Metabolic stability of LASSBio-1632 in rat liver microsome

Asthma is the most common inflammatory disease of the lungs. The prevalence of asthma is increasing in the world representing a substantial global health and economic burden. The inhibition of phosphodiesterase 4 are considered a promise therapeutic strategy to treat asthma. Recently, our group identified the prototype LASSBio-1632 as a new PDE-4 inhibitor equipotent to rolipram. Besides its favorable pharmacodynamic activity, none information about its pharmacokinetic profile are already studied. Therefore, in this abstract we described the studies to determine LASSBio-1632 metabolic stability, using rat liver microsomes. Until the moment, LASSBio-1632 solubility and chemical stability were performed, the analytical methodology was defined, microsomes were prepared and validated. The preliminary results revealed that LASSBio-1632 was was rapidly metabolized, resulting in the generation of two major metabolites (M1 and M2).