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

Stem definitionDrug idCAS RN
Vitamin D analogues/derivatives 464 19356-17-3

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • calcifediol
  • calcidiol
  • calderol
The major circulating metabolite of VITAMIN D3. It is produced in the LIVER and is the best indicator of the body's vitamin D stores. It is effective in the treatment of RICKETS and OSTEOMALACIA, both in azotemic and non-azotemic patients. Calcifediol also has mineralizing properties.
  • Molecular weight: 400.65
  • Formula: C27H44O2
  • CLOGP: 7.27
  • LIPINSKI: 1
  • HAC: 2
  • HDO: 2
  • TPSA: 40.46
  • ALOGS: -5.26
  • ROTB: 6

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
30 mcg O

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Aug. 5, 1980 FDA

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
Hyponatraemia 37.22 27.25 27 1445 96112 50507540
Drug interaction 28.66 27.25 32 1440 199589 50404063
Spinal fracture 27.82 27.25 12 1460 15561 50588091

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
Intracranial pressure increased 40.37 36.13 11 878 3474 29570164
Thoracic vertebral fracture 39.39 36.13 9 880 1389 29572249

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
Thoracic vertebral fracture 56.60 25.61 16 2444 4537 64491735
Drug interaction 48.47 25.61 64 2396 362019 64134253
Hypertensive crisis 31.80 25.61 15 2445 18233 64478039
Acute kidney injury 31.45 25.61 59 2401 449181 64047091
Hyponatraemia 31.01 25.61 33 2427 148306 64347966
Intracranial pressure increased 30.21 25.61 11 2449 6978 64489294
Eosinophilia 26.32 25.61 17 2443 38059 64458213
Eosinophilic pleural effusion 25.89 25.61 5 2455 268 64496004

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC A11CC06 ALIMENTARY TRACT AND METABOLISM
VITAMINS
VITAMIN A AND D, INCL. COMBINATIONS OF THE TWO
Vitamin D and analogues
ATC H05BX05 SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS
CALCIUM HOMEOSTASIS
ANTI-PARATHYROID AGENTS
Other anti-parathyroid agents
MeSH PA D050071 Bone Density Conservation Agents
MeSH PA D018977 Micronutrients
MeSH PA D014815 Vitamins
CHEBI has role CHEBI:25212 metabolites
CHEBI has role CHEBI:50646 antiosteoporotic
CHEBI has role CHEBI:50733 Dietary Supplement
CHEBI has role CHEBI:75771 Mus musculus metabolites
CHEBI has role CHEBI:77746 Homo sapiens metabolite

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Hypophosphatemia indication 4996001
Hypocalcemia indication 5291005
Renal osteodystrophy indication 16726004 DOID:13068
Rickets indication 41345002 DOID:10609
Vitamin D deficiency off-label use 34713006
Hyperphosphatemia contraindication 20165001 DOID:0050459
Hypervitaminosis D contraindication 27712000 DOID:9971
Sarcoidosis contraindication 31541009 DOID:11335
Hypercalcemia contraindication 66931009 DOID:12678
Kidney disease contraindication 90708001 DOID:557
Kidney stone contraindication 95570007
Arteriosclerosis obliterans contraindication 361133006 DOID:5160




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
0.03MG RAYALDEE EIRGEN N208010 June 17, 2016 RX CAPSULE, EXTENDED RELEASE ORAL 9943530 Feb. 2, 2027 MAINTAINING SERUM 25-HYDROXYVITAMIN D AT A LEVEL OF AT LEAST 30 NG/ML WITH ORAL, SUSTAINED RELEASE 25-HYDROXYVITAMIN D
0.03MG RAYALDEE EIRGEN N208010 June 17, 2016 RX CAPSULE, EXTENDED RELEASE ORAL 11154509 April 25, 2028 TREATING SECONDARY HYPERPARATHYROIDISM IN STAGE 3/4 CHRONIC KIDNEY DISEASE WITH SUSTAINED RELEASE 25-HYDROXYVITAMIN D TO REDUCE THE PATIENTS SERUM PARATHYROID HORMONE LEVEL WHILE AVOIDING PTH OVERSUPPRESSION
0.03MG RAYALDEE EIRGEN N208010 June 17, 2016 RX CAPSULE, EXTENDED RELEASE ORAL 8207149 April 25, 2028 TREATMENT OF SECONDARY HYPERPARATHYROIDISM IN PATIENTS WITH STAGE 3 OR 4 CHRONIC KIDNEY DISEASE USING CONTROLLED RELEASE, ORAL 25-HYDROXYVITAMIN D
0.03MG RAYALDEE EIRGEN N208010 June 17, 2016 RX CAPSULE, EXTENDED RELEASE ORAL 8778373 April 25, 2028 ADMINISTRATION OF 25-HYDROXYVITAMIN D3 BY CONTROLLED RELEASE
0.03MG RAYALDEE EIRGEN N208010 June 17, 2016 RX CAPSULE, EXTENDED RELEASE ORAL 9408858 April 25, 2028 USE OF CONTROLLED RELEASE 25-HYDROXYVITAMIN D IN TREATING SECONDARY HYPERPARATHYROIDISM IN PATIENTS HAVING CHRONIC KIDNEY DISEASE
0.03MG RAYALDEE EIRGEN N208010 June 17, 2016 RX CAPSULE, EXTENDED RELEASE ORAL 9498486 April 25, 2028 USE OF EXTENDED RELEASE ORAL 25-HYDROXYVITAMIN D3 IN TREATING SECONDARY HYPERPARATHYROIDISM IN ADULT PATIENTS HAVING CHRONIC KIDNEY DISEASE STAGE 3 OR STAGE 4
0.03MG RAYALDEE EIRGEN N208010 June 17, 2016 RX CAPSULE, EXTENDED RELEASE ORAL 9925147 April 25, 2028 TREATING SECONDARY HYPERPARATHYROIDISM IN CHRONIC KIDNEY DISEASE WITH SUSTAINED RELEASE 25-HYDROXYVITAMIN D TO REDUCE THE PATIENTS SERUM PARATHYROID HORMONE LEVEL AND CMAX IS REDUCED COMPARED TO BOLUS IV INJECTION AND IMMEDIATE-RELEASE, ORAL DOSING
0.03MG RAYALDEE EIRGEN N208010 June 17, 2016 RX CAPSULE, EXTENDED RELEASE ORAL 9925147 April 25, 2028 TREATING SECONDARY HYPERPARATHYROIDISM IN CHRONIC KIDNEY DISEASE WITH SUSTAINED RELEASE 25-HYDROXYVITAMIN D TO REDUCE THE PATIENTS SERUM PARATHYROID HORMONE LEVEL AND THE SUSTAINED RELEASE IS OVER AT LEAST 10 HOURS
0.03MG RAYALDEE EIRGEN N208010 June 17, 2016 RX CAPSULE, EXTENDED RELEASE ORAL 9925147 April 25, 2028 TREATING SECONDARY HYPERPARATHYROIDISM IN CKD WITH SUSTAINED RELEASE CALCIFEDIOL TO REDUCE THE PATIENTS SERUM PARATHYROID HORMONE LEVEL AND CMAX24HR/C24HR IS REDUCED COMPARED TO BOLUS IV INJECTION AND IMMEDIATE-RELEASE, ORAL DOSING
0.03MG RAYALDEE EIRGEN N208010 June 17, 2016 RX CAPSULE, EXTENDED RELEASE ORAL 9925147 April 25, 2028 TREATING SECONDARY HYPERPARATHYROIDISM IN CKD WITH SUSTAINED RELEASE CALCIFEDIOL TO REDUCE THE PATIENTS SERUM PARATHYROID HORMONE LEVEL AND TMAX IS INCREASED COMPARED TO BOLUS IV INJECTION AND IMMEDIATE-RELEASE, ORAL DOSING
0.03MG RAYALDEE EIRGEN N208010 June 17, 2016 RX CAPSULE, EXTENDED RELEASE ORAL 9925147 April 25, 2028 TREATING SHPT IN CKD WITH SUSTAINED RELEASE CALCIFEDIOL TO REDUCE SERUM PARATHYROID HORMONE LEVEL AND CHANGE IN SERUM CONCENTRATION OF CALCIFEDIOL IN DOSE INTERVAL IS REDUCED COMPARED TO BOLUS IV INJECTION AND IMMEDIATE-RELEASE, ORAL DOSING
0.03MG RAYALDEE EIRGEN N208010 June 17, 2016 RX CAPSULE, EXTENDED RELEASE ORAL 8426391 Aug. 27, 2028 USE OF SUSTAINED RELEASE 25-HYDROXYVITAMIN D IN TREATING PATIENTS HAVING 25-HYDROXYVITAMIN D INSUFFICIENCY OR DEFICIENCY

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 CHEMBL CHEMBL
Vitamin D3 receptor Nuclear hormone receptor EC50 6.22 CHEMBL

External reference:

IDSource
4022405 VUID
N0000020410 NUI
D00122 KEGG_DRUG
1889 RXNORM
C0006657 UMLSCUI
CHEBI:17933 CHEBI
CHEMBL1040 ChEMBL_ID
CHEMBL3544909 ChEMBL_ID
DB00146 DRUGBANK_ID
6921 IUPHAR_LIGAND_ID
P6YZ13C99Q UNII
5283731 PUBCHEM_CID
399 MMSL
4321 MMSL
d03127 MMSL
001016 NDDF
259337002 SNOMEDCT_US
88519001 SNOMEDCT_US
4021905 VANDF
4022405 VANDF
D002112 MESH_DESCRIPTOR_UI
63283-36-3 SECONDARY_CAS_RN

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Rayaldee HUMAN PRESCRIPTION DRUG LABEL 1 70301-1001 CAPSULE, EXTENDED RELEASE 30 ug ORAL NDA 26 sections