LY2775240

LY2775240 is a highly selective, potent, and orally administered small molecule inhibitor of phosphodiesterase 4 (PDE4). It is being developed as a treatment option for inflammatory disorders, such as psoriasis. By inhibiting PDE4, LY2775240 increases intracellular cyclic adenosine monophosphate (cAMP) levels in immune cells, leading to reduced production of pro-inflammatory cytokines like TNFα. In preclinical models and early-phase clinical trials in healthy volunteers, LY2775240 demonstrated significant reductions in TNFα production and was well-tolerated with common adverse events including nausea, diarrhea, and headache. The drug has shown greater potency than apremilast (another PDE4 inhibitor) in ex vivo assays. Its pharmacokinetic profile supports once-daily oral dosing[1][2][3][4][7].