Calcitriol
Vitamin D3 Analog — ALIMENTARY TRACT AND METABOLISM
Also known as: 1,25-dihydroxyvitamin D3, Dihydroxyvitamin D3, rocaltrol, topitriol
Data last refreshed: (DrugCentral release 2024-11-01)
Key facts
Calcitriol is an ofp drug in the Vitamin D3 Analog class catalogued in DrugCentral. It was first approved by the FDA in 1978. DrugCentral lists 10 molecular targets, including VDR, Vdr and VDR. Recorded indications include Hyperparathyroidism Secondary to Chronic Renal Failure, Hypocalcemia, Hypocalcemia from End-Stage Renal Disease with Dialysis and Hypoparathyroidism.
- Approval status: ofp (first approved 1978 by the FDA).
- Drug class: Vitamin D3 Analog.
- Molecular targets: VDR, Vdr, VDR and VDR (10 listed in DrugCentral).
- Indications: Hyperparathyroidism Secondary to Chronic Renal Failure, Hypocalcemia, Hypocalcemia from End-Stage Renal Disease with Dialysis, Hypoparathyroidism and Hypophosphatemia and others.
- ATC code: A11CC04 (Vitamin D and analogues).
- Molecular formula: C27H44O3; molecular weight 416.65 g/mol.
Indications & contraindications
Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).
Indications (7)
- Hyperparathyroidism Secondary to Chronic Renal Failure
- Hypocalcemia
- Hypocalcemia from End-Stage Renal Disease with Dialysis
- Hypoparathyroidism
- Hypophosphatemia
- Plaque psoriasis
- Renal osteodystrophy
Off-label uses (5)
- Familial x-linked hypophosphatemic vitamin D refractory rickets
- Neonatal hypocalcemic tetany
- Rickets
- Vitamin D deficiency
- Vitamin D Dependent Rickets
Contraindications (8)
- Arteriosclerosis obliterans
- Hypercalcemia
- Hypercalcemia associated with Sarcoidosis
- Hyperphosphatemia
- Hypervitaminosis D
- Kidney disease
- Kidney stone
- Sarcoidosis
Mechanism & targets
| Established pharmacologic class | Vitamin D3 Analog |
|---|
Molecular targets (10)
| Target | Gene | Action | Activity |
|---|---|---|---|
| Vitamin D3 receptor | VDR | unknown | Ki 10.60 |
| Vitamin D3 receptor | Vdr | unknown | Ki 10.30 |
| Vitamin D3 receptor | VDR | unknown | EC50 10.30 |
| Vitamin D3 receptor | VDR | unknown | Kd 10.15 |
| Vitamin D3 receptor | VDR | agonist | EC50 8.40 |
| Vitamin D3 receptor A | vdra | unknown | EC50 8.26 |
| Vitamin D-binding protein | GC | unknown | Kd 7.62 |
| Vitamin D3 receptor | Vdr | unknown | EC50 7.00 |
| 25-hydroxyvitamin D-1 alpha hydroxylase, mitochondrial | CYP27B1 | unknown | — |
| Vitamin D 25-hydroxylase | CYP2R1 | unknown | — |
Regulatory approvals (1)
| Date | Agency | Marketed as | Applicant | Orphan |
|---|---|---|---|---|
| 1978-08-17 | FDA | — | VALIDUS PHARMS |
ATC classification
| ATC code | Therapeutic hierarchy |
|---|---|
A11CC04 | ALIMENTARY TRACT AND METABOLISM › VITAMINS › VITAMIN A AND D, INCL. COMBINATIONS OF THE TWO › Vitamin D and analogues |
D05AX03 | DERMATOLOGICALS › ANTIPSORIATICS › ANTIPSORIATICS FOR TOPICAL USE › Other antipsoriatics for topical use |
Reported adverse-event signals
Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.
| MedDRA term | LLR |
|---|---|
| Recalled product | 1333.7 |
| Hypercalcaemia | 836.0 |
| Hypocalcaemia | 784.6 |
| Appendicolith | 631.5 |
| Appendicitis | 494.8 |
| Blood phosphorus increased | 490.8 |
| Milk-alkali syndrome | 464.4 |
| Peritonitis bacterial | 394.7 |
| Hyperphosphataemia | 371.6 |
| Cardiogenic shock | 361.1 |
| Drug hypersensitivity | 355.1 |
| Calciphylaxis | 295.4 |
Chemical structure
Full physicochemical, ADMET and 3D-structure analysis of Calcitriol is on its molecule page.
| Molecular formula | C27H44O3 |
|---|---|
| Molecular weight | 416.65 g/mol |
| CAS number | 32222-06-3 |
| InChIKey | GMRQFYUYWCNGIN-NKMMMXOESA-N |
| PubChem CID | 5280453 |
Frequently asked questions
Answers are generated from the structured data on this page, not written by hand.
What is Calcitriol used for?
DrugCentral lists the following indications for Calcitriol: Hyperparathyroidism Secondary to Chronic Renal Failure, Hypocalcemia, Hypocalcemia from End-Stage Renal Disease with Dialysis, Hypoparathyroidism, Hypophosphatemia, Plaque psoriasis and Renal osteodystrophy.
How does Calcitriol work?
Its molecular targets in DrugCentral include VDR, Vdr, VDR and VDR.
When was Calcitriol first approved?
Calcitriol was first approved by the FDA in 1978.
What drug class does Calcitriol belong to?
Calcitriol is in the Vitamin D3 Analog class.
What is the chemical formula of Calcitriol?
Calcitriol has the molecular formula C27H44O3 and a molecular weight of 416.65 g/mol.
Browse: all drugs starting with C · drug guides by category · protein targets A–Z.
Sources
- DrugCentral drug card 466 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
- ChEMBL CHEMBL846 — compound record and bioactivity
- PubChem CID 5280453 — chemical identifiers
- DrugBank DB00136 — drug record
- FDA UNII FXC9231JVH — substance identity
- DailyMed: FDA labels for Calcitriol — current prescribing information (label search)
- UniProt P11473 (VDR) — target protein
- UniProt P02774 (GC) — target protein
- UniProt O15528 (CYP27B1) — target protein
- UniProt Q6VVX0 (CYP2R1) — target protein
- FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral
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