MedPath

Calcitriol

Generic Name
Calcitriol
Brand Names
Rocaltrol, Vectical
Drug Type
Small Molecule
Chemical Formula
C27H44O3
CAS Number
32222-06-3
Unique Ingredient Identifier
FXC9231JVH
Background

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 D, 1,25-dihydroxyvitamin D. 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 . Calcitriol is considered to be the most potent metabolite of vitamin D in humans . Renal production of calcitriol is stimulated in response to PTH, low calcium and low phosphate . 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 . There is also evidence that calcitriol modulates the action of cytokines and may regulate immune and inflammatory response, cell turnover, cell differentiation .

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).

Indication

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
Hypocalcemia, Mild to Moderate Plaque Psoriasis, Osteodystrophy, Secondary Hyperparathyroidism (SHPT), Vitamin D Resistant Rickets

Calcitriol in Advanced Intrahepatic Cholangiocarcinoma

Phase 2
Conditions
Advanced Intrahepatic Cholangiocarcinoma
First Posted Date
2009-12-24
Last Posted Date
2009-12-24
Lead Sponsor
National Science and Technology Development Agency, Thailand
Target Recruit Count
28
Registration Number
NCT01039181
Locations
🇹🇭

Srinagarind Hospital, Faculty of Medicine, Khon Kaen University, Khon Kaen, Thailand

hCAP18 Levels and Vitamin D Deficiency in Chronic Kidney Disease

Not Applicable
Withdrawn
Conditions
Chronic Kidney Disease
Vitamin D Deficiency
Interventions
First Posted Date
2009-12-04
Last Posted Date
2015-09-23
Lead Sponsor
Massachusetts General Hospital
Registration Number
NCT01026363
Locations
🇺🇸

Massachusetts Institute of Technology, Cambridge, Massachusetts, United States

Safety and Efficacy Study of Combination Treatment With Excimer Laser, Clobex Spray, and Vectical Ointment in the Treatment of Psoriasis

Phase 4
Completed
Conditions
Chronic Stable Plaque Psoriasis
Interventions
First Posted Date
2009-11-13
Last Posted Date
2015-06-18
Lead Sponsor
University of California, San Francisco
Target Recruit Count
30
Registration Number
NCT01012713
Locations
🇺🇸

UCSF Psoriasis and Skin Treatment Center, San Francisco, California, United States

Study of Vitamin D Supplementation to Male HIV Sero-positive Patients

Not Applicable
Completed
Conditions
HIV Seropositive
Interventions
First Posted Date
2009-10-07
Last Posted Date
2012-09-17
Lead Sponsor
Hvidovre University Hospital
Target Recruit Count
60
Registration Number
NCT00990678
Locations
🇩🇰

Dept. of endocrinology, Hvidovre Hospital, Copenhagen, Denmark

Vitamin D Plus Celecoxib Therapy to Stimulate Intratumoral Immune Reactivity

Phase 1
Completed
Conditions
Mouth Neoplasms
Interventions
First Posted Date
2009-08-06
Last Posted Date
2017-03-07
Lead Sponsor
VA Office of Research and Development
Target Recruit Count
21
Registration Number
NCT00953849
Locations
🇺🇸

Ralph H. Johnson VA Medical Center, Charleston, SC, Charleston, South Carolina, United States

Gene Expression Profile of Breast Cancer Samples After Vitamin D Supplementation

Not Applicable
Conditions
Breast Neoplasms
Postmenopausal Disorder
Interventions
First Posted Date
2009-06-23
Last Posted Date
2012-11-01
Lead Sponsor
University of Sao Paulo General Hospital
Target Recruit Count
60
Registration Number
NCT00926315
Locations
🇧🇷

Instituto Brasileiro de Controle do Câncer - IBCC, São Paulo, SP, Brazil

The Pharmacokinetics of Rocaltrol When Administered Alone or in Combination With Fosrenol or Renvela in Healthy Volunteers

Phase 1
Completed
Conditions
Healthy
Interventions
Drug: Lanthanum carbonate + Calcitriol
First Posted Date
2009-06-22
Last Posted Date
2021-06-15
Lead Sponsor
Shire
Target Recruit Count
41
Registration Number
NCT00925704
Locations
🇺🇸

West Coast Clinical Trials, Cypress, California, United States

Calcitriol, Physical Activity, and Bone Health in Cancer Survivors

Phase 2
Completed
Conditions
Breast Neoplasms
Bone and Bones
Interventions
Dietary Supplement: Multivitamin
Behavioral: Exercise
First Posted Date
2009-05-19
Last Posted Date
2019-04-23
Lead Sponsor
University of Rochester
Target Recruit Count
41
Registration Number
NCT00904033
Locations
🇺🇸

University of Rochester Medical Center, Rochester, New York, United States

Calcitriol in the Treatment of Immunoglobulin A Nephropathy

Phase 4
Conditions
Glomerulonephritis
Autoimmune Diseases
Interventions
First Posted Date
2009-03-17
Last Posted Date
2011-02-17
Lead Sponsor
Peking University First Hospital
Target Recruit Count
40
Registration Number
NCT00862693
Locations
🇨🇳

Renal Division, Peking University First Hospital, Beijing, Beijing, China

Paricalcitol Versus Calcitriol for Efficacy and Safety in Stage 3/4 Chronic Kidney Disease (CKD) With Secondary Hyperparathyroidism (SHPT)

Phase 4
Completed
Conditions
Chronic Kidney Disease
Secondary Hyperparathyroidism
Interventions
First Posted Date
2009-01-15
Last Posted Date
2014-08-07
Lead Sponsor
Washington University School of Medicine
Target Recruit Count
110
Registration Number
NCT00823303
Locations
🇺🇸

Northwestern University, Chicago, Illinois, United States

🇺🇸

Northshore University Health System, Evanston, Illinois, United States

🇺🇸

Washington University, St. Louis, Missouri, United States

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