What is calcipotriene?

Calcipotriene: A Vitamin D Analog for Psoriasis Treatment

Calcipotriene is a synthetic vitamin D3 analog that works by binding to vitamin D receptors to inhibit keratinocyte proliferation and enhance keratinocyte differentiation, effectively normalizing the hyperproliferative state of psoriatic skin. 1, 2

Mechanism of Action

• Calcipotriene (also known as calcipotriol) is a synthetic analog of vitamin D3 that inhibits epidermal cell proliferation and promotes keratinocyte differentiation in psoriatic plaques 2, 3
• It works by binding to vitamin D receptors, which helps normalize the accelerated cell turnover seen in psoriasis 1, 2
• After topical application, approximately 6% (±3%) of the applied dose is absorbed systemically when applied to psoriasis plaques, with much of the absorbed active ingredient converted to inactive metabolites within 24 hours 3

Formulations and Administration

• Available in several formulations including ointment, cream, solution, foam, and in combination with betamethasone dipropionate 4, 5
• The chemical composition includes calcipotriene 50 mcg/g in various bases depending on the formulation 3
• For adults, the maximum recommended dosage is 100g/week to prevent hypercalcemia 6
• For pediatric patients, dosing should be limited to 50g/week/m² to prevent hypercalcemia 6

Clinical Efficacy

• Calcipotriene has demonstrated significant efficacy in treating psoriasis, with 65-70% of patients experiencing marked improvement or clearing 2
• The full therapeutic effect typically takes up to 8 weeks to develop, with limited efficacy observed at 4 weeks 1, 6
• In clinical trials, calcipotriene foam showed significantly better results than vehicle foam for the treatment of mild to moderate plaque-type psoriasis after 8 weeks 4
• For scalp psoriasis, calcipotriene foam was more effective than vehicle in achieving clear or almost clear status (40.9% vs 24.2%) after 8 weeks 1

Combination Therapy

• Combination with betamethasone dipropionate has shown enhanced efficacy compared to either agent alone 1, 5
• In a 52-week study, 69-74% of patients treated with calcipotriene 0.005% plus betamethasone 0.064% once or twice daily achieved clear or almost clear status compared with 27% of patients treated with vehicle control 1
• For facial psoriasis, calcipotriene combined with hydrocortisone is recommended for 8 weeks 1, 6
• The American Academy of Dermatology recommends adding calcipotriene to standard dose methotrexate therapy for treating moderate to severe psoriasis 1

Treatment Recommendations

• The American Academy of Dermatology-National Psoriasis Foundation guidelines support long-term use of topical vitamin D analogues (including calcipotriene) for up to 52 weeks for treating mild to moderate psoriasis 6
• For maintenance therapy, a regimen of vitamin D analogues twice daily on weekdays combined with high-potency topical corticosteroids twice daily on weekends can be considered 6
• For scalp psoriasis, calcipotriene foam and calcipotriene plus betamethasone dipropionate gel is recommended for 4-12 weeks 1

Safety Considerations and Precautions

• At recommended doses, systemic effects on calcium metabolism are rare 2
• Calcipotriene should be used with caution in patients with disorders of calcium metabolism or renal disease 6, 2
• Common adverse events include mild and transient local reactions, with irritant dermatitis being most common, especially when applied to the face 7, 8
• No serious adverse events, including striae or hypothalamic-pituitary-adrenal axis suppression, were observed over 52-week treatment periods with calcipotriene 0.005% and betamethasone 0.064% 1

Important Caveats and Interactions

• Simultaneous use of salicylic acid with calcipotriene should be avoided because the acid pH will inactivate calcipotriene and reduce its effectiveness 1, 6
• UVA radiation can decrease the concentration of calcipotriene on the skin; if used with phototherapy, calcipotriene should be applied after the treatment 1, 6
• Thick layers of calcipotriene can block UVB radiation, potentially increasing the minimal erythema dose 1, 6
• Calcipotriene has a corticosteroid-sparing function, making it particularly valuable for long-term management of psoriasis 2