High Purity EP Standard Calcipotriol CAS 112965-21-6/112828-00-9 Calcipotriene Raw Material Powder

Calcipotriol More Info

Calcipotriol, also known as calcipotriene, is a synthetic derivative of calcitriol, a form of vitamin D, used in adult patients with unusual psoriasis and is the first line of topical treatment for psoriasis.

Mechanism of Action

Calcipotriol functions by binding to the vitamin D receptor (VDR), modulating gene transcription related to cell differentiation and proliferation. It has a comparable affinity for the VDR as calcitriol but exhibits less than 1% of calcitriol's activity in regulating calcium metabolism. This mechanism helps reduce keratinocyte proliferation and promotes their differentiation, which is crucial in managing conditions like psoriasis

Immunomodulatory Effects

The drug also demonstrates immunomodulatory properties by decreasing inflammatory cytokines such as interleukin-1 (IL-1) and IL-6, while increasing transforming growth factor-β (TGF-β) levels, which inhibit epithelial cell growth. This dual action helps mitigate the inflammatory processes associated with psoriasis

Applications

Calcipotriol is primarily indicated for:
1. Chronic Plaque Psoriasis: It is effective in treating moderate plaque psoriasis in adults and children.
2. Other Skin Conditions: It has shown efficacy in conditions like alopecia areata and certain keratinization disorders

Routes of Administration

Calcipotriol is available in several formulations:
1. Ointment: Commonly used for plaque psoriasis on trunk and limbs.
2. Cream: Suitable for use in body folds or on sensitive areas like the face.
3. Scalp Solution: Designed for application on hairy areas.
The standard application regimen involves twice-daily use, although combinations with other treatments may be employed

Safety and Side Effects

Calcipotriol is generally well-tolerated. Common side effects include:
1. Local Skin Reactions: Approximately 20% of patients may experience irritation at the application site.
2. Photosensitization: Increased sensitivity to sunlight can occur, particularly when used alongside UVB phototherapy.
3. Rare Reactions: Contact dermatitis is infrequent, but caution is advised due to potential systemic absorption leading to elevated serum calcium levels if used excessively

Contraindications

Contraindications include:
1. Hypercalcemia
2. Pregnancy and nursing
3. Known hypersensitivity to calcipotriol or its components

Pharmacokinetics

After topical application, calcipotriol undergoes rapid hepatic metabolism. The primary metabolites are less potent than the parent compound. Systemic absorption from topical formulations is relatively low, with studies indicating about 6% absorption when applied to psoriatic plaques

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