Movement to the Clinic of Soluble Epoxide Hydrolase Inhibitor EC5026 as an Analgesic for Neuropathic Pain and for Use as a Nonaddictive Opioid Alternative
Bruce D. Hammock, Cindy B. McReynolds, Karen Wagner, Alan R. Buckpitt, Irene Cortés‐Puch, Glenn Croston, Kin Sing Stephen Lee, Jun Yang, W. Schmidt, Sung Hee Hwang
Abstract
and confers beneficial effects. This mechanism addresses disease states by shifting endoplasmic reticulum stress from promoting cellular senescence and inflammation toward cell survival and homeostasis. We describe the synthesis and optimization of EC5026 and its development through human Phase 1a trials with no drug-related adverse events. Additionally, we outline fundamental work leading to discovery of the analgesic and inflammation-resolving CYP450 branch of the arachidonate cascade.
Topics & Concepts
Epoxide hydrolase 2AnalgesicChemistryInflammationPharmacologyEpoxide hydrolaseNeuropathic painOpioidBiochemistryEnzymeMedicineImmunologyReceptorMicrosomeEicosanoids and Hypertension PharmacologyPharmacogenetics and Drug MetabolismHormonal Regulation and Hypertension