SAR of a series of inhaled A(2A) agonists and comparison of inhaled pharmacokinetics in a preclinical model with clinical pharmacokinetic data.
Mantell SJ, Stephenson PT, Monaghan SM, Maw GN, Trevethick MA, Yeadon M, Walker DK, Selby MD, Batchelor DV, Rozze S, Chavaroche H, Lemaitre A, Wright KN, Whitlock L, Stuart EF, Wright PA, Macintyre F.
COPD is a major cause of mortality in the western world. A(2A) agonists are postulated to reduce the lung inflammation that causes COPD. The cardiovascular effects of A(2A) agonists dictate that a compound needs to be delivered by inhalation to be therapeutically useful. The pharmacological and pharmacokinetic SAR of a series of inhaled A(2A) agonists is described leading through to human pharmacokinetic data for a clinical candidate.