- Samirao A, Berry TM, Goreshi R, Simpson EL. A pilot study of an oral phosphodiesterase inhibitor (apremilast) for atopic dermatitis in adults. Arch Dermatol 2012;148(8):890–7.
- Li H, Zuo J, Tang W. Phosphodiesterase-4 Inhibitors for the Treatment of Inflammatory Diseases. Front Pharmacol 2018;9:1048.
- Konrad FM, Bury A, Schick MA, et al. The unrecognized effects of phosphodiesterase 4 on epithelial cells in pulmonary inflammation. PLoS ONE 2015;10(4):e0121725.
- Peter D, Jin SL, Conti M, et al. Differential expression and function of phosphodiesterase 4 (PDE4) subtypes in human primary CD4+ T cells: predominant role of PDE4D. J Immunol 2007;178(8):4820–31.
- Schafer PH, Truzzi F, Parton A, et al. Phosphodiesterase 4 in inflammatory diseases: Effects of apremilast in psoriatic blood and in dermal myofibroblasts through the PDE4/CD271 complex. Cell Signal 2016;28(7):753–63.
- Conteras S, Milara J, Morcillo E, Cortijo J. Selective Inhibition of Phosphodiesterases 4A, B, C and D Isoforms in Chronic Respiratory Diseases: Current and Future Evidences. Curr Pharm Des 2017;23(14):2073–83.
Orismilast pharmacology
Key messages
- Orismilast is a highly selective PDE4i, with no or negligible activity against the other 10 PDEs.
- Compared to apremilast, orismilast is a more potent inhibitor of PDE subtypes relevant for inflammation.
- Orismilast also inhibits TNFα secretion more potently than apremilast in PBMC and whole blood.
- Preclinical findings demonstrate orismilast is a potent inhibitor of PDE4 subtypes involved in inflammatory signaling cascades associated with chronic inflammatory diseases.