FDA approved PDE4 inhibitor roflumilast for atopic dermatitis

On July 9th, 2024, the U.S. FDA approved Arcutis Biotherapeutics' ZORYVE ® (roflumilast) for treating atopic dermatitis (AD), the most common type of eczema affecting millions in the U.

S. This once-daily, steroid-free cream could become a new standard of care for AD. The approval underscores the growing importance of researching Phosphodiesterase 4 (PDE4) and other PDEs as immunomodulatory targets for various inflammatory diseases.

Sino Biological, and its subsidiary SignalChem Biotech, support drug discovery and development targeting PDEs by providing a broad range of PDE families and isoforms. Roflumilast is a phosphodiesterase-4 (PDE4) inhibitor that reduces inflammation by increasing cyclic adenosine monophosphate (cAMP) levels, an important molecule in regulating inflammation. PDE4, which breaks down cAMP, has four subtypes (PDE4A, PDE4B, PDE4C, PDE4D) and about 20 isoforms.

The anti-inflammatory effects of PDE4 inhibitors are mainly due to inhibiting PDE4B and PDE4D, which are highly expressed in immune cells. By inhibiting these subtypes, roflumilast raises cAMP levels, decreasing pro-inflammatory mediators (e.g.

, TNF alpha, IL-4, IL-5, IL-13, IL-17A, IL-17F, IL-22) and increasing the anti-inflammatory mediator IL-10. This helps manage inflammatory conditions like atopic dermatitis, alleviating symptoms such as redness, itching, and swelling. PDE enzymes control essential body functions by managing cAMP and cGMP levels.

Various PDE inhibitors are developed for disease.