Crisaborole and Apremilast: PDE4 Inhibitors with Similar Mechanism of Action, Different Indications for Management of Inflammatory Skin Conditions

Abstract

Two selective phosphodiesterase-4 (PDE4) inhibitors-viz., crisaborole (Eucrisa ® , Pfizer) and apremilast (Otezla ® , Celgene)-have recently received approval by the United States Food and Drug Administration for the treatment of related but different dermatologic skin conditions (viz., atopic dermatitis and plaque psoriasis, respectively). The purpose of this review is to summarize the underlying biochemistry and pathophysiology associated with these dermatologic conditions, review the chemistry, pharmacology and safety of each of these products, and present preclinical and clinical evidence that may help explain why these two PDE4 inhibitors offer new treatment options for these skin conditions.

Influence of heat processing on the anti-inflammatory activity of fresh Smilax glabra based on PDE4 inhibition

“…Generally, the larger the IC 50 value, the weaker enzyme inhibition ability ( Brooks et al, 2012 ). In this study, PDE4 inhibitor Apremilast was used as positive control with an IC 50 value of 43.35 nM ( Table 3 ), which was similar to previous report ( Kitzen et al, 2018 ). Four astilbin isomers showed varying degrees of PDE4 inhibition capacity, among which astilbin had the lowest IC 50 value (14.44 μM), followed by neoastilbin (43.03 μM), neoisoastilbin (103.28 μM) and isoastilbin (129.57 μM).…”