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CP671305 is a potent, orally active, selective inhibitor of phosphodiesterase-4-D, and possesses high activities.

CP-671,305 is identified as a substrate of MRP2 and BCRP, but not MDR1. CP-671,305 is a substrate of human OATP2B1 with a high affinity (Km=4 uM) but not a substrate for human OATP1B1 or OATP1B3. CP-671,305 displays high affinity (Km=12 uM) for rat hepatic Oatp1a4[1]. CP-671,305 does not exhibit competitive inhibition of the five major cytochrome P450 enzymes, namely CYP1A2, 2C9, 2C19, 2D6 and 3A4 (IC50s > 50 uM). Likewise, no time-dependent inactivation of the five major cytochrome P450 enzymes is discernible with CP-671,305[2].

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