Development of an Oral Analgesic for Neuropathic Pain

慢性疼痛是一种使人虚弱的健康状况，目前现有的治疗方法还不足以治疗这种疾病。那里 越来越需要开发替代方案来治疗慢性疼痛，特别是糖尿病神经病变 在全球范围内正在增加，50%的糖尿病患者会发生痛性神经病变。最近，这项工作的重要性 脂类作为信号媒介及其在伤害性感受中的功能意义已被阐明。环氧脂肪 细胞色素P450产生的酸性代谢物介导镇痛，我们已经合成了小分子 他们的代谢酶的抑制剂，可溶性环氧化物水解酶(SEH)，以提高他们在体内的水平。使用 我们的目标是开发一种新的、安全的sEH口服抑制剂，用于治疗周围神经病 在糖尿病患者中。我们的候选药物EC5026的临床前研究表明，其疗效超过了目前的水平 糖尿病神经病变的治疗方法。基于疗效、良好的PK/ADME特性和稳定性，EicOsis具有 选择EC5026进入进一步的开发阶段。EicOsis将与Blueprint开发团队合作 制定开发计划并启动研究，以在第一阶段临床试验中测试EC5026的安全性。

Chronic pain is a debilitating health condition that is currently insufficiently treated by available therapies. There is a growing need to develop alternatives to treat chronic pain and specifically diabetic neuropathy as diabetes is increasing worldwide and painful neuropathy occurs in 50% of diabetic patients. Recently, the importance of lipids as signaling mediators and their functional significance in nociception has been elucidated. Epoxy-fatty acid metabolites generated by cytochrome P450s mediate analgesia, and we have synthesized small molecule inhibitors of their metabolizing enzyme, the soluble epoxide hydrolase (sEH), to elevate their levels in vivo. With this proposal, we aim to develop a novel and safe oral inhibitor of sEH for the treatment of peripheral neuropathy in diabetic patients. Preclinical studies with our candidate, EC5026, demonstrate efficacy that exceeds current therapies for diabetic neuropathy. Based on efficacy, good PK/ADME properties and stability, EicOsis has selected EC5026 to enter further development stages. EicOsis will work with Blueprint Development Teams to create a development plan and initiate studies to test the safety of EC5026 in Phase 1 clinical trials.