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Calcitriol
drug data and news
Calcitriol drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.
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| Generic name | Calcitriol | ||
| Brand Names/Synonyms | Calcijex; Calcitriol; Rocaltrol | ||
| 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. | ||
| Sponsored links | Description | Not Available | |
| Pharmacology | Calcitriol, a pharmaceutical form of vitamin D, has anti-osteoporotic, immunomodulatory, anticarcinogenic, antipsoriatic, antioxidant, and mood-modulatory activities. Calcitriol has been found to be effective in the treatment of psoriasis when applied topically. Calcitriol has been found to induce differentiation and/or inhibit cell proliferation in a number of malignant cell lines including human prostate cancer cells. Vitamin D deficiency has long been suspected to increase the susceptibility to tuberculosis. The active form of Calcitriol, 1,25 (OH)2 D, has been found to enhance the ability of mononuclear phagocytes to suppress the intracellular growth of Mycobacterium tuberculosis. 1,25(OH)2D has demonstrated beneficial effects in animal models of such autoimmune diseases as rheumatoid arthritis. It 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. 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)2D 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)2D 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. | ||
| Calcitriol News (When available) |
ASCO Prostate: Intermittent Chemotherapy Controls Androgen ... Feb 28, 2006 Treatment “Holidays� Effective in Hormone-Refractory Prostate ... Mar 1, 2006 Calcium Benefits for Better Health Feb 20, 2006 Local Anesthesia Rivaling General for Thyroid Surgery Feb 20, 2006 Teva and Ivax Cleared to Complete Merger Jan 27, 2006 FTC gives Ivax and Teva final go-ahead for merger Jan 23, 2006 Sapphire Therapeutics, Inc. Appoints New Director and Scientific ... Jan 17, 2006 Preserving Competition, FTC Requires Divestitures Before Allowing ... Jan 23, 2006 Sapphire Therapeutics, Inc. Builds Drug Development Team Through ... Jan 9, 2006 Calcitriol and QW-1624-F2-2 are promising for prevention of ... Nov 20, 2005 Vitamin D May Help Treat Some Asthma Dec 8, 2005 FAMILY DOCTOR: LIchen sclerosis affects sexual function Dec 9, 2005 Vitamin D plus taxotere extends lives of men with advanced ... Nov 7, 2005 Vitamin D sufficiency may be more important than high calcium ... Nov 10, 2005 Long-Term Exposure to Warfarin Associated with Aortic Valve ... Nov 11, 2005 Calcitriol Can Be Safely Added to Chemotherapy for Prostate Cancer Sep 23, 2005 The Washington Legal Foundation (WLF) today called on DDMAC to ... Oct 4, 2005 Tumor-Induced Osteomalacia Sep 13, 2005 Rejuvenon Corp. Changes Name to Sapphire Therapeutics, Inc. ... Oct 5, 2005 Calcitriol [Vitamin D] with combination of painkillers for cancer ... Sep 7, 2005 Calcitriol and NSAIDs Together Block Rrostate Cancer Cell Growth Sep 2, 2005 Prostate Cancer Growth Slowed Dramatically by Vitamin D with Pain ... Sep 1, 2005 Vitamin D, NSAIDS Provide Double Whammy Against Prostate Cancer ... Sep 1, 2005 Activated vitamin D and NSAIDs form one-two punch against prostate ... Aug 31, 2005 Vitamin D boosts NSAID cancer-fighting power Sep 2, 2005 Vitamin D, NSAIDS Provide Double Whammy Against Prostate Cancer Sep 1, 2005 Vitamin D Can Halt Growth Of Cancer Cells Sep 5, 2005 Double whammy of vitamin D and anti-inflammatory zaps prostrate ... Sep 6, 2005 Vitamin D and Painkiller Slow Prostate Cancer Sep 1, 2005 Vitamin D, painkillers battle prostate cancer Sep 1, 2005 Vitamin D, painkillers battle prostate cancer: Sep 2, 2005 Vitamin D-NSAID Duo Shows Promise Against Prostate Cancer Sep 1, 2005 Vitamin D-NSAID Duo Shows Promise Against Prostate Cancer Sep 4, 2005 Drugs 'may combat prostate cancer' Sep 1, 2005 Vitamin D and NSAIDs Slow Prostate Cancer Aug 31, 2005 Little Miss Muffet's whey found to aid weight loss Aug 3, 2005 Rejuvenon's RC-8800 for Prostate Cancer Enters Human Testing; RC ... Jul 20, 2005 Vitamin D, Taxotere Combination Promising For Advanced Prostate ... Jul 12, 2005 Diet experts tackle 12 weight-loss questions Jul 25, 2005 Elderly benefit from calcium and vitamin D combo, confirms review Jul 21, 2005 ON NUTRITION: HELAYNE WALDMAN Vitamin D plays crucial role in well ... Jul 12, 2005 Vitamin D: The New Wonder Vitamin Jul 1, 2005 A Long-Term, Open-Label Extension Study on the Safety of Treatment ... Jun 11, 2005 | ||
| Dosage Forms | Capsule, solution | ||
| Drug_Category | ATC:A11CC04; ATC:D05AX03; Antihypocalcemic Agents; Antihypoparathyroid Agents; Essential Vitamin; Vitamins (Vitamin D) | ||
| Absorption | Rapidly absorbed from the intestine. | ||
| Interactions | [an error occurred while processing this directive]Toxicity | LD50 (oral, rat) = 620 μg/kg; LD50 (intraperitoneal, rat) > 5 mg/kg; Overdose evident in elevated blood calcium levels causing symptoms of anorexia, nausea and vomiting, polyuria, polydipsia, weakness, pruritus, and nervousness, potentially with irreversible calcification of soft tissue in the kidney and liver. | |
| Organisms Affected | Humans and other mammals | ||
| Chemical IUPAC Name | 5-[2-[1-(6-hydroxy-6-methyl-heptan-2-yl)-7a-methyl-2,3,3a,5,6,7-hexahydro-1H-inden-4-ylidene]ethylidene]-4-methylidene-cyclohexane-1,3-diol | ||
| Chemical Formula | C27H44O3 | ||
| Molecular Weight | 416.636 g/mol | ||
| Smiles String | CC(CCCC(C)(C)O)C1CCC2C1(CCCC2=CC=C3CC(CC(C3=C)O)O)C | ||
| Melting Point | 113 °C | ||
| Water Solubility | Insoluble | ||
| State | Solid | ||
| LogP/Hphobicity | 4.96 | ||
| Isoelectric Point | Not Available | ||
| Biotransformation | 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. The lactone appears to be the major metabolite circulating in humans. | ||
| Half Life | 5-8 hours | ||
| Protein Binding [%] | 99.90% | ||
| RxList Link | RXlist | ||
| Sponsored links | |||
| Drug Reference |
http://www.drugs.com/cons/Calcitriol.html http://www.pharmgkb.org/views/index.jsp?objId= | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00246 | ||
| CAS Registry Number | 32222-06-3 | ||
| KEGG Compound ID | C01673 | ||
| PubChem ID | SID:4817 | ||
| PharmGKB ID | PA448717 | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | 2245686 |
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