PF-05089771

PF-05089771 is a potent and selective, peripherally restricted small-molecule inhibitor of the voltage-gated sodium channel Nav1.7 (encoded by SCN9A), developed by Pfizer as a novel analgesic for the treatment of acute and chronic pain conditions[1][4][5]. It exhibits high selectivity for Nav1.7 over other sodium channels, with an IC50 value of approximately 0.011 μM in humans[1][6]. The drug has been investigated in clinical trials for indications such as dental pain following third molar extraction, diabetic painful neuropathy (DPN), osteoarthritis knee pain, and inherited erythromelalgia[3][4][5]. Despite promising preclinical data and good tolerability in humans, efficacy results in phase II trials were modest or not statistically significant compared to placebo for painful DPN[3][7]. Its mechanism of action involves blocking the Nav1.7 channel on sensory neurons, thereby reducing neuronal excitability associated with pain signaling[1].

Other names

Nav1.7 blockerNav-1.7 blockerNav 1.7 blockerSCN9A blockerSCN-9A blockerSCN 9A blockerVoltage-gated sodium channel 1.7 blocker