Name: | calcipotriene |
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PubChem Compound ID: | 2522 |
Molecular formula: | C27H40O3 |
Molecular weight: | 412.605 g/mol |
Name: | calcipotriene |
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Name (isomeric): | DB02300 |
Drug Type: | small molecule |
Synonyms: |
Calcipotriene
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Brand: | Davonex, Dovonex |
Category: | Antipsoriatic Agents, Vitamin D3 Receptor inhibitor, Dermatologic Agents |
CAS number: | 112965-21-6 |
Indication: | For the treatment of moderate plaque psoriasis in adults. |
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Pharmacology: | Calcipotriene is a synthetic analog of vitamin D. In humans, the natural supply of vitamin D depends mainly on exposure to the ultraviolet rays of the sun for conversion of 7-dehydrocholesterol to vitamin D3 (cholecalciferol) in the skin. |
Mechanism of Action: |
The precise mechanism of calcipotriol in remitting psoriasis is not well-understood. However, it has been shown to have comparable affinity with calcitriol 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 superfamil...
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Absorption: | Clinical studies with radiolabeled ointment indicate that approximately 6% (+3%, SD) of the applied dose of calcipotriene is absorbed systemically when the ointment is applied topically to psoriasis plaques or 5% (+2.6%, SO) when applied to normal skin. |
Biotransformation: | Hepatic. Calcipotriene metabolism following systemic uptake is rapid, and occurs via a similar pathway to the natural hormone. The primary metabolites are much less potent than the parent compound. |
Route of elimination: | The active form of the vitamin, 1,25-dihydroxy vitamin D3 (calcitriol), is known to be recycled via the liver and excreted in the bile. There is evidence that maternal 1,25-dihydroxy vitamin D3 (calcitriol) may enter the fetal circulation, but it is not known whether it is excreted in human milk. |
Toxicity: | Topically applied calcipotriene can be absorbed in sufficient amounts to produce systemic effects. Elevated serum calcium has been observed with excessive use of calcipotriene. |
Affected organisms: | Humans and other mammals |
Drug interaction: |
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