PF-05186462

PF-05186462 is a potent and selective small molecule inhibitor of the human Nav1.7 voltage-gated sodium channel, with an IC50 of 21 nM. Nav1.7 (Sodium channel protein type IX alpha subunit) is highly expressed in pain-sensing nerve fibers and plays a critical role in the perception and transmission of pain signals. By inhibiting this channel, PF-05186462 was developed as a potential analgesic for the treatment of acute or chronic pain conditions. The drug was investigated by Pfizer in early-phase clinical trials to assess its pharmacokinetics via both oral and intravenous administration in healthy volunteers[1][2][8]. However, development was discontinued after phase 1 due to insufficient efficacy compared to other candidates[9].