Accession Number
DB00136  (NUTR00003, APRD00246, DB05314)
Small Molecule
Approved, Nutraceutical

Calcitriol is an active metabolite of vitamin D with 3 hydroxyl (OH) groups and is commonly referred to as 1,25-dihydroxycholecalciferol, or 1alpha,25-dihydroxyvitamin D3, 1,25-dihydroxyvitamin D3. It is produced in the body after series of conversion steps of 7-dehydrocholesterol from exposure to UV light. 7-dehydrocholesterol is converted to Vitamin D3 (vitamin D3) in the skin, which is then converted to Calcifediol in the liver and kidneys. Calcifediol undergoes hydroxylation to form calcitriol via 1α-hydroxylase (CYP27B1) activity 4. Calcitriol is considered to be the most potent metabolite of vitamin D in humans 1. Renal production of calcitriol is stimulated in response to PTH, low calcium and low phosphate 4. Calcitriol plays a role in plasma calcium regulation in concert with parathyroid hormone (PTH) by enhancing absorption of dietary calcium and phosphate from the gastrointestinal tract, promoting renal tubular reabsorption of calcium in the kidneys, and stimulating the release of calcium stores from the skeletal system. In addition to promoting fatty acid synthesis and inhibiting lipolysis, calcitriol has been demonstrated to increase energy efficiency by suppressing UCP2 expression, which is modulated by signaling pathways of classical nuclear receptors (nVDR), where calcitriol acts as a natural ligand 3. There is also evidence that calcitriol modulates the action of cytokines and may regulate immune and inflammatory response, cell turnover, cell differentiation 4.

Administered orally and intravenously, calcitriol is commonly used as a medication in the treatment of secondary hyperparathyroidism and resultant metabolic bone disease, hypocalcemia in patients undergoing chronic renal dialysis, and osteoporosis. It is also available in topical form for the treatment of mild to moderate plaque psoriasis in adults. Calcitriol is marketed under various trade names including Rocaltrol (Roche), Calcijex (Abbott) and Decostriol (Mibe, Jesalis).

  • (1S,3R,5Z,7E)-9,10-secocholesta-5,7,10-triene-1,3,25-triol
  • (1α,3β,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-1,3,25-triol
  • (5Z,7E)-(1S,3R)-9,10-secocholesta-5,7,10(19)-triene-1,3,25-triol
  • 1-alpha-25-Dihydroxyvitamin D3
  • 1,25-DHCC
  • 1,25-dihydroxycholecalciferol
  • 1α,25-dihydroxycholecalciferol
  • 1α,25-dihydroxyvitamin D3
  • 1α,25(OH)2D3
  • Calcitriol
  • Calcitriolum
External IDs
DN-101 / RO 21-5535 / RO-21-5535 / RO-215535
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
CalcijexSolution2 mcgIntravenousAbbvie1990-12-312017-01-13Canada
CalcijexSolution1 mcgIntravenousAbbvie1990-12-312017-01-13Canada
CalcijexInjection, solution1 ug/1mLIntravenousAbbvie2010-06-012012-08-01Us
CalcitriolSolution1 ug/1mLIntravenousNEPHRX, LLC2009-01-27Not applicableUs
CalcitriolOintment3 ug/1gTopicalPerrigo New York Inc2012-03-08Not applicableUs
CalcitriolInjection, solution2 ug/1mLIntravenousAMERICAN REGENT, INC.2007-01-012007-01-01Us
Calcitriol CapsulesCapsuleOralStrides Pharma Canada Inc2020-03-09Not applicableCanada
Calcitriol CapsulesCapsuleOralStrides Pharma Canada Inc2020-03-09Not applicableCanada
Calcitriol InjectionSolutionIntravenousFresenius Kabi2003-07-07Not applicableCanada
Calcitriol Injection USPSolutionIntravenousSterimax Inc2015-04-16Not applicableCanada
Additional Data Available
  • Application Number
    Application Number

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  • Product Code
    Product Code

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Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
CalcitriolCapsule0.25 ug/1OralWest-Ward Pharmaceuticals Corp.2006-03-27Not applicableUs00054 0007 25 nlmimage10 6f3fb7bd
CalcitriolCapsule0.25 ug/1OralSun Pharmaceutical Industries, Inc.2009-08-26Not applicableUs
CalcitriolCapsule, liquid filled0.25 ug/1OralGolden State Medical Supply Inc.2013-05-24Not applicableUs
CalcitriolInjection1 ug/1mLIntravenousAkorn2011-10-14Not applicableUs
CalcitriolCapsule0.25 ug/1OralAmerican Health Packaging2019-01-23Not applicableUs
CalcitriolCapsule, liquid filled0.50 ug/1OralGolden State Medical Supply2014-11-262017-01-02Us
CalcitriolCapsule, liquid filled0.5 ug/1OralTeva Pharmaceuticals USA, Inc.2016-07-01Not applicableUs
CalcitriolCapsule, liquid filled0.25 ug/1OralNucare Pharmaceuticals,inc.2013-05-29Not applicableUs
CalcitriolCapsule, liquid filled0.25 ug/1OralTeva Pharmaceuticals USA, Inc.2016-08-25Not applicableUs
CalcitriolCapsule, liquid filled0.50 ug/1OralBionpharma Inc.2018-06-12Not applicableUs
Additional Data Available
  • Application Number
    Application Number

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  • Product Code
    Product Code

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Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
ValidermCalcitriol (0.2 mg/0.2mg) + Fluticasone propionate (0.05 g/0.05g) + Tacrolimus hydrate (0.05 g/0.05g)KitTopicalAccumix Pharmaceuticals2014-12-152015-07-17Us
International/Other Brands
Asentar (Novacea) / Calcitriol Oral Solution (Roxane) / Decostriol (Mibe Jena (Germany), Jesalis (Hong Kong, Thailand))
CAS number
Average: 416.6365
Monoisotopic: 416.329045274
Chemical Formula
InChI Key



Used to treat vitamin D deficiency or insufficiency, refractory rickets (vitamin D resistant rickets), familial hypophosphatemia and hypoparathyroidism, and in the management of hypocalcemia and renal osteodystrophy in patients with chronic renal failure undergoing dialysis. Also used in conjunction with calcium in the management and prevention of primary or corticosteroid-induced osteoporosis.

Associated Conditions

Calcitriol is a biologically active calcitrophic hormone with anti-osteoporotic, immunomodulatory, anticarcinogenic, antipsoriatic, antioxidant, and mood-modulatory activities. Its main sites of action are the intestine, bone, kidney and parathyroid hormone Label. Calcitriol is a ligand for the vitamin D nuclear receptor, which is expressed in, but not limited to, gastrointestinal (GI) tissues, bones, and kidneys 1. As an active form of vitamin D3, calcitriol elevates the plasma levels of calcium by stimulating intestinal calcium uptake, increasing reabsorption of calcium by the kidneys, and possibly increasing the release of calcium from skeletal stores. The duration of pharmacologic activity of a single dose of exogenous calcitriol is expected to be about 3 to 5 days Label.

In addition to its important role in calcium metabolism, other pharmacological effects of calcitriol have been studied in various conditions including cancer models. Various studies demonstrated expression of vitamin D receptors in cancer cell lines, including mouse myeloid leukemia cells 1. Calcitriol has been found to induce differentiation and/or inhibit cell proliferation in vitro and in vivo in many cell types, such as malignant cell lines carcinomas of the breast, prostate, colon, skin, and brain, myeloid leukemia cells, and others 2. In early human prostate cancer trials, administration of 1.5 µg/d calcitriol in male participants resulted in a reduction in the rate of PSA rise in most participants, however it was coincided with dose-limiting hypercalcemia in most participants 1. Hypercalcemia and hypercalcuria were evident in numerous initial trials, and this may be due to these trials not testing the drug at concentrations that are active in preclinical systems 2. Findings from preclinical data show an additive or synergistic antineoplastic action of calcitriol when combined with agents including dexamethasone, retinoids, and radiation, as well as several cytotoxic chemotherapy drugs such as platinum compounds 2.

Vitamin D deficiency has long been suspected to increase the susceptibility to tuberculosis. The active form of calcitriol, 1,25-(OH)2-D3, has been found to enhance the ability of mononuclear phagocytes to suppress the intracellular growth of Mycobacterium tuberculosis. 1,25-(OH)2-D3 has demonstrated beneficial effects in animal models of such autoimmune diseases as rheumatoid arthritis. Vitamin D appears to demonstrate both immune-enhancing and immunosuppressive effects.

Mechanism of action

The mechanism of action of calcitriol in the treatment of psoriasis is accounted for by their antiproliferative activity for keratinocytes and their stimulation of epidermal cell differentiation. The anticarcinogenic activity of the active form of Calcitriol appears to be correlated with cellular vitamin D receptor (VDR) levels. Vitamin D receptors belong to the superfamily of steroid-hormone zinc-finger receptors. VDRs selectively bind 1,25-(OH)2-D3 and retinoic acid X receptor (RXR) to form a heterodimeric complex that interacts with specific DNA sequences known as vitamin D-responsive elements. VDRs are ligand-activated transcription factors. The receptors activate or repress the transcription of target genes upon binding their respective ligands. It is thought that the anticarcinogenic effect of Calcitriol is mediated via VDRs in cancer cells. The immunomodulatory activity of calcitriol is thought to be mediated by vitamin D receptors (VDRs) which are expressed constitutively in monocytes but induced upon activation of T and B lymphocytes. 1,25-(OH)2-D3 has also been found to enhance the activity of some vitamin D-receptor positive immune cells and to enhance the sensitivity of certain target cells to various cytokines secreted by immune cells.

A study suggests that calcitriol plays an immunoregulatry role by suppressing the aryl hydrocarbon receptor (AhR) expression in human Th9, a pro-inflammatory CD4 T cell subset 9. This suppression subsequently leads to repressed expression of BATF, a transcription factor essential for Th9 9. Calcitriol has also been found to induce monocyte differentiation and to inhibit lymphocyte proliferation and production of cytokines, including interleukin IL-1 and IL-2, as well as to suppress immunoglobulin secretion by B lymphocytes.

AVitamin D3 receptor
UHomeobox protein Hox-A10Not AvailableHumans
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Upon administration, calcitriol is rapidly absorbed from the intestines. When a single oral dose of 0.5 mcg of calcitriol was administered, the mean serum concentrations of calcitriol rose from a baseline value of 40.0±4.4 (SD) pg/mL to 60.0±4.4 pg/mL at 2 hours, and declined to 53.0±6.9 at 4 hours, 50±7.0 at 8 hours, 44±4.6 at 12 hours and 41.5±5.1 at 24 hours Label. Following administration of single doses of 0.25 to 1.0 mcg of calcitriol, the peak plasma concentrations were reached within 3 to 6 hours Label. In a pharmacokinetic study, the oral bioavailability was 70.6±5.8% in healthy male volunteers and 72.2±4.8% in male patients with uraemia 8.

Volume of distribution

Upon intravenous administration, the volume of distribution of calcitriol was 0.49±0.14 L/kg in healthy male volunteers and 0.27±0.06 l/kg in uraemic male patients participating in a pharmacokinetic study 8. There is some evidence that calcitriol is transferred into human milk at low levels (ie, 2.2±0.1 pg/mL) in mothers Label. Calcitriol from maternal circulation may also enter the fetal circulation Label.

Protein binding

Calcitriol is approximately 99.9% bound in blood, mostly by an alpha-globulin vitamin D binding protein Label.


Metabolism of calcitriol involves two pathways Label. The first pathway involves 24-hydroxylase activity in the kidney; this enzyme is also present in many target tissues which possess the vitamin D receptor such as the intestine. The end product of this pathway is a side chain shortened metabolite, calcitroic acid. The second pathway involves the conversion of calcitriol via the stepwise hydroxylation of carbon-26 and carbon-23, and cyclization to yield ultimately 1a,25R(OH)2-26,23S-lactone D3, which appears to be the major metabolite circulating in humans.

Ohter identified metabolites of calcitriol include 1α, 25(OH)2-24-oxo-D3; 1α, 23,25(OH)3-24-oxo-D3; 1α, 24R,25(OH)3D3; 1α, 25S,26(OH)3D3; 1α, 25(OH)2-23-oxo-D3; 1α, 25R,26(OH)3-23-oxo-D3 and 1α, (OH)24,25,26,27-tetranor-COOH-D3 Label.

Route of elimination

In normal subjects, approximately 27% and 7% of the radioactivity appeared in the feces and urine, respectively, within 24 hours Label. Calcitriol undergoes enterohepatic recycling and biliary excretion. The metabolites of calcitriol are excreted primarily in feces. Cumulative excretion of radioactivity on the sixth day following intravenous administration of radiolabeled calcitriol averaged 16% in urine and 49% in feces Label.

Half life

After administration of single oral doses, the elimination half life was 5-8 hours Label.


The metabolic clearance rate was 23.5±4.34 ml/min in healthy male volunteers and 10.1±1.35 ml/min in male patients with uraemia 8. In the pediatric patients undergoing peritoneal dialysis receiving dose of 10.2 ng/kg (SD 5.5 ng/kg) for 2 months, the clearance rate was 15.3 mL/hr/kg Label.


LD50 (oral, rat) = 620 μg/kg; LD50 (intraperitoneal, rat) > 5 mg/kg MSDS.

Symptoms of calcitriol toxicity mirrors the early and late signs and symptoms of vitamin D intoxication associated with hypercalcemia 10. Early signs include weakness, headache, somnolence, nausea, vomiting, dry mouth, constipation, muscle pain, bone pain and metallic taste. Late signs are characterized by polyuria, polydipsia, anorexia, weight loss, nocturia, conjunctivitis (calcific), pancreatitis, photophobia, rhinorrhea, pruritus, hyperthermia, decreased libido, elevated BUN, albuminuria, hypercholesterolemia, elevated SGOT and SGPT, ectopic calcification, hypertension, cardiac arrhythmias and, rarely, overt psychosis 10.

Affected organisms
  • Humans and other mammals
Not Available
Pharmacogenomic Effects/ADRs
Not Available


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.
(R)-warfarinThe metabolism of (R)-warfarin can be increased when combined with Calcitriol.
(S)-WarfarinThe metabolism of (S)-Warfarin can be increased when combined with Calcitriol.
1alpha-Hydroxyvitamin D5The risk or severity of adverse effects can be increased when Calcitriol is combined with 1alpha-Hydroxyvitamin D5.
1alpha,24S-Dihydroxyvitamin D2The risk or severity of adverse effects can be increased when Calcitriol is combined with 1alpha,24S-Dihydroxyvitamin D2.
4-hydroxycoumarinThe metabolism of 4-hydroxycoumarin can be increased when combined with Calcitriol.
9-aminocamptothecinThe metabolism of 9-aminocamptothecin can be increased when combined with Calcitriol.
AbirateroneThe metabolism of Abiraterone can be increased when combined with Calcitriol.
AcalabrutinibThe metabolism of Acalabrutinib can be increased when combined with Calcitriol.
AcenocoumarolThe metabolism of Acenocoumarol can be increased when combined with Calcitriol.
AcetyldigitoxinThe risk or severity of ventricular arrhythmias and Cardiac Arrhythmia can be increased when Calcitriol is combined with Acetyldigitoxin.
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Food Interactions
No interactions found.


Synthesis Reference

Raymond E. Conrow, "Process for preparation of calcitriol lactone and related intermediates." U.S. Patent US5457245, issued April, 1994.

General References
  1. Brawer MK: Recent Progress in the Treatment of Advanced Prostate Cancer With Intermittent Dose-Intense Calcitriol (DN-101). Rev Urol. 2007 Winter;9(1):1-8. [PubMed:17396166]
  2. Beer TM, Javle M, Lam GN, Henner WD, Wong A, Trump DL: Pharmacokinetics and tolerability of a single dose of DN-101, a new formulation of calcitriol, in patients with cancer. Clin Cancer Res. 2005 Nov 1;11(21):7794-9. [PubMed:16278401]
  3. Zemel MB, Sun X: Calcitriol and energy metabolism. Nutr Rev. 2008 Oct;66(10 Suppl 2):S139-46. doi: 10.1111/j.1753-4887.2008.00099.x. [PubMed:18844841]
  4. Rodriguez M, Munoz-Castaneda JR, Almaden Y: Therapeutic use of calcitriol. Curr Vasc Pharmacol. 2014 Mar;12(2):294-9. [PubMed:23713873]
  5. Dechant KL, Goa KL: Calcitriol. A review of its use in the treatment of postmenopausal osteoporosis and its potential in corticosteroid-induced osteoporosis. Drugs Aging. 1994 Oct;5(4):300-17. doi: 10.2165/00002512-199405040-00006. [PubMed:7827399]
  6. Toussaint ND, Damasiewicz MJ: Do the benefits of using calcitriol and other vitamin D receptor activators in patients with chronic kidney disease outweigh the harms? Nephrology (Carlton). 2017 Mar;22 Suppl 2:51-56. doi: 10.1111/nep.13026. [PubMed:28429545]
  7. Farach-Carson MC, Nemere I: Membrane receptors for vitamin D steroid hormones: potential new drug targets. Curr Drug Targets. 2003 Jan;4(1):67-76. [PubMed:12528991]
  8. Brandi L, Egfjord M, Olgaard K: Pharmacokinetics of 1,25(OH)2D3 and 1α(OH)D3 in normal and uraemic men Nephrology Dialysis Transplantation. 2002 May 1;17(5):829–842.
  9. Takami M, Fujimaki K, Nishimura MI, Iwashima M: Cutting Edge: AhR Is a Molecular Target of Calcitriol in Human T Cells. J Immunol. 2015 Sep 15;195(6):2520-3. doi: 10.4049/jimmunol.1500344. Epub 2015 Aug 14. [PubMed:26276877]
  10. 1,25-DIHYDROXYCHOLECALCIFEROL - National Library of Medicine HSDB Database - ToxNet - NIH [Link]
External Links
Human Metabolome Database
KEGG Compound
PubChem Compound
PubChem Substance
Therapeutic Targets Database
Guide to Pharmacology
GtP Drug Page
PDBe Ligand
RxList Drug Page Drug Page
PDRhealth Drug Page
ATC Codes
D05AX03 — CalcitriolA11CC04 — Calcitriol
AHFS Codes
  • 84:92.00 — Misc. Skin and Mucous Membrane Agents
  • 88:16.00 — Vitamin D
PDB Entries
1db1 / 1ie9 / 1rk3 / 2hc4 / 2zbz / 2zlc / 3cv9 / 3m7r / 3vt3 / 3vt7
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Clinical Trials

Clinical Trials
0CompletedNot AvailableAnemia of Chronic Disease / Chronic Kidney Disease (CKD)1
0Not Yet RecruitingTreatmentPostmenopausal Osteoporoses1
0RecruitingTreatmentHypophosphatemic Rickets / Hypophosphatemic Rickets, X-Linked Dominant / X-linked Hypophosphatemia (XLH)1
0TerminatedTreatmentDeficiency, Vitamin D / High Blood Pressure (Hypertension)1
1Active Not RecruitingPreventionBreast Cancer / Cervical Cancers / Endometrial Cancer / Malignancies / Ovarian Cancer / Primary Peritoneal Carcinoma / Sarcoma, Bone / Tumors, Solid1
1CompletedNot AvailableHealthy Volunteers1
1CompletedNot AvailablePostmenopausal Osteoporosis, Multiple Sites / To Study the Safety and Tolerability of 2MD in Postmenopausal Women, the Intended Target Population1
1CompletedPreventionAdenocarcinomas / Colorectal Adenomas / Colorectal Polyps1
1CompletedTreatmentPsoriasis / Psoriasis Vulgaris (Plaque Psoriasis)1
1Not Yet RecruitingPreventionPre-Diabetic1
1Not Yet RecruitingTreatmentAttention Deficit Disorder With Hyperactivity (ADHD)1
1, 2CompletedBasic ScienceMouth Neoplasms1
1, 2CompletedTreatmentCrohn's Disease (CD)1
1, 2CompletedTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
1, 2TerminatedTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
2Active Not RecruitingPreventionBone Loss / Calcifications, Vascular / End Stage Renal Disease (ESRD) / Fracture Bone / Transplantation, Kidney1
2Active Not RecruitingPreventionBreast Cancer1
2CompletedNot AvailableType 1 Diabetes Mellitus1
2CompletedPreventionBone and Bones / Neoplasms, Breast1
2CompletedPreventionType 1 Diabetes Mellitus1
2CompletedTreatmentBasal Cell Carcinoma (BCC)1
2CompletedTreatmentChronic Plaque Psoriasis1
2CompletedTreatmentEnd Stage Renal Disease (ESRD) / Renal Osteodystrophy1
2CompletedTreatmentHyperparathyroidism, Secondary / Renal Osteodystrophy1
2CompletedTreatmentKlinefelter's Syndrome / Men Infertility / Y-chromosome Microdeletions1
2CompletedTreatmentMyelodysplastic Syndromes1
2CompletedTreatmentPsoriasis Vulgaris (Plaque Psoriasis)1
2CompletedTreatmentSevere Sepsis or Septic Shock1
2CompletedTreatmentParathyroid deficiency1
2RecruitingPreventionAcute Kidney Injury (AKI) / Critically-ill Patients1
2RecruitingSupportive CareChronic Obstructive Pulmonary Disease (COPD)1
2SuspendedTreatmentMalignant Neoplasm of Pancreas1
2TerminatedTreatmentCastration-Resistant Prostate Cancer (CRPC)1
2TerminatedTreatmentHypocalcemia / Hypovitaminosis D1
2TerminatedTreatmentProstate Cancer1
2TerminatedTreatmentProstate Cancer / Prostatic Neoplasms1
2Unknown StatusTreatmentAdvanced Intrahepatic Cholangiocarcinoma1
2Unknown StatusTreatmentAndrogen Independent Prostate Cancer (AIPC) / Lung Cancer Non-Small Cell Cancer (NSCLC)1
2Unknown StatusTreatmentMyelodysplastic Syndrome1
2Unknown StatusTreatmentSystemic Lupus Erythematosus (SLE)1
2, 3Unknown StatusTreatmentProstate Cancer1
3CompletedPreventionCardiac Transplantation / Osteoporosis1
3CompletedTreatmentArterial Dysfunction / Chronic Kidney Disease (CKD)1
3CompletedTreatmentChronic Kidney Disease (CKD) / Deficiency, Vitamin D / Hyperparathyroidism, Secondary1
3CompletedTreatmentFacial Angiofibroma1
3RecruitingTreatmentDiabetic Nephropathies1
3RecruitingTreatmentSecondary Hyperparathyroidism-Chronic Kidney Disease1
3TerminatedPreventionAdenomatous Polyps1
3TerminatedTreatmentProstate Cancer1
4CompletedPreventionChronic Kidney Disease (CKD) / Coronary Calcification / Deficiency, Vitamin D / Disorders of Calcium and Bone Metabolism1
4CompletedTreatmentAnemia / Chronic Kidney Disease (CKD)1
4CompletedTreatmentCardiorenal Syndrome / Chronic Allograft Nephropathy (CAN)1
4CompletedTreatmentChronic Kidney Disease (CKD) / Hyperparathyroidism, Secondary2
4CompletedTreatmentChronic Stable Plaque Psoriasis1
4CompletedTreatmentDeficiency, Vitamin D1
4CompletedTreatmentEnd Stage Renal Disease (ESRD) / Hyperparathyroidism, Secondary1
4CompletedTreatmentIgA Nephropathy1
4CompletedTreatmentPityriasis Alba1
4CompletedTreatmentPostmenopausal Osteoporosis (PMO)1
4CompletedTreatmentPsoriasis Vulgaris (Plaque Psoriasis)4
4CompletedTreatmentStage 3 Chronic Kidney Disease1
4Enrolling by InvitationSupportive CareMalignancies1
4Not Yet RecruitingPreventionChronic Kidney Disease Stage 1 / Chronic Kidney Disease Stage 21
4Not Yet RecruitingTreatmentImmune Thrombocytopenia1
4RecruitingTreatmentX-linked Hypophosphatemia (XLH)1
4TerminatedTreatmentDialysis therapy / Hyperparathyroidism, Secondary1
4TerminatedTreatmentEnd-Stage Kidney Disease1
4TerminatedTreatmentHypercalcemia / Hyperparathyroidism, Secondary / Hyperphosphataemia / Renal Failure1
4Unknown StatusScreeningDiabetic Nephropathies1
4Unknown StatusTreatmentAsthma1
4Unknown StatusTreatmentAutoimmune Diseases / Glomerulonephritis1
4Unknown StatusTreatmentChronic Kidney Disease (CKD) / Proteinuria1
4Unknown StatusTreatmentOsteoporosis1
4Unknown StatusTreatmentProteinuria1
4WithdrawnTreatmentNephritis / Proteinuria / Systemic Lupus Erythematosus (SLE)1
Not AvailableCompletedPreventionBMI >30 kg/m2 / Type 2 Diabetes Mellitus1
Not AvailableCompletedPreventionLung Cancers / Precancerous Conditions / Tobacco Use Disorders1
Not AvailableCompletedTreatmentCrohn's Disease (CD) / Rheumatoid Arthritis1
Not AvailableCompletedTreatmentHIV Seropositive1
Not AvailableCompletedTreatmentHyperparathyroidism, Secondary / Hypocalcemia1
Not AvailableCompletedTreatmentHyperparathyroidism / Kidney Diseases1
Not AvailableCompletedTreatmentIgA Nephropathy1
Not AvailableCompletedTreatmentPsoriasis1
Not AvailableNot Yet RecruitingTreatmentDevelopment, Child1
Not AvailableTerminatedNot AvailableEnd Stage Renal Disease (ESRD) / End-Stage Renal Disease (ESRD) / Hyperparathyroidism, Secondary1
Not AvailableUnknown StatusNot AvailableNeoplasms, Breast / Postmenopausal Disorder1
Not AvailableUnknown StatusTreatmentProstatic Neoplasms1
Not AvailableWithdrawnTreatmentChronic Kidney Disease (CKD) / Deficiency, Vitamin D1
Not AvailableWithdrawnTreatmentHigh Blood Pressure (Hypertension)1
Not AvailableWithdrawnTreatmentPsoriasis1


  • Roxane laboratories inc
  • Teva pharmaceuticals usa inc
  • Validus pharmaceuticals llc
  • Abbott laboratories hosp products div
  • Akorn inc
  • App pharmaceuticals llc
  • Fresenius medical care north america
  • Genix therapeutics inc
  • Hospira inc
  • Luitpold pharmaceuticals inc
  • Lyne laboratories inc
  • Teva parenteral medicines inc
  • Galderma laboratories lp
  • Abbott Laboratories Ltd.
  • Akorn Inc.
  • American Regent
  • APP Pharmaceuticals
  • Atlantic Biologicals Corporation
  • Cardinal Health
  • Catalent Pharma Solutions
  • DSM Corp.
  • F Hoffmann-La Roche Ltd.
  • Galderma Laboratories
  • Gulf Pharmaceutical Industries
  • Hospira Inc.
  • Kaiser Foundation Hospital
  • Luitpold Pharmaceuticals Inc.
  • Nephrx LLC
  • Pharmaceutical Utilization Management Program VA Inc.
  • Physicians Total Care Inc.
  • Pierre Fabre
  • Ranbaxy Laboratories
  • Resource Optimization and Innovation LLC
  • Roxane Labs
  • Teva Pharmaceutical Industries Ltd.
  • Tya Pharmaceuticals
  • Validus Pharmaceuticals
Dosage forms
SolutionIntravenous1 mcg
SolutionIntravenous2 mcg
CapsuleOral0.25 ug/1
CapsuleOral0.5 ug/1
Capsule, liquid filledOral0.50 ug/1
InjectionIntravenous1 ug/1mL
InjectionIntravenous2 ug/1mL
Injection, solutionIntravenous1 mg/1mL
Injection, solutionIntravenous1 ug/1mL
Injection, solutionIntravenous2 ug/1mL
SolutionIntravenous1 ug/1mL
Capsule, gelatin coatedOral0.25 ug/1
Capsule, gelatin coatedOral0.5 ug/1
Capsule, liquid filledOral0.25 ug/1
Capsule, liquid filledOral0.5 ug/1
SolutionOral1 ug/1mL
OintmentTopical3 ug/1g
Unit descriptionCostUnit
Calcijex 2 mcg/ml19.38USD ml
Calcijex 1 mcg/ml ampul14.7USD ml
Calcijex 1 mcg/ml10.68USD ml
Calcitriol 1 mcg/ml ampul6.0USD ml
Vectical 3 mcg/g ointment4.68USD g
Rocaltrol 0.5 mcg capsule2.02USD capsule
Calcitriol 0.5 mcg capsule1.97USD capsule
Rocaltrol 0.25 mcg capsule1.46USD capsule
Calcitriol 0.25 mcg capsule1.45USD capsule
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patent NumberPediatric ExtensionApprovedExpires (estimated)
Additional Data Available
  • Filed On
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Experimental Properties
melting point (°C)113-114Uskokovic, M.R., Narwid, T.A., lacobelli, J.A. and Baggiolini, E.; U.S. Patent 3,993,675; November 23, 1976; assigned to Hoffmann-La Roche, Inc.
water solubilityInsolubleNot Available
logP5Not Available
Predicted Properties
Water Solubility0.00667 mg/mLALOGPS
pKa (Strongest Acidic)14.39ChemAxon
pKa (Strongest Basic)-1.3ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count3ChemAxon
Polar Surface Area60.69 Å2ChemAxon
Rotatable Bond Count6ChemAxon
Refractivity126.53 m3·mol-1ChemAxon
Polarizability51.02 Å3ChemAxon
Number of Rings3ChemAxon
Rule of FiveYesChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
Human Intestinal Absorption+0.9924
Blood Brain Barrier+0.8524
Caco-2 permeable+0.7812
P-glycoprotein substrateSubstrate0.7843
P-glycoprotein inhibitor INon-inhibitor0.6065
P-glycoprotein inhibitor IINon-inhibitor0.6073
Renal organic cation transporterNon-inhibitor0.8178
CYP450 2C9 substrateNon-substrate0.8367
CYP450 2D6 substrateNon-substrate0.9022
CYP450 3A4 substrateSubstrate0.7506
CYP450 1A2 substrateNon-inhibitor0.9033
CYP450 2C9 inhibitorNon-inhibitor0.8354
CYP450 2D6 inhibitorNon-inhibitor0.9495
CYP450 2C19 inhibitorNon-inhibitor0.7796
CYP450 3A4 inhibitorNon-inhibitor0.813
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.6175
Ames testNon AMES toxic0.9133
BiodegradationNot ready biodegradable0.9937
Rat acute toxicity5.1352 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8734
hERG inhibition (predictor II)Non-inhibitor0.8579
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)


Mass Spec (NIST)
Not Available
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


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.
Organic compounds
Super Class
Lipids and lipid-like molecules
Steroids and steroid derivatives
Sub Class
Vitamin D and derivatives
Direct Parent
Vitamin D and derivatives
Alternative Parents
Triterpenoids / Tertiary alcohols / Secondary alcohols / Cyclic alcohols and derivatives / Hydrocarbon derivatives
Triterpenoid / Tertiary alcohol / Cyclic alcohol / Secondary alcohol / Organic oxygen compound / Hydrocarbon derivative / Organooxygen compound / Alcohol / Aliphatic homopolycyclic compound
Molecular Framework
Aliphatic homopolycyclic compounds
External Descriptors
triol, D3 vitamins, hydroxycalciol (CHEBI:17823) / Steroid hormones (C01673) / Vitamin D3 and derivatives (LMST03020258)


1. Vitamin D3 receptor
Pharmacological action
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
Uniprot ID
Uniprot Name
Vitamin D3 receptor
Molecular Weight
48288.64 Da
  1. Reinhart GA: Vitamin D analogs: novel therapeutic agents for cardiovascular disease? Curr Opin Investig Drugs. 2004 Sep;5(9):947-51. [PubMed:15503649]
  2. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
Pharmacological action
General Function
Sequence-specific transcription factor which is part of a developmental regulatory system that provides cells with specific positional identities on the anterior-posterior axis. Binds to the DNA sequence 5'-AA[AT]TTTTATTAC-3'.
Specific Function
Histone deacetylase binding
Gene Name
Uniprot ID
Uniprot Name
Homeobox protein Hox-A10
Molecular Weight
42413.825 Da
  1. Du H, Daftary GS, Lalwani SI, Taylor HS: Direct regulation of HOXA10 by 1,25-(OH)2D3 in human myelomonocytic cells and human endometrial stromal cells. Mol Endocrinol. 2005 Sep;19(9):2222-33. Epub 2005 May 19. [PubMed:15905361]


Pharmacological action
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...
Gene Name
Uniprot ID
Uniprot Name
1,25-dihydroxyvitamin D(3) 24-hydroxylase, mitochondrial
Molecular Weight
58874.695 Da
  1. Schuster I: Cytochromes P450 are essential players in the vitamin D signaling system. Biochim Biophys Acta. 2011 Jan;1814(1):186-99. doi: 10.1016/j.bbapap.2010.06.022. Epub 2010 Jul 7. [PubMed:20619365]
  2. Bikle DD: Vitamin D metabolism, mechanism of action, and clinical applications. Chem Biol. 2014 Mar 20;21(3):319-29. doi: 10.1016/j.chembiol.2013.12.016. Epub 2014 Feb 13. [PubMed:24529992]
  3. Anderson PH, O'Loughlin PD, May BK, Morris HA: Determinants of circulating 1,25-dihydroxyvitamin D3 levels: the role of renal synthesis and catabolism of vitamin D. J Steroid Biochem Mol Biol. 2004 May;89-90(1-5):111-3. doi: 10.1016/j.jsbmb.2004.03.089. [PubMed:15225756]
  4. Jones G, Prosser DE, Kaufmann M: 25-Hydroxyvitamin D-24-hydroxylase (CYP24A1): its important role in the degradation of vitamin D. Arch Biochem Biophys. 2012 Jul 1;523(1):9-18. doi: 10.1016/ Epub 2011 Nov 12. [PubMed:22100522]
Pharmacological action
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 react...
Gene Name
Uniprot ID
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
  1. Xu Y, Hashizume T, Shuhart MC, Davis CL, Nelson WL, Sakaki T, Kalhorn TF, Watkins PB, Schuetz EG, Thummel KE: Intestinal and hepatic CYP3A4 catalyze hydroxylation of 1alpha,25-dihydroxyvitamin D(3): implications for drug-induced osteomalacia. Mol Pharmacol. 2006 Jan;69(1):56-65. Epub 2005 Oct 5. [PubMed:16207822]


Pharmacological action
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
Uniprot ID
Uniprot Name
Vitamin D-binding protein
Molecular Weight
52963.025 Da
  1. Davey RX: Vitamin D-binding protein as it is understood in 2016: is it a critical key with which to help to solve the calcitriol conundrum? Ann Clin Biochem. 2017 Mar;54(2):199-208. doi: 10.1177/0004563216677100. Epub 2016 Dec 11. [PubMed:27742848]
  2. Arnaud J, Constans J: Affinity differences for vitamin D metabolites associated with the genetic isoforms of the human serum carrier protein (DBP). Hum Genet. 1993 Sep;92(2):183-8. [PubMed:8370586]

Drug created on June 13, 2005 07:24 / Updated on June 04, 2020 15:41

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