LX9211 (BMS-9861761) is a highly selective, CNS-penetrable, and potent AAK1 inhibitor with IC50 of 2.0 nM.
BMS-986176 showed excellent efficacy in two rodent neuropathic pain models and excellent central nervous system (CNS) penetration and target engagement at the spinal cord with an average brain to plasma ratio of 20 in rat.
BMS-986176 exhibited favorable physicochemical and pharmacokinetic properties, had an acceptable preclinical toxicity profile
BMS-986176 has completed phase I trials with good human pharmacokinetics and minimum adverse events and is currently in phase II clinical trials for diabetic peripheral neuropathic pain.
