Calcipotriol
| File:Calcipotriol.svg | |
| Clinical data | |
|---|---|
| Pregnancy category | |
| Routes of administration | Topical |
| ATC code | |
| Legal status | |
| Legal status | |
| Pharmacokinetic data | |
| Bioavailability | 5 to 6% |
| Metabolism | Hepatic |
| Excretion | Biliary |
| Identifiers | |
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| CAS Number | |
| PubChem CID | |
| E number | {{#property:P628}} |
| ECHA InfoCard | {{#property:P2566}}Lua error in Module:EditAtWikidata at line 36: attempt to index field 'wikibase' (a nil value). |
| Chemical and physical data | |
| Formula | C27H40O3 |
| Molar mass | 412.605 g/mol |
Calcipotriol (INN) or calcipotriene (USAN) is a synthetic derivative of calcitriol or Vitamin D. It is used in the treatment of psoriasis, marketed under the trade name Dovonex®.
Mechanism
The efficacy of calcipotriol in the treatment of psoriasis was first noticed by the observation of patients receiving various forms of Vitamin D in an osteoporosis study. Unexpectedly, a patient's psoriasis lesions dramatically disappeared. [1]
The precise mechanism of calcipotriol in remitting psoriasis is not well-understood. However, it has been shown to have comparable affinity with calcitriol (Vit D) for the Vitamin D receptor, while being less than 1% as active as the calcitriol in regulating calcium metabolism. The Vitamin D receptor (VDR) belongs to the steroid/thyroid receptor superfamily, and is found on the cells of many different tissues including the thyroid, bone, kindney, and T cells of the immune system. T cells are known to play a role in psoriasis, and it is thought that the binding of calcipotriol to the VDR modulates the T cells gene transcription of cell differentiation and proliferation related genes.
Usage and Efficacy
Available as a cream, ointment or scalp solution (50mcg/mL), Calcipotriol is applied twice daily to plaque psoriasis on the body or scalp, but not the face. Improvement is usually detectable within 2 weeks. Most patients show some improvement, slightly more so than is seen with the use of corticosteroids alone. Tachyphylaxis does not occur, an improvement over glucocorticoid therapy.[2]
Side effects
Calcipotriol has been shown in clinical trials to have an excellent safety profile. [3] Reports of hypercalcemia are rare.[4]
It is also available in combination with the synthetic glucocorticoid betamethasone under the trade name Dovobet®.
References
- ↑ Morimoto, S., Kumahara, Y. A patient with psoriasis cured by 1-α-hydroxyvitamin D3. Med. J. Osaka Univ., 1985, 35:51-54
- ↑ Kragbelle, K. Treatment of psoriasis with calcipotriol and other Vitamin D analogues. J. Am. Acad. Dermatol., 1992, 27:1001-1008.
- ↑ Brunton, Laurence. Goodman and Gilman's The Pharmacological Basis of Therapeutics, 11th ed. McCraw-Hill, 2006. p. 1664. p. 1704-5.
- ↑ Hardman et al. Hypercalcemia associated with calcipotriol (DOVONEX) treatment. Br Med J., 1993, 306:896.
External links
- Leo Pharmaceuticals Product Monograph- Detailed information from the manufacturers, includes the blood testing recommendation (.pdf document).
- Calcipotriene information - U.S. NLM/NIH
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- ECHA InfoCard ID from Wikidata
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- Dermatological preparations