Therapeutic potential and mechanism of action of Crisaborole

Introduction to Crisaborole

Crisaborole is a topical phosphodiesterase-4 (PDE-4) inhibitor that was approved in 2016 for the treatment of mild to moderate atopic dermatitis (AD) in adults and children over the age of 2.

Mechanism of action

It functions topically as a selective phosphodiesterase-4 (PDE-4) inhibitor, thereby increasing intracellular levels of cyclic adenosine monophosphate, which in turn results in downstream changes in the levels of several inflammatory cytokines. Specifically, in vitro studies have shown that crisaborole reduces secretion of interferon (IFN)-γ, tumor necrosis factor-α, interleukin (IL)-2, IL-4, IL-5, IL-13, and IL-17.

Crisaborole for other diseases

Crisaborole may prove to be an effective treatment option for both facial and nonfacial vitiligo given its small molecular size, rapid systemic metabolization, and shared mechanism of action with apremilast. Early clinical studies have shown that crisaboroleate reduces the progression of vitiligo lesions and induces repigmentation, but the paucity of evidence suggests that larger sample sizes and longer-term observations are needed^[1].

References:

[1] MAKINSCAITLYN; GrewalParbeer S ;SangheraRavina. Off-Label Therapeutic Potential of Crisaborole.[J]. Journal of Cutaneous Medicine and Surgery, 2020, 24 3: 292-296. DOI:10.1177/1203475420909794.