Characterization of LY2775240, a selective phosphodiesterase‐4 inhibitor, in nonclinical models and in healthy subjects

• Published in: Clinical and translational science Vol. 14; no. 3; pp. 1037 - 1048
• Main Authors: Patel, Dipak R., Urva, Shweta, Ho, Stephen, Buckman, Cody J., Ma, Yanfei, Lim, Jean, Sissons, Sean E., Zuniga, Mary S., Philips, Diane, Cox, Karen, Dairaghi, Daniel J.
• Format: Journal Article
• Language: English
• Published: United States John Wiley & Sons, Inc 01.05.2021; John Wiley and Sons Inc; Wiley
• Subjects: Administration, Oral; Adult; Adverse events; Animals; Autoimmune diseases; Cross-Over Studies; Cyclic Nucleotide Phosphodiesterases, Type 4 - metabolism; Cytokines; Dermatitis; Diarrhea; Disease; Dosage; Drug dosages; Drug Evaluation, Preclinical; Drugs, Investigational - pharmacology; Drugs, Investigational - therapeutic use; Enzyme Assays; Enzymes; Female; Healthy Volunteers; Humans; Immune response; Inflammatory diseases; Macaca mulatta; Male; Mice; Middle Aged; Monoclonal antibodies; Nausea; Pharmacodynamics; Pharmacokinetics; Phosphodiesterase; Phosphodiesterase 4 Inhibitors - pharmacology; Phosphodiesterase 4 Inhibitors - therapeutic use; Phosphodiesterase IV; Plasma; Psoriasis; Psoriasis - drug therapy; Rheumatoid arthritis; Thalidomide - analogs & derivatives; Thalidomide - pharmacology; Thalidomide - therapeutic use; Tumor necrosis factor-α; United States > US; Indianapolis Indiana

LY2775240 is a highly selective, potent and orally‐administered inhibitor of phosphodiesterase 4 (PDE4), and is being investigated as a treatment option for inflammatory disorders, such as psoriasis. LY2775240 was investigated in rodent and rhesus monkey nonclinical models. Treatment with LY2775240...