Tofimilast (CP-325366) is a potent, selective PDE4 inhibitor with IC50 of 23, 13 and 13 nM for PDE4A, PDE4B, and PDE4D, respectively.
Tofimilast (CP-325366) shows weakly or no inhibition for PDE4C, and no activity for PDE1, PDE2, PDE3, PDE5, PDE6, and PDE7.
Tofimilast (CP-325366) increases cAMP levels in PGE1-stimulated U937 cells with an EC50 of 230 nM, inhibits human monocyte PDE mediated cAMP catabolism with an IC50 of 67 nM and LPS stimulated human monocyte TNFα release with an IC50 of 59 nM.
Tofimilast (CP-325366) shows low oral bioavailability and no emesis-associated behaviors in the ferret emesis model.
