A Comprehensive Monograph on Calcipotriol (DB02300)

Executive Summary & Key Findings

Calcipotriol, known in the United States as calcipotriene, is a synthetic vitamin D analog that has become a cornerstone in the topical treatment of mild to moderate plaque psoriasis. Developed as a small molecule drug, it functions as a selective agonist for the Vitamin D Receptor (VDR), a nuclear transcription factor that plays a critical role in cellular growth and immune function. The primary therapeutic action of Calcipotriol stems from its ability to normalize the pathological processes underlying psoriasis: it inhibits the hyperproliferation of skin cells (keratinocytes) and promotes their proper differentiation, while simultaneously exerting immunomodulatory effects that dampen the localized inflammatory cascade characteristic of the disease.

The pivotal pharmacological feature of Calcipotriol is the successful dissociation of its potent anti-psoriatic effects from the systemic calcemic activity inherent to natural vitamin D3 (calcitriol). While exhibiting an affinity for the VDR comparable to calcitriol, Calcipotriol is over 100 times less potent in its influence on systemic calcium metabolism. This remarkable selectivity, achieved through targeted medicinal chemistry, allows for effective topical treatment with a significantly reduced risk of hypercalcemia, a major dose-limiting toxicity of other vitamin D compounds.