Development of a Soluble Epoxide Hydrolase Inhibitor to Spare or Replace Opioid Analgesics

总结/摘要 EicOsis正在开发一种一流的止痛药，对神经性疼痛有效， 替代和剂量备用阿片类药物，从而预防阿片类药物使用障碍（OUD）。的目标 小分子抑制剂EC 5026是可溶性环氧化物水解酶，一种主要的调节酶 其调节内源性生物活性脂质的活性。EC 5026的开发是 目前正在进行中，正在进行IND申请，并准备在以下方面产生重大影响： 治疗人类的慢性疼痛在本提案中，我们概述了以下目标： EC 5026的临床人体临床试验以及其他临床前研究， 在人类中最常见的慢性疼痛病症模型中的有效性 用阿片类药物治疗此外，我们提出了详细的药代动力学，代谢和 将为高级临床试验提供所需信息的分销研究 在人体内检测疗效。我们还建议优化配方以满足这些需求。 所有这些目标都是为了满足2年里程碑（UG 3）并持续到 随着这些里程碑的实现，开发（UH 3）中的下一个计划步骤。Eicosis会议 目前的发展目标和EC 5026是很好的定位，以满足迫切需要减少 阿片类药物的使用，因为即使给予最新的策略，以治疗疼痛与多模式 药物是治疗疼痛的基础。EC 5026代表了首次 类镇痛药，不是阿片类药物，也不是NSAID，但可有效缓解慢性疼痛。 神经性疼痛

Summary/Abstract EicOsis is developing a first-in-class analgesic with efficacy against neuropathic pain that will replace and dose spare opioids and thus prevent opioid use disorders (OUDs). The target of the small molecule inhibitor EC5026 is the soluble epoxide hydrolase, a master regulatory enzyme that modulates the activity of endogenous bioactive lipids. The development of EC5026 is currently in progress and progressing to an IND filing and is poised to have a high impact in treating chronic pain in humans. In this proposal we outline aims to reach the next steps in clinical human clinical trials with EC5026 as well as additional preclinical studies to expand the efficacy into models of chronic pain conditions presenting in humans which are most frequently treated with opioids. Additionally, we propose detailed pharmacokinetic, metabolism and distribution studies that will provide the required information for advanced clinical trials examining efficacy in humans. We also propose to optimize a formulation to meet these needs. All of these individual aims are structured to meet 2 year milestones (UG3) and continue to the next planned steps in development (UH3) as these milestones are met. EicOsis is meeting current development goals and EC5026 is well positioned to meet the urgent need of reducing opioid use because even given the updated strategy to treating pain with multimodal approaches, pharmaceuticals are the foundation of treating pain. EC5026 represents a first-in- class analgesic that is not an opioid nor a NSAID but offers effective pain relief for chronic neuropathic pain.