calcifediol
Small moleculeapproved
Approved
Aug 5, 1980
Calcifediol (25-Hydroxyvitamin D3 or 25-hydroxycholecalciferol) is a biologically active vitamin D3 metabolite. It is concluded that the liver is the major if not the only physiologic site of hydroxylation of vitamin D3 into calcifediol. Calcifediol is a prohormone of the active form of vitamin D3, calcitriol (1,25-dihydroxyvitamin D3). Calcifediol is converted to calcitriol by cytochrome P450 27B1 (CYP27B1), also called 1-alpha hydroxylase, primarily in the kidney. Calcitriol binds to the vitamin D receptor in target tissues and activates vitamin D responsive pathways that result in increased intestinal absorption of calcium and phosphorus and reduced parathyroid hormone synthesis. RAYALDEE (calcifediol) extended-release capsules is indicated for the treatment of secondary hyperparathyroidism in adult patients with stage 3 or 4 chronic kidney disease. — NCATS
Clinical trial activity
28 trials · 51 clinical orgs · 2 marketing orgs
Phase 1
5
Phase 2
11
Phase 3
5
Phase 4
8
Earliest trial started Oct 1, 1999 (NCT00018538)
Timeline
1990s
- Jan 1, 1999
Earliest Phase 2 Sponsor(trial)
Indications
Approved for
Studied for
- Accidental Falls · Phase 2
- Acute Kidney Injury · Phase 2
- Asthma · Phase 4
- Cardiovascular Diseases · Phase 4
- Chronic Kidney Disease-Mineral and Bone Disorder · Phase 4
- Coronavirus · Phase 2
- COVID-19 · Phase 2
- Critical Illness · Phase 2
- Cytokine Release Syndrome · Phase 2
- Diabetes Mellitus, Type 2 · Phase 3
- Frail Elderly · Phase 1
- Healthy Volunteers · Phase 1
- Hip Fractures · Phase 4
- Hyperparathyroidism · Phase 4
- Hyperparathyroidism, Secondary · Phase 4
- Hypertension, Pulmonary · Phase 4
- Kidney Failure, Chronic · Phase 4
- Malabsorption Syndromes · Early Phase 1
- Myocardial Infarction · Phase 3
- Osteomalacia · Phase 4
- Osteoporosis · Phase 3
- Prostatic Neoplasms · Phase 2
- Severe Acute Respiratory Syndrome · Phase 2
- Sleep Apnea, Obstructive · Phase 2
- Vitamin D Deficiency · Phase 4
Mechanism of action
- Vitamin D receptorAGONIST
VDR agonist
Approval history
- approvedAug 5, 1980
Chemistry & pharmacology
Loading structure…
SMILES
C=C1CC[C@H](O)C/C1=C/C=C1\CCC[C@]2(C)[C@@H]([C@H](C)CCCC(C)(C)O)CC[C@@H]12- Mol. weight
- 400.65 g/mol
- Lipinski Ro5
- 1 violation(s)
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral
- Availability
- Prescription Only
Oral
Yes
Parenteral
No
Topical
No
Sources
- ChEMBLCHEMBL1040 ↗
- WikipediaCalcifediol ↗
- NCATST0WXW8F54E ↗
- ChEMBLCHEMBL3544909 ↗
Also known as
- 25-hydroxycholecalciferol
- 25-hydroxycholecalciferol
- 25-hydroxycholecalciferol
- 25-hydroxy vitamin d
- 25-hydroxy vitamin d
- 25-hydroxy vitamin d3
- 25-hydroxy vitamin d3
- 25-hydroxyvitamin d3
- 25-hydroxyvitamin d3
- (3s,5z,7e)-9,10-secocholesta-5,7,10-triene-3,25-diol
- (3s,5z,7e)-9,10-secocholesta-5,7,10-triene-3,25-diol
- (3β,5z,7e)-9,10-secocholesta-5,7,10(19)-triene-3,25-diol
- (3β,5z,7e)-9,10-secocholesta-5,7,10(19)-triene-3,25-diol
- (5z,7e)-(3s)-9,10-secocholesta-5,7,10(19)-triene-3,25-diol
- (5z,7e)-(3s)-9,10-secocholesta-5,7,10(19)-triene-3,25-diol
- calcidiol
- calcidiol
- calcidiol
- calcidiol
- calcidiol
- calcifediol
- calcifediol
- calcifediol
- calcifediol
- calcifediol
- calcifediol
- calcifediol
- calcifediol
- calcifediol
- calcifediol
- calcifediol
- calcifédiol
- calcifédiol
- calcifediol anhydrous
- calcifediol anhydrous
- calcifediolum
- calcifediolum
- calcifidiol
- calderol
- calderol
- calderol
- calderol
- u-32070e
- u-32070e
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT06258850 | Phase 4 | Jul 1, 2024 | Hospital Universitario Ramon y Cajal, Institut Hospital del Mar d'Investigacions Mèdiques, Universidad Autonoma de Barcelona, Universidad Complutense de Madrid, University of Barcelona, University of Cantabria, University of Seville, University of Valencia |
| NCT05502068 | N/A | Feb 1, 2021 | Pauls Stradins Clinical University Hospital |
| NCT04735926 | Phase 2/Phase 3 (Phase 3) | Dec 23, 2020 | Faes Farma, S.A. |
| NCT04551911 | Phase 2 | Oct 26, 2020 | Opko |
| NCT04366908 | Phase 2 | Apr 28, 2020 | Dynamic Solutions, Faes Farma, S.A., Hospital Universitario Reina Sofía, Junta de Andalucía, Universidad de Cordoba |
| NCT03401541 | Early Phase 1 (Phase 1) | Sep 30, 2018 | Boston University |
| NCT03660800 | Phase 1 | Aug 20, 2018 | Opko, WCCT Global |
| NCT03588884 | Phase 4 | Jun 8, 2018 | Opko |
| NCT03213886 | Phase 4 | Jan 1, 2018 | Consorci Sanitari de Terrassa, Fundacio Salut i Envelliment UAB |
| NCT02962102 | Phase 2 | Apr 3, 2017 | Brigham and Women's Hospital, Harvard University, National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK) |
| NCT03403933 | Phase 4 | Jan 16, 2017 | University of Milan |
| NCT02805907 | Phase 4 | Jun 1, 2016 | MurciaSalud |
| NCT02548364 | Phase 3 | Oct 1, 2015 | Fondo de Investigacion Sanitaria, Spanish Society of Cardiology, Universidad Autonoma de Madrid |
| NCT02527668 | Phase 2 | Sep 1, 2015 | DSM, Tufts University, University of Zurich |
| NCT02349282 | N/A | Dec 1, 2014 | DSM, Top Institute Food and Nutrition, Wageningen University |
| NCT02091219 | Early Phase 1 (Phase 1) | Jun 1, 2014 | National Institute of Arthritis and Musculoskeletal and Skin Diseases (NIAMS), University of California, Los Angeles |
| NCT01939977 | Phase 4 | Jan 1, 2014 | AbbVie, Effice Servicios Para la Investigacion S.L., Fundación Senefro, University of Barcelona |
| NCT02802449 | N/A | Sep 1, 2013 | Charles Drew University, Morehouse University, National Institutes of Health (NIH) |
| NCT01868945 | Phase 1 | Apr 1, 2013 | DSM, Maastricht University, Wageningen University |
| NCT01457001 | Phase 3 | Nov 1, 2012 | Italian Society of Nephrology |
Showing 20 of 28 trials
Page 1 / 2
Organizations
Research & Development (51)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| DSM | For profit | 3 | 2 | 3 | 2013 |
| Opko | For profit | 3 | 3 | 3 | 2018 |
| University of Zurich | Academic/Hospital | 3 | 2 | 2 | 2008 |
| Faes Farma, S.A. | For profit | 2 | 1 | 2 | 2020 |
| University of Barcelona | Academic/Hospital | 2 | 0 | 1 | 2014 |
| Wageningen University | Academic/Hospital | 2 | 1 | 2 | 2013 |
| AbbVie | For profit | 1 | 0 | 1 | 2014 |
| Boston University | Academic/Hospital | 1 | 1 | 1 | 2018 |
| Brigham and Women's Hospital | Academic/Hospital | 1 | 1 | 1 | 2017 |
| Centre de Recherche en Nutrition Humaine Rhone-Alpe | Academic/Hospital | 1 | 0 | 1 | 2011 |
| Charles Drew University | Academic/Hospital | 1 | 1 | 1 | 2013 |
| Consorci Sanitari de Terrassa | Academic/Hospital | 1 | 1 | 1 | 2018 |
| Department of Veteran Affairs | Government | 1 | 1 | 1 | 1999 |
| Dynamic Solutions | For profit | 1 | 0 | 1 | 2020 |
| Effice Servicios Para la Investigacion S.L. | For profit | 1 | 0 | 1 | 2014 |
| Fondo de Investigacion Sanitaria | Academic/Hospital | 1 | 0 | 1 | 2015 |
| Fundación Senefro | Academic/Hospital | 1 | 1 | 1 | 2014 |
| Fundacio Salut i Envelliment UAB | Academic/Hospital | 1 | 0 | 1 | 2018 |
| Harvard University | Academic/Hospital | 1 | 0 | 1 | 2017 |
| Hospital Universitario Ramon y Cajal | Academic/Hospital | 1 | 0 | 1 | 2024 |
51 organizations
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