • 1-hydroxycholecalciferol
  • 1alpha-hydroxycholecalciferol
  • 1α-hydroxy-vitamin D3
  • 1α-hydroxycholecalciferol
  • 1α-hydroxyvitamin D3
  • 9,10-secocholesta-5,7,10(19)-triene-1α,3β-diol
  • Alfacalcidol
  • Alfacalcidolum

Pharmacology

Indication

Alfacalcidol is indicated in adult patients with chronic renal failure for the management of hypocalcemia, secondary hyperparathyroidism, or osteodystrophy.9

Alfacalcidol is indicated in the management of nutritional and malabsorptive rickets and osteomalacia, vitamin D-dependent rickets and osteomalacia, and hypophosphataemic vitamin D resistant rickets and osteomalacia.11,12

Pharmacology
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Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
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Pharmacodynamics

Alfacalcidol works to increase serum levels of calcium by stimulating intestinal calcium absorption, reabsorption of calcium from bone, and possibly the renal reabsorption of calcium. It also modestly promotes intestinal phosphorus absorption.9 In patients with renal failure, alfacalcidol increased intestinal calcium and phosphorus absorption in a dose-related manner. This increase in calcium and phosphorus levels occurs within three days following drug administration: this effect was reversed within three days of drug discontinuation. In patients with chronic renal failure, serum calcium levels were elevated while parathyroid hormone and alkaline phosphatase levels returned to normal levels within five days following alfacalcidol administration.12 Since alfacalcidol suppresses parathyroid hormone, a reduction in parathyroid hormone levels is achieved more rapidly in patients on intermittent intravenous therapy, with significant reductions occurring within three months of therapy. In patients receiving daily oral therapy of alfacalcidol, the time it takes alfacalcidol to normalize plasma calcium levels may be up to several months, possibly reflecting calcium being utilized for bone mineralization.9 In patients with nutritional osteomalacia, alfacalcidol increased calcium absorption with six hours of oral administration and the effects peaked at 24 hours.12

Mechanism of action

In conditions like chronic renal failure, renal bone disease, hypoparathyroidism, and vitamin D dependent rickets, the kidneys' capacity for 1α-hydroxylation is impaired, leading to reduced production of endogenous 1,25-dihydroxyvitamin D and aberrated mineral metabolism. As an active and potent analog of vitamin D, alfacalcidol works to restore the functions and activities of endogenous 1,25-dihydroxyvitamin D.12

TargetActionsOrganism
AVitamin D3 receptor
agonist
Humans
U25-hydroxyvitamin D-1 alpha hydroxylase, mitochondrialNot AvailableHumans
URetinoic acid receptor RXR-alphaNot AvailableHumans
Absorption

Alfacalcidol is absorbed passively and almost completely in the small intestine.12

Volume of distribution

Not Available

Protein binding

The active metabolite of alfacalcidol, 1,25-dihydroxyvitamin D, is transported to tissues via globulin, a specific transport protein.12

Metabolism

Alfacalcidol is rapidly converted in the liver to 1,25-dihydroxyvitamin D, which is essentially the metabolite of vitamin D that regulates calcium and phosphate metabolism. Alfacalcidol is further metabolized to other polar inactive metabolites, excreted primarily through the bile.12

Route of elimination

Not Available

Half-life

The half-life of alfacalcidol ranges from three to four hours.9,12

Clearance

Not Available

Adverse Effects
Medicalerrors
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Toxicity

There is a discrepancy across a number of reported LD50 values for alfacalcidol, which can be attributed to differences in the procedures used in laboratories. Oral LD50 in mice ranges from 440 to 490 mcg/kg. Intravenous in mice was 290 mcg/kg; however, another source presented 56 mcg/kg in female mice and 71 mcg/kg in male mice. Oral LD50 in rats ranges from 340 to 720 mcg/kg.9

In case of an acute accidental overdose following oral administration, emesis or gastric lavage can be induced to prevent further drug absorption. Mineral oil may be used to promote fecal drug elimination in instances where the drug was already absorbed in the stomach.9

Alfacalcidol overdose can lead to hypercalcemia, hypercalciuria, and hyperphosphatemia. Similarly, a high intake of calcium and phosphate concurrently with a therapeutic dose of alfacalcidol can result in those conditions.9 Hypercalcemia most commonly presents with headache, weakness, hypertension, somnolence, dizziness, sweating, anorexia, nausea, vomiting, diarrhea, constipation, polyuria, polydipsia and muscle and bone pain, and metallic taste.12 Hypercalcemia should be responded to with discontinuation of alfacalcidol, a low calcium diet and withdrawal of calcium supplements.9 Prolonged hypercalcemia can lead to nephrocalcinosis, nephrolithiasis, and reduced kidney function. In cases of severe hypercalcemia, general supportive measures are recommended, which may include forced diuresis and close monitoring of renal function, electrolytes, and electrocardiographs. Monitoring for abnormalities is especially critical in patients receiving digitalis glycosides. Management with glucocorticosteroids, loop diuretics, bisphosphonates, and calcitonin, as well as hemodialysis with low calcium content, may be considered.12

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AcetyldigitoxinThe risk or severity of ventricular arrhythmias and Cardiac Arrhythmia can be increased when Alfacalcidol is combined with Acetyldigitoxin.
Aluminum hydroxideThe serum concentration of Aluminum hydroxide can be increased when it is combined with Alfacalcidol.
Beclomethasone dipropionateThe therapeutic efficacy of Alfacalcidol can be decreased when used in combination with Beclomethasone dipropionate.
BendroflumethiazideThe risk or severity of hypercalcemia can be increased when Bendroflumethiazide is combined with Alfacalcidol.
BenzthiazideThe risk or severity of hypercalcemia can be increased when Benzthiazide is combined with Alfacalcidol.
BetamethasoneThe therapeutic efficacy of Alfacalcidol can be decreased when used in combination with Betamethasone.
Betamethasone phosphateThe therapeutic efficacy of Alfacalcidol can be decreased when used in combination with Betamethasone phosphate.
BudesonideThe therapeutic efficacy of Alfacalcidol can be decreased when used in combination with Budesonide.
CalcifediolThe risk or severity of adverse effects can be increased when Calcifediol is combined with Alfacalcidol.
CalcitriolThe risk or severity of adverse effects can be increased when Calcitriol is combined with Alfacalcidol.
Interactions
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Food Interactions
  • Take with or without food. Food does not affect the bioavailability.

Products

Products
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International/Other Brands
Alsiodol / One Alpha
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
One-alphaCapsule1 mcgOralLeo Pharma1980-12-31Not applicableCanada flag
One-alphaSolution / drops2 mcg / mLOralLeo Pharma2000-12-04Not applicableCanada flag
One-alphaCapsule0.5 mcgOralLeo PharmaNot applicableNot applicableCanada flag
One-alphaCapsule0.25 mcgOralLeo Pharma1980-12-31Not applicableCanada flag
One-alphaLiquid2 mcg / mLIntravenousLeo Pharma2001-02-20Not applicableCanada flag
One-alpha Sol 0.2mcg/mlLiquid.2 mcg / mLOralLeo Pharma1989-12-312000-12-04Canada flag
Over the Counter Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Alfa-D 0.25mcg CapsuleCapsuleOralPAHANG PHARMACY SDN. BHD.2020-09-08Not applicableMalaysia flag
Alfa-D 1.00mcg CapsuleCapsuleOralPAHANG PHARMACY SDN. BHD.2020-09-08Not applicableMalaysia flag
Alfacip 0.25mcg capsuleCapsuleOralCIPLA MALAYSIA SDN BHD2020-09-08Not applicableMalaysia flag
Alfacip 1mcg capsuleCapsuleOralCIPLA MALAYSIA SDN BHD2020-09-08Not applicableMalaysia flag
ALPHA D3 1 MCGCapsule1 mcgOralบริษัท ซิลลิค ฟาร์มา จำกัด จำกัด2019-08-29Not applicableThailand flag
BON-ONE TABLET 0.25MCGTabletOralSOMEDICO SDN. BHD.2020-09-08Not applicableMalaysia flag
BON-ONE TABLET 0.5MCGTabletOralSOMEDICO SDN. BHD.2020-09-08Not applicableMalaysia flag
BON-ONE TABLET 1.0MCGTabletOralSOMEDICO SDN. BHD.2020-09-08Not applicableMalaysia flag
Medi-α 1 (1mcg Capsules)Capsule, gelatin coatedOralMEGA LIFESCIENCES SDN. BHD.2020-09-08Not applicableMalaysia flag
Medi-alpha Capsule 0.25 mcgCapsuleOralMEGA LIFESCIENCES SDN. BHD.2020-09-08Not applicableMalaysia flag

Categories

ATC Codes
A11CC03 — AlfacalcidolM05BB06 — Alendronic acid and alfacalcidol, sequential
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as vitamin d and derivatives. These are compounds containing a secosteroid backbone, usually secoergostane or secocholestane.
Kingdom
Organic compounds
Super Class
Lipids and lipid-like molecules
Class
Steroids and steroid derivatives
Sub Class
Vitamin D and derivatives
Direct Parent
Vitamin D and derivatives
Alternative Parents
Triterpenoids / Secondary alcohols / Cyclic alcohols and derivatives / Hydrocarbon derivatives
Substituents
Alcohol / Aliphatic homopolycyclic compound / Cyclic alcohol / Hydrocarbon derivative / Organic oxygen compound / Organooxygen compound / Secondary alcohol / Triterpenoid
Molecular Framework
Aliphatic homopolycyclic compounds
External Descriptors
diol, seco-cholestane, D3 vitamins, hydroxycalciol (CHEBI:31186) / Vitamin D3 and derivatives (LMST03020231)
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
URQ2517572
CAS number
41294-56-8
InChI Key
OFHCOWSQAMBJIW-AVJTYSNKSA-N
InChI
InChI=1S/C27H44O2/c1-18(2)8-6-9-19(3)24-13-14-25-21(10-7-15-27(24,25)5)11-12-22-16-23(28)17-26(29)20(22)4/h11-12,18-19,23-26,28-29H,4,6-10,13-17H2,1-3,5H3/b21-11+,22-12-/t19-,23-,24-,25+,26+,27-/m1/s1
IUPAC Name
(1R,3S,5Z)-5-{2-[(1R,3aS,4E,7aR)-7a-methyl-1-[(2R)-6-methylheptan-2-yl]-octahydro-1H-inden-4-ylidene]ethylidene}-4-methylidenecyclohexane-1,3-diol
SMILES
CC(C)CCC[C@@H](C)[C@@]1([H])CC[C@@]2([H])\C(CCC[C@]12C)=C\C=C1\C[C@@H](O)C[C@H](O)C1=C

References

General References
  1. Galesanu C, Ciubotariu C, Melnic G, Galesanu MR: [Postmenopausal osteoporosis. Digital Rx radiogrammetry in the diagnosis and follow-up of treatment with alfacalcidol]. Rev Med Chir Soc Med Nat Iasi. 2006 Oct-Dec;110(4):833-41. [Article]
  2. Ringe JD, Schacht E: Improving the outcome of established therapies for osteoporosis by adding the active D-hormone analog alfacalcidol. Rheumatol Int. 2007 Dec;28(2):103-11. doi: 10.1007/s00296-007-0422-6. Epub 2007 Aug 1. [Article]
  3. Vervloet M: Clinical uses of 1-alpha-hydroxycholecalciferol. Curr Vasc Pharmacol. 2014 Mar;12(2):300-5. doi: 10.2174/15701611113119990132. [Article]
  4. Richy F, Deroisy R, Lecart MP, Hanssens L, Mawet A, Reginster JY: D-hormone analog alfacalcidol: an update on its role in post-menopausal osteoporosis and rheumatoid arthritis management. Aging Clin Exp Res. 2005 Apr;17(2):133-42. doi: 10.1007/BF03324586. [Article]
  5. Shiraishi A, Takeda S, Masaki T, Higuchi Y, Uchiyama Y, Kubodera N, Sato K, Ikeda K, Nakamura T, Matsumoto T, Ogata E: Alfacalcidol inhibits bone resorption and stimulates formation in an ovariectomized rat model of osteoporosis: distinct actions from estrogen. J Bone Miner Res. 2000 Apr;15(4):770-9. doi: 10.1359/jbmr.2000.15.4.770. [Article]
  6. Shiraishi A, Higashi S, Ohkawa H, Kubodera N, Hirasawa T, Ezawa I, Ikeda K, Ogata E: The advantage of alfacalcidol over vitamin D in the treatment of osteoporosis. Calcif Tissue Int. 1999 Oct;65(4):311-6. doi: 10.1007/s002239900704. [Article]
  7. O'Donnell S, Moher D, Thomas K, Hanley DA, Cranney A: Systematic review of the benefits and harms of calcitriol and alfacalcidol for fractures and falls. J Bone Miner Metab. 2008;26(6):531-42. doi: 10.1007/s00774-008-0868-y. Epub 2008 Nov 1. [Article]
  8. Schacht E, Richy F, Reginster JY: The therapeutic effects of alfacalcidol on bone strength, muscle metabolism and prevention of falls and fractures. J Musculoskelet Neuronal Interact. 2005 Jul-Sep;5(3):273-84. [Article]
  9. LEO Pharma Inc. Product Monograph: ONE-ALPHA (alfacalcidol), for oral and intravenous use [Link]
  10. Biosynth Carbosynth: Alfacalcidol Safety Data Sheet [Link]
  11. AIFA Package Leaflet: DEDIOL (Alfacalcidol) for oral and intravenous use [Link]
  12. Summary of Product Characteristics: Alfacalcidol Aristo oral capsules [Link]
Human Metabolome Database
HMDB0015504
KEGG Drug
D01518
PubChem Compound
5282181
PubChem Substance
46505115
ChemSpider
4445376
RxNav
12062
ChEBI
31186
ChEMBL
CHEMBL1601669
ZINC
ZINC000012484965
PharmGKB
PA164746469
PDBe Ligand
M9B
Wikipedia
Alfacalcidol
AHFS Codes
  • 88:16.00 — Vitamin D
PDB Entries
6t0h
FDA label
Download (123 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedPreventionCardiac Valve Replacement Complication1
4CompletedTreatmentEnd Stage Renal Disease (ESRD) / Secondary Hyperparathyroidism (SHPT)1
4CompletedTreatmentFall / Osteopenia / Postmenopausal Osteoporosis1
4CompletedTreatmentSystemic Lupus Erythematosus (SLE)1
4CompletedTreatmentType 2 Diabetic Nephropathy1
4RecruitingTreatmentNephrotic Syndrome1
4Unknown StatusTreatmentElderly Infection / Frail Elderly Syndrome1
4Unknown StatusTreatmentOsteoporosis1
4WithdrawnPreventionAgeing / Falls, Accidental / Renal Insufficiency,Chronic1
3CompletedPreventionGiant Cell Arteritis (GCA) / Granulomatosis With Polyangiitis / Polymyalgia Rheumatica / Polymyositis / Rheumatoid Arthritis1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
CapsuleOral0.25 UG
CapsuleOral0.5 UG
CapsuleOral1 UG
CapsuleOral1.0 UG
TabletOral
Solution / dropsOral
SolutionOral2 UG/ML
CapsuleOral
Injection, solutionIntravenous
Capsule, liquid filledOral
Capsule, gelatin coatedOral
CapsuleOral1 mcg
CapsuleOral0.5 mcg
LiquidIntravenous2 mcg / mL
Solution / dropsOral2 mcg / mL
CapsuleOral0.25 mcg
LiquidOral.2 mcg / mL
Tablet
Prices
Unit descriptionCostUnit
One-Alpha 2 mcg/ml17.28USD ml
One-Alpha 2 mcg/ml Drops5.39USD ml
One-Alpha 1 mcg Capsule1.41USD capsule
One-Alpha 0.25 mcg Capsule0.47USD capsule
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)136 °CPhysProp
water solubility<1 mg/mLhttps://www.selleck.cn/msds/MSDS_S1468.pdf
Predicted Properties
PropertyValueSource
Water Solubility0.00163 mg/mLALOGPS
logP6.68ALOGPS
logP5.82ChemAxon
logS-5.4ALOGPS
pKa (Strongest Acidic)14.39ChemAxon
pKa (Strongest Basic)-2.8ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area40.46 Å2ChemAxon
Rotatable Bond Count6ChemAxon
Refractivity124.7 m3·mol-1ChemAxon
Polarizability50.55 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+0.9865
Blood Brain Barrier+0.9142
Caco-2 permeable+0.7866
P-glycoprotein substrateSubstrate0.7469
P-glycoprotein inhibitor INon-inhibitor0.5785
P-glycoprotein inhibitor IIInhibitor0.5574
Renal organic cation transporterNon-inhibitor0.7945
CYP450 2C9 substrateNon-substrate0.8188
CYP450 2D6 substrateNon-substrate0.8945
CYP450 3A4 substrateSubstrate0.7656
CYP450 1A2 substrateNon-inhibitor0.8249
CYP450 2C9 inhibitorNon-inhibitor0.8802
CYP450 2D6 inhibitorNon-inhibitor0.9434
CYP450 2C19 inhibitorNon-inhibitor0.7466
CYP450 3A4 inhibitorNon-inhibitor0.8596
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.5436
Ames testNon AMES toxic0.9077
CarcinogenicityNon-carcinogens0.9003
BiodegradationNot ready biodegradable0.9944
Rat acute toxicity4.6023 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.7959
hERG inhibition (predictor II)Non-inhibitor0.8176
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Targets

Drugtargets
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Kind
Protein
Organism
Humans
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...
Gene Name
VDR
Uniprot ID
P11473
Uniprot Name
Vitamin D3 receptor
Molecular Weight
48288.64 Da
References
  1. Reinhart GA: Vitamin D analogs: novel therapeutic agents for cardiovascular disease? Curr Opin Investig Drugs. 2004 Sep;5(9):947-51. [Article]
  2. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
  3. Fujishima T, Tsuji G, Tanaka C, Harayama H: Novel vitamin D receptor ligands having a carboxyl group as an anchor to arginine 274 in the ligand-binding domain. J Steroid Biochem Mol Biol. 2010 Jul;121(1-2):60-2. doi: 10.1016/j.jsbmb.2010.04.020. Epub 2010 May 6. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Iron ion binding
Specific Function
Catalyzes the conversion of 25-hydroxyvitamin D3 (25(OH)D) to 1-alpha,25-dihydroxyvitamin D3 (1,25(OH)2D) plays an important role in normal bone growth, calcium metabolism, and tissue differentiation.
Gene Name
CYP27B1
Uniprot ID
O15528
Uniprot Name
25-hydroxyvitamin D-1 alpha hydroxylase, mitochondrial
Molecular Weight
56503.475 Da
References
  1. Uchida E, Kagawa N, Sakaki T, Urushino N, Sawada N, Kamakura M, Ohta M, Kato S, Inouye K: Purification and characterization of mouse CYP27B1 overproduced by an Escherichia coli system coexpressing molecular chaperonins GroEL/ES. Biochem Biophys Res Commun. 2004 Oct 15;323(2):505-11. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Curator comments
Partial agonist.
General Function
Zinc ion binding
Specific Function
Receptor for retinoic acid. Retinoic acid receptors bind as heterodimers to their target response elements in response to their ligands, all-trans or 9-cis retinoic acid, and regulate gene expressi...
Gene Name
RXRA
Uniprot ID
P19793
Uniprot Name
Retinoic acid receptor RXR-alpha
Molecular Weight
50810.835 Da
References
  1. Zhang J, Chalmers MJ, Stayrook KR, Burris LL, Garcia-Ordonez RD, Pascal BD, Burris TP, Dodge JA, Griffin PR: Hydrogen/deuterium exchange reveals distinct agonist/partial agonist receptor dynamics within vitamin D receptor/retinoid X receptor heterodimer. Structure. 2010 Oct 13;18(10):1332-41. doi: 10.1016/j.str.2010.07.007. [Article]

Carriers

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Vitamin transporter activity
Specific Function
Involved in vitamin D transport and storage, scavenging of extracellular G-actin, enhancement of the chemotactic activity of C5 alpha for neutrophils in inflammation and macrophage activation.
Gene Name
GC
Uniprot ID
P02774
Uniprot Name
Vitamin D-binding protein
Molecular Weight
52963.025 Da
References
  1. Nykjaer A, Dragun D, Walther D, Vorum H, Jacobsen C, Herz J, Melsen F, Christensen EI, Willnow TE: An endocytic pathway essential for renal uptake and activation of the steroid 25-(OH) vitamin D3. Cell. 1999 Feb 19;96(4):507-15. [Article]
  2. Verboven C, Rabijns A, De Maeyer M, Van Baelen H, Bouillon R, De Ranter C: A structural basis for the unique binding features of the human vitamin D-binding protein. Nat Struct Biol. 2002 Feb;9(2):131-6. [Article]
  3. Houghton LA, Vieth R: The case against ergocalciferol (vitamin D2) as a vitamin supplement. Am J Clin Nutr. 2006 Oct;84(4):694-7. [Article]
  4. Yamamoto N, Naraparaju VR: Vitamin D3-binding protein as a precursor for macrophage activating factor in the inflammation-primed macrophage activation cascade in rats. Cell Immunol. 1996 Jun 15;170(2):161-7. [Article]
  5. Yamamoto N, Naraparaju VR: Role of vitamin D3-binding protein in activation of mouse macrophages. J Immunol. 1996 Aug 15;157(4):1744-9. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Binder
General Function
Not Available
Specific Function
Heme binding
Gene Name
Not Available
Uniprot ID
V9H1D9
Uniprot Name
Alpha globin
Molecular Weight
13582.405 Da
References
  1. LEO Pharma Inc. Product Monograph: ONE-ALPHA (alfacalcidol), for oral and intravenous use [Link]
  2. Summary of Product Characteristics: Alfacalcidol Aristo oral capsules [Link]

Drug created on July 26, 2007 12:34 / Updated on June 23, 2021 06:08